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Design and synthesis of potent, selective, and orally active fluorine-containing renin inhibitors Annette M. Doherty, Ila Sircar, Brian E. Kornberg, John Quin, III, R. Thomas Winters, James S. Kaltenbronn, Michael D. Taylor, Brian L. Batley, Stephen R. Rapundalo, and et al. pp 2 - 14; DOI: 10.1021/jm00079a001 |
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Muscarinic activity of the thiolactone, lactam, lactol, and thiolactol analogs of pilocarpine and a hypothetical model for the binding of agonists to the M1 receptor Gideon Shapiro, P. Floersheim, J. Boelsterli, R. Amstutz, G. Bolliger, H. Gammenthaler, G. Gmelin, P. Supavilai, and M. Walkinshaw pp 15 - 27; DOI: 10.1021/jm00079a002 |
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Structure-antigastrin activity relationships of new (R)-4-benzamido-5-oxopentanoic acid derivatives Francesco Makovec, Walter Peris, Laura Revel, Roberto Giovanetti, Laura Mennuni, and Lucio C. Rovati pp 28 - 38; DOI: 10.1021/jm00079a003 |
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Synthesis, characterization, and biological evaluation of a novel class of N-(arylethyl)-N-alkyl-2-(1-pyrrolidinyl)ethylamines: structural requirements and binding affinity at the .sigma. receptor Brian R. De Costa, Lilian Radesca, Lisa Di Paolo, and Wayne D. Bowen pp 38 - 47; DOI: 10.1021/jm00079a004 |
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Synthesis, antinociceptive activity and opioid receptor profiles of substituted trans-3-(decahydro- and octahydro-4a-isoquinolinyl)phenols Duncan B. Judd, Dearg S. Brown, Jane E. Lloyd, Andrew B. McElroy, David I. C. Scopes, Phillip J. Birch, Ann G. Hayes, and Michael J. Sheehan pp 48 - 56; DOI: 10.1021/jm00079a005 |
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Di- and triester prodrugs of the varicella-zoster antiviral agent 6-methoxypurine arabinoside Lynda A. Jones, Allan R. Moorman, Stanley D. Chamberlain, Paulo De Miranda, David J. Reynolds, Charlene L. Burns, and Thomas A. Krenitsky pp 56 - 63; DOI: 10.1021/jm00079a006 |
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Total synthesis of uracil analogs of sinefungin Derek H. R. Barton, Stephane D. Gero, Francoise Lawrence, Malka Robert-Gero, Beatrice Quiclet-Sire, and Mohammad Samadi pp 63 - 67; DOI: 10.1021/jm00079a007 |
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(.+-.)-3-Allyl-7-halo-8-hydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines as selective high affinity D1 dopamine receptor antagonists: synthesis and structure-activity relationship Nandkishore Baindur, Mai Tran, Hyman B. Niznik, H. C. Guan, Phillip Seeman, and John L. Neumeyer pp 67 - 72; DOI: 10.1021/jm00079a008 |
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Synthesis and biological activity of new dimers in the 7H-pyrido[4,3-c]carbazole antitumor series C. Garbay-Jaureguiberry, M. C. Barsi, A. Jacquemin-Sablon, J. B. Le Pecq, and B. P. Roques pp 72 - 81; DOI: 10.1021/jm00079a009 |
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Oxidation chemistry and biochemistry of the central mammalian alkaloid 1-methyl-6-hydroxy-1,2,3,4-tetrahydro-.beta.-carboline Fa Zhang, R. N. Goyal, C. LeRoy Blank, and Glenn Dryhurst pp 82 - 93; DOI: 10.1021/jm00079a010 |
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Synthesis and antibacterial activity of new tetracyclic quinolone antibacterials Masahiro Taguchi, Hirosato Kondo, Yoshimasa Inoue, Yoshihiro Kawahata, Yoshikazu Jinbo, Fumio Sakamoto, and Goro Tsukamoto pp 94 - 99; DOI: 10.1021/jm00079a011 |
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Synthesis, specificity, and antifungal activity of inhibitors of the Candida albicans .DELTA.24-sterol methyltransferase Mark A. Ator, Stanley J. Schmidt, Jerry L. Adams, Roland E. Dolle, Lawrence I. Kruse, Carrie L. Frey, and Janice M. Barone pp 100 - 106; DOI: 10.1021/jm00079a012 |
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Heterocyclic excitatory amino acids. Synthesis and biological activity of novel analogs of AMPA Ulf Madsen and Erik H. F. Wong pp 107 - 111; DOI: 10.1021/jm00079a013 |
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Decorporation of aged americium deposits by oral administration of lipophilic polyamino carboxylic acids Fred W. Bruenger, Gabriela Kuswik-Rabiega, and Scott C. Miller pp 112 - 118; DOI: 10.1021/jm00079a014 |
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Synthesis and biological activities of fatty acid conjugates of a cyclic lactam .alpha.-melanotropin Fahad Al-Obeidi, Victor J. Hruby, Nader Yaghoubi, Mohamed M. Marwan, and Mac E. Hadley pp 118 - 123; DOI: 10.1021/jm00079a015 |
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Conformationally restrained analogs of pravadoline: nanomolar potent, enantioselective, (aminoalkyl)indole agonists of the cannabinoid receptor Thomas E. D'Ambra, Kimberly G. Estep, Malcolm R. Bell, Michael A. Eissenstat, Kurt A. Josef, Susan J. Ward, Dean A. Haycock, Eugene R. Baizman, Frances M. Casiano, and et al. pp 124 - 135; DOI: 10.1021/jm00079a016 |
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2.beta.-Substituted analogs of cocaine. Synthesis and inhibition of binding to the cocaine receptor Anita H. Lewin, Yigong Gao, Philip Abraham, John W. Boja, Michael J. Kuhar, and F. Ivy Carroll pp 135 - 140; DOI: 10.1021/jm00079a017 |
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N-Modified analogs of cocaine: synthesis and inhibition of binding to the cocaine receptor Philip Abraham, J. Bruce Pitner, Anita H. Lewin, John W. Boja, Michael J. Kuhar, and F. Ivy Carroll pp 141 - 144; DOI: 10.1021/jm00079a018 |
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Synthesis and evaluation of some water-soluble prodrugs and derivatives of taxol with antitumor activity Abraham E. Mathew, Magdalena R. Mejillano, Jyoti P. Nath, Richard H. Himes, and Valentino J. Stella pp 145 - 151; DOI: 10.1021/jm00079a019 |
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Preparation and biological activities of potential vasopressin photoaffinity labels David Barbeau, Sylvain Guay, Witold Neugebauer, and Emanuel Escher pp 151 - 157; DOI: 10.1021/jm00079a020 |
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New conformationally restricted technetium-99m N2S2 complexes as myocardial perfusion imaging agents Yoshiro Ohmomo, Lynn Francesconi, Mei Ping Kung, and Hank F. Kung pp 157 - 162; DOI: 10.1021/jm00079a021 |
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A novel class of cardiotonic agents: synthesis and biological evaluation of 5-substituted 3,6-dihydrothiadiazin-2-ones with cyclic AMP phosphodiesterase inhibiting and myofibrillar calcium sensitizing properties Marie Claire Forest, Philippe Lahouratate, Michel Martin, Guy Nadler, Marie Josee Quiniou, and Richard G. Zimmermann pp 163 - 172; DOI: 10.1021/jm00079a022 |
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Heteroatom analogs of bemoradan: chemistry and cardiotonic activity of 1,4-benzothiazinylpyridazinones Donald W. Combs, Marianne S. Rampulla, James P. Demers, Robert Falotico, and John B. Moore pp 172 - 176; DOI: 10.1021/jm00079a023 |
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Inhibitors of protein kinase C. 1. 2,3-bisarylmaleimides Peter D. Davis, Christopher H. Hill, Geoffrey Lawton, John S. Nixon, Sandra E. Wilkinson, Steven A. Hurst, Elizabeth Keech, and Susan E. Turner pp 177 - 184; DOI: 10.1021/jm00079a024 |
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Phenylalkyl isothiocyanate-cysteine conjugates as glutathione S-transferase stimulating agents Guo Qiang Zheng, Patrick M. Kenney, and Luke K. T. Lam pp 185 - 188; DOI: 10.1021/jm00079a025 |
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Syntheses of 5-HT2 antagonist activity of bicyclic 1,2,4-triazol-3(2H)-one and 1,3,5-triazine-2,4(3H)-dione derivatives Yoshifumi Watanabe, Hiroyuki Usui, Shozo Kobayashi, Hirotaka Yoshiwara, Toshiro Shibano, Tsuyoshi Tanaka, Yoshiyuki Morishima, Megumi Yasuoka, and Munefumi Kanao pp 189 - 194; DOI: 10.1021/jm00079a026 |
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Synthesis, stability, and biological evaluation of water-soluble prodrugs of a new echinocandin lipopeptide. Discovery of a potential clinical agent for the treatment of systemic candidiasis and Pneumocystis carinii pneumonia (PCP) James M. Balkovec, Regina M. Black, Milton L. Hammond, James V. Heck, Robert A. Zambias, George Abruzzo, Ken Bartizal, Helmut Kropp, Charlotte Trainor, and et al. pp 194 - 198; DOI: 10.1021/jm00079a027 |
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Potent non-6-fluoro-substituted quinolone antibacterials: synthesis and biological activity Benoit Ledoussal, Daniel Bouzard, and Evangelos Coroneos pp 198 - 200; DOI: 10.1021/jm00079a028 |
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Crystal structure of nevirapine, a non-nucleoside inhibitor of HIV-1 reverse transcriptase, and computational alignment with a structurally diverse inhibitor Philip W. Mui, Stephen P. Jacober, Karl D. Hargrave, and Julian Adams pp 201 - 202; DOI: 10.1021/jm00079a029 |
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Editorial - Communications to the Editor: A Vehicle for the Rapid Publication of Reports of Unusual Significance and Comtemporary Interest. Philip S. Portoghese pp 1 - 1; DOI: 10.1021/jm00079a600 |
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Stereoselective LSD-like activity in d-lysergic acid amides of R- and S-2-aminobutane Robert Oberlender, Robert C. Pfaff, Michael P. Johnson, Xuemei Huang, and David E. Nichols pp 203 - 211; DOI: 10.1021/jm00080a001 |
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The three binding domain model of adenosine receptors: molecular modeling aspects Michael J. Dooley and Ronald J. Quinn pp 211 - 216; DOI: 10.1021/jm00080a002 |
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Inactivation of calpain by peptidyl fluoromethyl ketones Herbert Angliker, John Anagli, and Elliott Shaw pp 216 - 220; DOI: 10.1021/jm00080a003 |
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Structure-function studies in a series of carboxyl-terminal octapeptide analogs of anaphylatoxin C5a Megumi Kawai, David A. Quincy, Benjamin Lane, Karl W. Mollison, Yat Sun Or, Jay R. Luly, and George W. Carter pp 220 - 223; DOI: 10.1021/jm00080a004 |
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Preparation and opioid activity of analogs of the analgesic dipeptide 2,6-dimethyl-L-tyrosyl-N-(3-phenylpropyl)-D-alaninamide Nizal S. Chandrakumar, Peter K. Yonan, Awilda Stapelfeld, Michael Savage, Elaine Rorbacher, Patricia C. Contreras, and Donna Hammond pp 223 - 233; DOI: 10.1021/jm00080a005 |
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.beta.-Proline analogs as agonists at the strychnine-sensitive glycine receptor Graham Johnson, James T. Drummond, Peter A. Boxer, and Robert F. Bruns pp 233 - 241; DOI: 10.1021/jm00080a006 |
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Nucleosides and nucleotides. 103. 2-Alkynyladenosines: a novel class of selective adenosine A2 receptor agonists with potent antihypertensive effects Akira Matsuda, Misao Shinozaki, Toyofumi Yamaguchi, Hiroshi Homma, Rie Nomoto, Tadashi Miyasaka, Yohko Watanabe, and Toichi Abiru pp 241 - 252; DOI: 10.1021/jm00080a007 |
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Substituted 4,6-diaminoquinolines as inhibitors of C5a receptor binding Thomas J. Lanza, Philippe L. Durette, Thomas Rollins, Salvatore Siciliano, Dana N. Cianciarulo, Sumire V. Kobayashi, Charles G. Caldwell, Martin S. Springer, and William K. Hagmann pp 252 - 258; DOI: 10.1021/jm00080a008 |
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Potential antitumor agents. 64. Synthesis and antitumor evaluation of dibenzo[1,4]dioxin-1-carboxamides: a new class of weakly binding DNA-intercalating agents Ho H. Lee, Brian D. Palmer, Maruta Boyd, Bruce C. Baguley, and William A. Denny pp 258 - 266; DOI: 10.1021/jm00080a009 |
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Synthesis and antitumor activity of tropolone derivatives. 7. Bistropolones containing connecting methylene chains Masatoshi Yamato, Junko Ando, Katsuhito Sakaki, Kuniko Hashigaki, Yusuke Wataya, Shigeru Tsukagoshi, Tazuko Tashiro, and Takashi Tsuruo pp 267 - 273; DOI: 10.1021/jm00080a010 |
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A new, general synthetic route to multidentate N,S ligands for use in technetium-99m radiopharmaceuticals. Preparation of diamido disulfur, diamino dithiol, and tripodal N3S3 prototypes. Comparative biodistributions of [99mTcVO-DADS]- analogs which contain 5,5,5- and 5,7,5-membered chelate ring systems Danuta Stepniak-Biniakiewicz, Baohe Chen, and Edward Deutsch pp 274 - 279; DOI: 10.1021/jm00080a011 |
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Synthesis and evaluation of radioiodinated 2-(2(RS)-aminopropyl)-5-iodothiophenes as brain imaging agents Mark M. Goodman, George W. Kabalka, Ronald C. Marks, F. F. Knapp, J. Lee, and Y. Liang pp 280 - 285; DOI: 10.1021/jm00080a012 |
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Phenyl-substituted analogs of oxotremorine as muscarinic antagonists Bjoern M. Nilsson, Hugo M. Vargas, Bjoern Ringdahl, and Uli Hacksell pp 285 - 294; DOI: 10.1021/jm00080a013 |
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Synthesis and muscarinic activity of quinuclidinyl- and (1-azanorbornyl)pyrazine derivatives Leslie J. Street, Raymond Baker, Tracey Book, Austin J. Reeve, John Saunders, Timothy Willson, Rosemarie S. Marwood, Shailendra Patel, and Stephen B. Freedman pp 295 - 305; DOI: 10.1021/jm00080a014 |
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Conformational studies of muscarone analogs: x-ray analysis and molecular mechanics calculations Patrick J. Carroll, Marco De Amici, Carlo De Micheli, and Lucio Toma pp 305 - 309; DOI: 10.1021/jm00080a015 |
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Zatosetron, a potent, selective, and long-acting 5HT3 receptor antagonist: synthesis and structure-activity relationships David W. Robertson, William B. Lacefield, William Bloomquist, William Pfeifer, Richard L. Simon, and Marlene L. Cohen pp 310 - 319; DOI: 10.1021/jm00080a016 |
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Synthesis and antifolate properties of 5,10-ethano-5,10-dideazaaminopterin Joseph I. DeGraw, Pamela H. Christie, William T. Colwell, and Francis M. Sirotnak pp 320 - 324; DOI: 10.1021/jm00080a017 |
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New neplanocin analogs. 1. Synthesis of 6'-modified neplanocin A derivatives as broad-spectrum antiviral agents Satoshi Shuto, Takumi Obara, Minoru Toriya, Mitsuaki Hosoya, Robert Snoeck, Graciela Andrei, Jan Balzarini, and Erik De Clercq pp 324 - 331; DOI: 10.1021/jm00080a018 |
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Synthesis and antifolate evaluation of the 10-propargyl derivatives of 5-deazafolic acid, 5-deazaaminopterin, and 5-methyl-5-deazaaminopterin J. R. Piper, N. D. Malik, M. S. Rhee, J. Galivan, and F. M. Sirotnak pp 332 - 337; DOI: 10.1021/jm00080a019 |
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Structure-activity relationships of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine analogs: effect of substitutions at the C-6 phenyl ring and at the C-5 position on anti-HIV-1 activity Hiromichi Tanaka, Hideaki Takashima, Masaru Ubasawa, Kouichi Sekiya, Issei Nitta, Masanori Baba, Shiro Shigeta, Richard T. Walker, Erik De Clercq, and Tadashi Miyasaka pp 337 - 345; DOI: 10.1021/jm00080a020 |
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Structure-function studies of peptides inhibiting the ribonucleotide reductase activity of herpes simplex virus type I Pierrette Gaudreau, Paul Brazeau, Manon Richer, Jean Cormier, Daniel Langlois, and Yves Langelier pp 346 - 350; DOI: 10.1021/jm00080a021 |
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Bis basic substituted diaminobenzobisthiazoles as potential antiarthritic agents Ernest Cullen, Reinhold Becker, Kurt Freter, Thelma LeClerq, Genus Possanza, and Hin Chor Wong pp 350 - 361; DOI: 10.1021/jm00080a022 |
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New 8-(trifluoromethyl)-substituted quinolones. The benefits of the 8-fluoro group with reduced phototoxic risk J. P. Sanchez, A. J. Bridges, R. Bucsh, J. M. Domagala, R. D. Gogliotti, S. E. Hagen, C. L. Heifetz, E. T. Joannides, J. C. Sesnie, and et al. pp 361 - 367; DOI: 10.1021/jm00080a023 |
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Synthesis of novel 2-phenyl-2H-pyrazolo[4,3-c]isoquinolin-3-ols: topological comparisons with analogs of 2-phenyl-2,5-dihydropyrazolo[4,3-c]quinolin-3-(3H)-ones at benzodiazepine receptors Michael S. Allen, Phil Skolnick, and James M. Cook pp 368 - 374; DOI: 10.1021/jm00080a024 |
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Synthesis and substance P receptor binding activity of androstano[3,2-b]pyrimido[1,2-a]benzimidazoles Bhaskar R. Venepalli, Lisa D. Aimone, Kenneth C. Appell, Malcolm R. Bell, John A. Dority, Ramanuj Goswami, Patricia L. Hall, Virendra Kumar, Kristine B. Lawrence, and et al. pp 374 - 378; DOI: 10.1021/jm00080a025 |
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Chromophore-modified antineoplastic imidazoacridinones. Synthesis and activity against murine leukemias Wieslaw M. Cholody, Sante Martelli, and Jerzy Konopa pp 378 - 382; DOI: 10.1021/jm00080a026 |
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Synthesis and some pharmacological properties of potent and selective antagonists of the vasopressor (V1-receptor) response to arginine-vasopressin Maurice Manning, Stoytcho Stoev, Krzysztof Bankowski, Aleksandra Misicka, Bernard Lammek, Nga Ching Wo, and Wilbur H. Sawyer pp 382 - 388; DOI: 10.1021/jm00080a027 |
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Structure-activity relationships associated with 3,4,5-triphenyl-1H-pyrazole-1-nonanoic acid, a nonprostanoid prostacyclin mimetic Nicholas A. Meanwell, Michael J. Rosenfeld, J. J. Kim Wright, Catherine L. Brassard, John O. Buchanan, Marianne E. Federici, J. Stuart Fleming, and Steven M. Seiler pp 389 - 397; DOI: 10.1021/jm00080a028 |
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Synthesis and biological activity of 2'-fluoro-2-halo derivatives of 9-.beta.-D-arabinofuranosyladenine John A. Montgomery, Anita T. Shortnacy-Fowler, Sarah D. Clayton, James M. Riordan, and John A. Secrist pp 397 - 401; DOI: 10.1021/jm00080a029 |
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Improvements in the minimum binding sequence of C5a: examination of His-67 Yat Sun Or, Richard F. Clark, Benjamin Lane, Karl W. Mollison, George W. Carter, and Jay R. Luly pp 402 - 406; DOI: 10.1021/jm00080a030 |
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Adenosine receptors: pharmacology, structure-activity relationships, and therapeutic potential Kenneth A. Jacobson, Philip J. M. Van Galen, and Michael Williams pp 407 - 422; DOI: 10.1021/jm00081a001 |
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Effect of N-alkylation on the affinities of analogs of spiperone for dopamine D2 and serotonin 5-HT2 receptors Robert H. Mach, Joseph R. Jackson, Robert R. Luedtke, Kathryn J. Ivins, Perry B. Molinoff, and Richard L. Ehrenkaufer pp 423 - 430; DOI: 10.1021/jm00081a002 |
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Structure and DNA binding activity of analogs of 1,5-bis(4-amidinophenoxy)pentane (pentamidine) Michael Cory, Richard R. Tidwell, and Terri A. Fairley pp 431 - 438; DOI: 10.1021/jm00081a003 |
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2-[(2-Pyridylmethyl)sulfinyl]-1H-thieno[3,4-d]imidazoles. A novel class of gastric H+/K+-ATPase inhibitors Klaus Weidmann, Andreas W. Herling, Hans Jochen Lang, Karl Heinz Scheunemann, Robert Rippel, Hildegard Nimmesgern, Thomas Scholl, Martin Bickel, and Heinz Metzger pp 438 - 450; DOI: 10.1021/jm00081a004 |
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.alpha.-Keto amide inhibitors of aminopeptidases Timothy D. Ocain and Daniel H. Rich pp 451 - 456; DOI: 10.1021/jm00081a005 |
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Potent, orally active aldose reductase inhibitors related to zopolrestat: surrogates for benzothiazole side chain Banavara L. Mylari, Thomas A. Beyer, Pamela J. Scott, Charles E. Aldinger, Michael F. Dee, Todd W. Siegel, and William J. Zembrowski pp 457 - 465; DOI: 10.1021/jm00081a006 |
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Synthesis of halogenated trimetoquinol derivatives and evaluation of their .beta.-agonist and thromboxane A2 (TXA2) antagonist activities K. M. Markovich, V. Tantishaiyakul, A. Hamada, D. D. Miller, K. J. Romstedt, G. Shams, Y. Shin, P. F. Fraundorfer, K. Doyle, and D. R. Feller pp 466 - 479; DOI: 10.1021/jm00081a007 |
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Centrally acting .alpha.1-adrenoceptor agonists based on hexahydronaphth[2,3-b]-1,4-oxazines and octahydrobenzo[g]quinolines Joachim Nozulak, Jean M. Vigouret, Anne L. Jaton, Alfred Hofmann, Anant R. Dravid, Hans P. Weber, Hans O. Kalkman, and Malcolm D. Walkinshaw pp 480 - 489; DOI: 10.1021/jm00081a008 |
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New .kappa.-receptor agonists based upon a 2-[(alkylamino)methyl]piperidine nucleus David I. C. Scopes, Norman F. Hayes, David E. Bays, David Belton, John Brain, Dearg S. Brown, Duncan B. Judd, Andrew B. McElroy, Clive A. Meerholz, and et al. pp 490 - 501; DOI: 10.1021/jm00081a009 |
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A study on the contribution of the 1-phenyl substituent to the molecular electrostatic potentials of some benzazepines in relation to selective dopamine D-1 receptor activity Ingrid Pettersson, Klaus Gundertofte, Jonas Palm, and Tommy Liljefors pp 502 - 507; DOI: 10.1021/jm00081a010 |
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3-Carboxy-5-methyl-N-[4-(trifluoromethyl)phenyl]-4-isoxazolecarboxamide, new prodrug for the antiarthritic agent 2-cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]-2-butenamide John W. Patterson, Paul S. Cheung, and Michael J. Ernest pp 507 - 510; DOI: 10.1021/jm00081a011 |
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Synthesis and cytotoxic activity of C-glycosidic nicotinamide riboside analogs Karsten Krohn, Heidi Heins, and Klaus Wielckens pp 511 - 517; DOI: 10.1021/jm00081a012 |
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Fluoronaphthyridines as antibacterial agents. 4. Synthesis and structure-activity relationships of 5-substituted 6-fluoro-7-(cycloalkylamino)-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acids D. Bouzard, P. Di Cesare, M. Essiz, J. P. Jacquet, B. Ledoussal, P. Remuzon, R. E. Kessler, and J. Fung-Tomc pp 518 - 525; DOI: 10.1021/jm00081a013 |
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Synthesis, antiproliferative, and antiviral activity of certain 4-aminopyrrolo[2,3-d]pyridazine nucleosides: an entry into a novel series of adenosine analogs Eric A. Meade, Linda L. Wotring, John C. Drach, and Leroy B. Townsend pp 526 - 533; DOI: 10.1021/jm00081a014 |
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Synthesis and anti-HIV activity of 4'-thio-2',3'-dideoxynucleosides John A. Secrist, Robert M. Riggs, Kamal N. Tiwari, and John A. Montgomery pp 533 - 538; DOI: 10.1021/jm00081a015 |
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Synthesis and biological activity of certain alkyl 5-(alkoxycarbonyl)-1H-benzimidazole-2-carbamates and related derivatives: a new class of potential antineoplastic and antifilarial agents Siya Ram, Dean S. Wise, Linda L. Wotring, John W. McCall, and Leroy B. Townsend pp 539 - 547; DOI: 10.1021/jm00081a016 |
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.alpha.-Methylated analogs of triiodothyroalkanoic acids: synthesis and biological activity N. Zenker, A. E. Ekpe, and L. S. Hubbard pp 548 - 552; DOI: 10.1021/jm00081a017 |
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Pyrrole Mannich bases as potential antipsychotic agents Malcolm K. Scott, Gregory E. Martin, Deena L. DiStefano, Cynthia L. Fedde, Michael J. Kukla, Donna L. Barrett, William J. Baldy, Robert J. Elgin Jr., James M. Kesslick, and et al. pp 552 - 558; DOI: 10.1021/jm00081a018 |
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Renin inhibitory pentols showing improved enteral bioavailability Heinz Werner Kleemann, Holger Heitsch, Rainer Henning, Werner Kramer, Walter Kocher, Ulrich Lerch, Wolfgang Linz, Wolf Ulrich Nickel, Dieter Ruppert, and et al. pp 559 - 567; DOI: 10.1021/jm00081a019 |
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Base-catalyzed isomerization of retinoic acid. Synthesis and differentiation-inducing activities of 14-alkylated all-trans-, 13-cis-, and 20,14-retro-retinoic acids Hideo Tanaka, Hiroyuki Kagechika, Emiko Kawachi, Hiroshi Fukasawa, Yuichi Hashimoto, and Koichi Shudo pp 567 - 572; DOI: 10.1021/jm00081a020 |
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Multivariate analysis by the minimum spanning tree method of the structural determinants of diphenylethylenes and triphenylacrylonitriles implicated in estrogen receptor binding, protein kinase C activity, and MCF7 cell proliferation Jean Christophe Dore, Jacques Gilbert, Eric Bignon, Andre Crastes de Paulet, Tiiu Ojasoo, Michel Pons, Jean Pierre Raynaud, and Jean Francois Miquel pp 573 - 583; DOI: 10.1021/jm00081a021 |
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Quantitative structure-activity relationship. QSAR, analyses of the substituted indanone and benzylpiperidine rings of a series of indanone-benzylpiperidine inhibitors of acetylcholinesterase Mario G. Cardozo, Youichi Iimura, Hachiro Sugimoto, Yoshiharu Yamanishi, and A. J. Hopfinger pp 584 - 589; DOI: 10.1021/jm00081a022 |
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Conformational analyses and molecular-shape comparisons of a series of indanone-benzylpiperidine inhibitors of acetylcholinesterase Mario G. Cardozo, Takatoshi Kawai, Youichi Iimura, Hachiro Sugimoto, Yoshiharu Yamanishi, and A. J. Hopfinger pp 590 - 601; DOI: 10.1021/jm00081a023 |
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A novel class of enkephalinase inhibitors containing a C-terminal sulfo group Tetsutaro Mimura, Yasuhisa Nakamura, Junko Nishino, Tadahiro Sawayama, Toshio Komiya, Takashi Deguchi, Atsuko Kita, Hideo Nakamura, and Junichi Matsumoto pp 602 - 608; DOI: 10.1021/jm00081a024 |
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Book Reviews pp 609 - 610; DOI: 10.1021/jm00081a600 |
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Synthesis and structure-activity relationships of 7-diazabicycloalkylquinolones, including danofloxacin, a new quinolone antibacterial agent for veterinary medicine Paul R. McGuirk, Martin R. Jefson, Douglas D. Mann, Nancy C. Elliott, Polly Chang, Eugene P. Cisek, C. Peter Cornell, Thomas D. Gootz, Susan L. Haskell, and et al. pp 611 - 620; DOI: 10.1021/jm00082a001 |
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3,4-Dihydroquinolin-2(1H)-ones as combined inhibitors of thromboxane A2 synthase and cAMP phosphodiesterase Gregory R. Martinez, Keith A. M. Walker, Donald R. Hirschfeld, John J. Bruno, Diana S. Yang, and Patrick J. Maloney pp 620 - 628; DOI: 10.1021/jm00082a002 |
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A steric and electrostatic comparison of three models for the agonist/antagonist binding site on the adenosine A1 receptor Eleonora M. Van der Wenden, Adriaan P. IJzerman, and Willem Soudijn pp 629 - 635; DOI: 10.1021/jm00082a003 |
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Decreased histamine release by luteinizing-hormone-releasing-hormone antagonists obtained upon translocation of the cationic amino acid from position 8 to position 7 George Flouret, Kevin Mahan, and Tadeusz Majewski pp 636 - 640; DOI: 10.1021/jm00082a004 |
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Inhibition of human leukocyte elastase (HLE) by N-substituted peptidyl trifluoromethyl ketones Jerry W. Skiles, Victor Fuchs, Clara Miao, Ronald Sorcek, Karl G. Grozinger, Scott C. Mauldin, Jana Vitous, Philip W. Mui, Stephen Jacober, and et al. pp 641 - 662; DOI: 10.1021/jm00082a005 |
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Crystal-structure-based design and synthesis of benz[cd]indole-containing inhibitors of thymidylate synthase Michael D. Varney, Gifford P. Marzoni, Cindy L. Palmer, Judith G. Deal, Stephanie Webber, Katherine M. Welsh, Russell J. Bacquet, Charlotte A. Bartlett, Catharine A. Morse, and et al. pp 663 - 676; DOI: 10.1021/jm00082a006 |
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4-Substituted 2-alkoxytetrahydrofurans as potent and long-lasting PAF antagonists Elena Carceller, Manuel Merlos, Marta Giral, Javier Bartroli, Julian Garcia-Rafanell, and Javier Forn pp 676 - 683; DOI: 10.1021/jm00082a007 |
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Systemic analgesic activity and .delta.-opioid selectivity in [2,6-dimethyl-Tyr1, D-Pen2, D-Pen5]enkephalin Donald W. Hansen, Awilda Stapelfeld, Michael A. Savage, Melvin Reichman, Donna L. Hammond, Ronald C. Haaseth, and Henry I. Mosberg pp 684 - 687; DOI: 10.1021/jm00082a008 |
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Novel anticancer prodrugs of butyric acid. 2 Abraham Nudelman, Margaretta Ruse, Adina Aviram, Ester Rabizadeh, Matityahu Shaklai, Yael Zimrah, and Ada Rephaeli pp 687 - 694; DOI: 10.1021/jm00082a009 |
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Synthesis and structure-activity relationships of acyclic .omega. chain conjugated diene analogs of enisoprost P. W. Collins, R. L. Shone, W. E. Perkins, A. F. Gasiecki, V. J. Kalish, S. W. Kramer, and R. G. Bianchi pp 694 - 704; DOI: 10.1021/jm00082a010 |
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Class III antiarrhythmic activity of novel substituted 4-[(methylsulfonyl)amino]benzamides and sulfonamides John W. Ellingboe, Walter Spinelli, Michael W. Winkley, Thomas T. Nguyen, Roderick W. Parsons, Issam F. Moubarak, Jan M. Kitzen, Donna Von Engen, and Jehan F. Bagli pp 705 - 716; DOI: 10.1021/jm00082a011 |
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Phenothiazines as lipid peroxidation inhibitors and cytoprotective agents Melvin J. Yu, Jefferson R. McCowan, K. Jeff Thrasher, Priscilla T. Keith, Charlotte A. Luttman, Peter P. K. Ho, Richard D. Towner, Barbara Bertsch, J. S. Horng, and et al. pp 716 - 724; DOI: 10.1021/jm00082a012 |
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.alpha.-Methyl polyamines: metabolically stable spermidine and spermine mimics capable of supporting growth in cells depleted of polyamines John R. Lakanen, James K. Coward, and Anthony E. Pegg pp 724 - 734; DOI: 10.1021/jm00082a013 |
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Binding of phenylalkylamine derivatives at 5-HT1C and 5-HT2 serotonin receptors: evidence for a lack of selectivity Richard A. Glennon, Reva Raghupathi, Piotr Bartyzel, Milt Teitler, and Sigrun Leonhardt pp 734 - 740; DOI: 10.1021/jm00082a014 |
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N,N'-disubstituted guanidine high-potency sweeteners George W. Muller, D. Eric Walters, and Grant. E. DuBois pp 740 - 743; DOI: 10.1021/jm00082a015 |
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Synthesis, cardiac electrophysiology, and .beta.-blocking activity of novel arylpiperazines with potential as class II/III antiarrhythmic agents Gary B. Phillips, Thomas K. Morgan, William C. Lumma, Robert P. Gomez, Joan M. Lind, Randall Lis, Thomas Argentieri, and Mark E. Sullivan pp 743 - 750; DOI: 10.1021/jm00082a016 |
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Synthesis and .alpha.-adrenergic activities of 2- and 4-substituted imidazoline and imidazole analogs Yoshiya Amemiya, Seoung S. Hong, Burrah V. Venkataraman, Popat N. Patil, Gamal Shams, Karl Romstedt, Dennis R. Feller, Fu Lian Hsu, and Duane D. Miller pp 750 - 755; DOI: 10.1021/jm00082a017 |
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Benzazepinone calcium channel blockers. 2. Structure activity and drug metabolism studies leading to potent antihypertensive agents. Comparison with benzothiazepinones David M. Floyd, S. David Kimball, John Krapcho, Jagabandhu Das, Chester F. Turk, Robert V. Moquin, Michael W. Lago, Keith J. Duff, Ving G. Lee, and et al. pp 756 - 772; DOI: 10.1021/jm00082a018 |
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Benzazepinone calcium channel blockers. 3. Synthesis and structure-activity studies of 3-alkylbenzazepinones Jagabandhu Das, David M. Floyd, S. David Kimball, Keith J. Duff, Michael W. Lago, Robert V. Moquin, Ving G. Lee, Jack Z. Gougoutas, Vu Chi Truc, and et al. pp 773 - 780; DOI: 10.1021/jm00082a019 |
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Benzazepinone calcium channel blockers. 4. Structure-activity overview and intracellular binding site S. David Kimball, David M. Floyd, Jagabandhu Das, John T. Hunt, John Krapcho, George Rovnyak, Keith J. Duff, Ving G. Lee, Robert V. Moquin, and et al. pp 780 - 793; DOI: 10.1021/jm00082a020 |
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Inhibitors of sterol synthesis. 3.beta.,25-Dihydroxy-5.alpha.-cholest-8(14)-en-15-one, an active metabolite of 3.beta.-hydroxy-5.alpha.-cholest-8(14)-en-15-one Shankar Swaminathan, Frederick D. Pinkerton, and George J. Schroepfer pp 793 - 795; DOI: 10.1021/jm00082a021 |
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Book Reviews pp 796 - 798; DOI: 10.1021/jm00082a600 |
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Novel inhibitors of prolyl 4-hydroxylase Robert I. Dowell and Elizabeth M. Hadley pp 800 - 804; DOI: 10.1021/jm00083a001 |
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Novel inhibitors of prolyl 4-hydroxylase. 2. 5-Amide substituted pyridine-2-carboxylic acids Howard Tucker and Dudley F. Thomas pp 804 - 807; DOI: 10.1021/jm00083a002 |
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Small atrial natriuretic peptide analogs: design, synthesis, and structural requirements for guanylate cyclase activation Thomas W. Von Geldern, Todd W. Rockway, Steven K. Davidsen, Gerald P. Budzik, Eugene N. Bush, Margaret Y. Chu-Moyer, Edward M. Devine Jr., William H. Holleman, Marty C. Johnson, and et al. pp 808 - 816; DOI: 10.1021/jm00083a003 |
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Synthesis and biological action of aminotetrahydroisoquinocarbazoles and related compounds: a new class of compounds with antiarrhythmic activity Yasuo Shimoji, Kuniyuki Tomita, Toshihiko Hashimoto, Fujio Saito, Yasuhiro Morisawa, Hiroshi Mizuno, Ryosuke Yorikane, and Hiroyuki Koike pp 816 - 822; DOI: 10.1021/jm00083a004 |
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New modified heterocyclic phenylalanine derivatives. Incorporation into potent inhibitors of human renin Timothy D. Ocain, David D. Deininger, Ralph Russo, Nancie A. Senko, Alan Katz, Jan M. Kitzen, Robert Mitchell, George Oshiro, Anthony Russo, and et al. pp 823 - 832; DOI: 10.1021/jm00083a005 |
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Synthesis and use of 3-amino-4-phenyl-2-piperidones and 4-amino-2-benzazepin-3-ones as conformationally restricted phenylalanine isosteres in renin inhibitors S. E. De Laszlo, B. L. Bush, J. J. Doyle, W. J. Greenlee, D. G. Hangauer, T. A. Halgren, R. J. Lynch, T. W. Schorn, and P. K. S. Siegl pp 833 - 846; DOI: 10.1021/jm00083a006 |
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Design and synthesis of novel 6,7-imidazotetrahydroquinoline inhibitors of thymidylate synthase using iterative protein crystal structure analysis Siegfried H. Reich, Mary Ann M. Fuhry, Dzuy Nguyen, Mark J. Pino, Katherine M. Welsh, Stephanie Webber, Cheryl A. Janson, Steven R. Jordan, David A. Matthews, and et al. pp 847 - 858; DOI: 10.1021/jm00083a007 |
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Syntheses and thymidylate synthase inhibitory activity of the poly-.gamma.-glutamyl conjugates of N-[5-[N-(3,4-dihydro-2-methyl-4-oxoquinazolin-6-ylmethyl)-N-methylamino]-2-thenoyl]-L-glutamic acid (ICI D1694) and other quinazoline antifolates Graham M. F. Bisset, Krzysztof Pawelczak, Ann L. Jackman, A. Hilary Calvert, and Leslie R. Hughes pp 859 - 866; DOI: 10.1021/jm00083a008 |
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Antitumor agents. 123. Synthesis and human DNA topoisomerase II inhibitory activity of 2'-chloro derivatives of etoposide and 4.beta.-(arylamino)-4'-O-demethylpodophyllotoxins Hong Hu, Su Ying Liu, Yung Chi Cheng, Kuo Hsiung Lee, and Zhe Qing Wang pp 866 - 871; DOI: 10.1021/jm00083a009 |
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Antitumor agents. 124. New 4.beta.-substituted aniline derivatives of 6,7-O,O-demethylene-4'-O-demethylpodophyllotoxin and related compounds as potent inhibitors of human DNA topoisomerase II Zhe-Qing Wang, Hong Hu, Hong-Xin Chen, Yung-Chi Cheng, and Kuo Hsiung Lee pp 871 - 877; DOI: 10.1021/jm00083a010 |
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New nonpeptide angiotensin II receptor antagonists. 1. Synthesis, biological properties and structure-activity relationships of 2-alkylbenzimidazole derivatives Andrew P. Thomas, Christopher P. Allott, Keith H. Gibson, John S. Major, Brian B. Masek, Alec A. Oldham, Arnold H. Ratcliffe, David A. Roberts, Simon T. Russell, and Douglas A. Thomason pp 877 - 885; DOI: 10.1021/jm00083a011 |
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5-(Aminomethyl)-3-aryldihydrofuran-2(3H)-ones, a new class of monoamine oxidase-B inactivators Zhaozhong Ding and Richard B. Silverman pp 885 - 889; DOI: 10.1021/jm00083a012 |
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Analgesic dipeptide derivatives. 7. 3,7-Diamino-2-hydroxyheptanoic acid (DAHHA) containing dipeptide analogs of the analgesic compound H-Lys-Trp(Nps)-OMe Rosario Herranz, Soledad Vinuesa, Concepcion Perez, M. Teresa Garcia-Lopez, Esther Lopez, Maria L. De Ceballos, and Joaquin Del Rio pp 889 - 895; DOI: 10.1021/jm00083a013 |
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Development of high-affinity 5-HT3 receptor antagonists. 1. Initial structure-activity relationship of novel benzamides R. D. Youssefyeh, H. F. Campbell, S. Klein, J. E. Airey, P. Darkes, M. Powers, M. Schnapper, K. Neuenschwander, L. R. Fitzpatrick, and et al. pp 895 - 903; DOI: 10.1021/jm00083a014 |
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Development of high-affinity 5-HT3 receptor antagonists. 2. Two novel tricyclic benzamides Raymond D. Youssefyeh, H. F. Campbell, J. E. Airey, S. Klein, M. Schnapper, M. Powers, R. Woodward, W. Rodriguez, S. Golec, and et al. pp 903 - 911; DOI: 10.1021/jm00083a015 |
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Synthesis and in vitro biological profile of all four isomers of the potent muscarinic agonist 3-(3-methyl-1,2,4-oxadiazol-5-yl)-1-azabicyclo[2.2.1]heptane Graham A. Showell, Raymond Baker, Juliet Davis, Richard Hargreaves, Stephen B. Freedman, Karst Hoogsteen, Shailendra Patel, and Roger J. Snow pp 911 - 916; DOI: 10.1021/jm00083a016 |
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Pyrazole-related nucleosides. Synthesis and antiviral/antitumor activity of some substituted pyrazole and pyrazolo[4,3-d]-1,2,3-triazin-4-one nucleosides Stefano Manfredini, Rita Bazzanini, Pier Giovanni Baraldi, Mario Guarneri, Daniele Simoni, Maria E. Marongiu, Alessandra Pani, Paolo La Colla, and Enzo Tramontano pp 917 - 924; DOI: 10.1021/jm00083a017 |
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8-Polycycloalkyl-1,3-dipropylxanthines as potent and selective antagonists for A1-adenosine receptors Junichi Shimada, Fumio Suzuki, Hiromi Nonaka, and Akio Ishii pp 924 - 930; DOI: 10.1021/jm00083a018 |
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Antiestrogens. 3. Estrogen receptor affinities and antiproliferative effects in MCF-7 cells of phenolic analogs of trioxifene, [3,4-dihydro-2-(4-methoxyphenyl)-1-naphthalenyl][4-[2-(1-pyrrolidinyl)ethoxy]phenyl[methanone Charles D. Jones, Larry C. Blaszczak, Mary E. Goettel, Tulio Suarez, Thomas A. Crowell, Thomas E. Mabry, Peter C. Ruenitz, and V. Srivatsan pp 931 - 938; DOI: 10.1021/jm00083a019 |
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Secondary metabolites by chemical screening. 17. Nigericinol derivatives: synthesis, biological activities and modeling studies Susanne Grabley, Peter Hammann, Robert Klein, Gerhard Seibert, Irvin Winkler, Achim Kroeger, and Frank Ditzel pp 939 - 944; DOI: 10.1021/jm00083a020 |
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Perfluorocarbon-based antidiabetic agents Kenneth L. Kees, Ted M. Smith, Michael L. McCaleb, Dorothy H. Prozialeck, Robert S. Cheeseman, Thomas E. Christos, William C. Patt, and Kurt E. Steiner pp 944 - 953; DOI: 10.1021/jm00083a021 |
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Synthesis and antibacterial activity of some novel 6-methyl- and 6-propenyl-substituted carbapenems Harold Mastalerz, Marcel Menard, Edward Ruediger, and Joan Fung-Tomc pp 953 - 958; DOI: 10.1021/jm00083a022 |
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Novel benzothiophene-, benzofuran-, and naphthalenecarboxamidotetrazoles as potential antiallergy agents David T. Connor, Wiaczeslaw A. Cetenko, Michael D. Mullican, Roderick J. Sorenson, Paul C. Unangst, Robert J. Weikert, Richard L. Adolphson, John A. Kennedy, David O. Thueson, and et al. pp 958 - 965; DOI: 10.1021/jm00083a023 |
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An ethidium analog that binds with high specificity to a base-bulged duplex from the TAR RNA region of the HIV-1 genome Lynda S. Ratmeyer, Ravi Vinayak, Gerald Zon, and W. David Wilson pp 966 - 968; DOI: 10.1021/jm00083a024 |
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Editorial - Subsidizing Color Graphics Philip S. Portoghese pp 799 - 799; DOI: 10.1021/jm00083a600 |
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Cocaine receptor: biochemical characterization and structure-activity relationships of cocaine analogs at the dopamine transporter F. Ivy Carroll, Anita H. Lewin, John W. Boja, and Michael J. Kuhar pp 969 - 981; DOI: 10.1021/jm00084a001 |
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A novel class of calcium-entry blockers: the 1-[[4-(aminoalkoxy)phenyl]sulfonyl]indolizines Jean Gubin, Jean Lucchetti, Jean Mahaux, Dino Nisato, Gilbert Rosseels, Martine Clinet, Peter Polster, and Pierre Chatelain pp 981 - 988; DOI: 10.1021/jm00084a002 |
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Antimitotic agents. Chiral isomers of ethyl 5-amino-1,2-dihydro-3-(4-hydroxyphenyl)-2-methylpyrido[3,4-b]pyrazin-7-ylcarbamate Carroll Temple and Gregory A. Rener pp 988 - 993; DOI: 10.1021/jm00084a003 |
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Inhibitors of protein kinase C. 2. Substituted bisindolylmaleimides with improved potency and selectivity Peter D. Davis, Lucy H. Elliott, William Harris, Christopher H. Hill, Steven A. Hurst, Elizabeth Keech, M. K. Hari Kumar, Geoffrey Lawton, John S. Nixon, and Sandra E. Wilkinson pp 994 - 1001; DOI: 10.1021/jm00084a004 |
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CoMFA analysis of the interactions of antipicornavirus compounds in the binding pocket of human rhinovirus-14 Guy D. Diana, Paul Kowalczyk, Adi M. Treasurywala, Richard C. Oglesby, Daniel C. Pevear, and Frank J. Dutko pp 1002 - 1008; DOI: 10.1021/jm00084a005 |
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Conformational effects on the activity of drugs. 13. A revision of previously proposed models for the activation of .alpha.- and .beta.-adrenergic receptors Bruno Macchia, Aldo Balsamo, Maria C. Breschi, Annalina Lapucci, Antonio Lucacchini, Franco Macchia, Clementina Manera, Adriano Martinelli, Claudia Martini, and et al. pp 1009 - 1018; DOI: 10.1021/jm00084a006 |
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Novel 5-HT3 antagonists: indol-3-ylspiro(azabicycloalkane-3,5'(4'H)oxazoles) C. J. Swain, R. Baker, C. Kneen, R. Herbert, J. Moseley, J. Saunders, E. M. Seward, G. I. Stevenson, M. Beer, and et al. pp 1019 - 1031; DOI: 10.1021/jm00084a007 |
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Renin inhibitors containing .alpha.-heteroatom amino acids as P2 residues Joseph T. Repine, James S. Kaltenbronn, Annette M. Doherty, James M. Hamby, Richard J. Himmelsbach, Brian E. Kornberg, Michael D. Taylor, ELizabeth A. Lunney, Christine Humblet, and et al. pp 1032 - 1042; DOI: 10.1021/jm00084a008 |
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Hybrid cholecystokinin-A antagonists based on molecular modeling of lorglumide and L-364,718 Arie Van der Bent, Armand G. S. Blommaert, Caroline T. M. Melman, Adriaan P. IJzerman, Ineke Van Wijngaarden, and Willem Soudijn pp 1042 - 1049; DOI: 10.1021/jm00084a009 |
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(H+, K+)-ATPase inhibiting 2-[(2-pyridylmethyl)sulfinyl]benzimidazoles. 4. A novel series of dimethoxypyridyl-substituted inhibitors with enhanced selectivity. The selection of pantoprazole as a clinical candidate Bernhard Kohl, Ernst Sturm, Joerg Senn-Bilfinger, W. Alexander Simon, Uwe Krueger, Hartmann Schaefer, Georg Rainer, Volker Figala, Kurt Klemm, and et al. pp 1049 - 1057; DOI: 10.1021/jm00084a010 |
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Synthesis of alkoxy-substituted diaryl compounds and correlation of ring separation with inhibition of tubulin polymerization: differential enhancement of inhibitory effects under suboptimal polymerization reaction conditions Zelleka Getahun, Leonard Jurd, Ping S. Chu, Chii M. Lin, and Ernest Hamel pp 1058 - 1067; DOI: 10.1021/jm00084a011 |
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Structure-activity relationships for inhibition of papain by peptide Michael acceptors Siming Liu and Robert P. Hanzlik pp 1067 - 1075; DOI: 10.1021/jm00084a012 |
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Dopaminergic and serotonergic activities of imidazoquinolinones and related compounds Malcolm W. Moon, Jeanette K. Morris, Richard F. Heier, Connie G. Chidester, William E. Hoffmann, Montford F. Piercey, John S. Althaus, Philip F. VonVoigtlander, Dawna L. Evans, and et al. pp 1076 - 1092; DOI: 10.1021/jm00084a013 |
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Noncataleptogenic, centrally acting dopamine D-2 and serotonin 5-HT2 antagonists within a series of 3-substituted 1-(4-fluorophenyl)-1H-indoles Jens Perregaard, Joern Arnt, Klaus P. Boegesoe, John Hyttel, and Connie Sanchez pp 1092 - 1101; DOI: 10.1021/jm00084a014 |
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Synthesis and cholinergic properties of bis[[(dimethylamino)methyl]furanyl] analogs of ranitidine J. Walter Sowell, Yunzhao Tang, Matthew J. Valli, James M. Chapman, Laura A. Usher, Celeste M. Vaughan, and J. W. Kosh pp 1102 - 1108; DOI: 10.1021/jm00084a015 |
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Synthesis and biological activity of acyclic analogs of 5,10-dideaza-5,6,7,8-tetrahydrofolic acid Chuan Shih, Lynn S. Gossett, John F. Worzalla, Sharon M. Rinzel, Gerald B. Grindey, Philip M. Harrington, and Edward C. Taylor pp 1109 - 1116; DOI: 10.1021/jm00084a016 |
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Selective irreversible inhibitors of aldose reductase Michael W. Smar, Jeffrey J. Ares, Toshihiro Nakayama, Hiroyuki Itabe, Peter F. Kador, and Duane D. Miller pp 1117 - 1120; DOI: 10.1021/jm00084a017 |
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Effect of the 7-amino substituent on the inhibitory potency of mechanism-based isocoumarin inhibitors for porcine pancreatic and human neutrophil elastases: a 1.85-.ANG. x-ray structure of the complex between porcine pancreatic elastase and 7-[(N-tosylphenylalanyl)amino]-4-chloro-3-methoxyisocoumarin Maria A. Hernandez, James C. Powers, Jan Glinski, Jozef Oleksyszyn, J. Vijayalakshmi, and Edgar F. Meyer pp 1121 - 1129; DOI: 10.1021/jm00084a018 |
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A novel synthesis and potent antiinflammatory activity of 4-hydroxy-2(1H)-oxo-1-phenyl-1,8-naphthyridine-3-carboxamides Takeshi Kuroda, Fumio Suzuki, Tadafumi Tamura, Kenji Ohmori, and Hisashi Hosoe pp 1130 - 1136; DOI: 10.1021/jm00084a019 |
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NG-allyl- and NG-cyclopropyl-L-arginine: two novel inhibitors of macrophage nitric oxide synthase Norman M. Olken and Michael A. Marletta pp 1137 - 1144; DOI: 10.1021/jm00084a020 |
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Probing the functional conformation of neuropeptide Y through the design and study of cyclic analogs Marlene Bouvier and John W. Taylor pp 1145 - 1155; DOI: 10.1021/jm00084a021 |
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Antibacterials. Synthesis and structure-activity studies of 3-aryl-2-oxooxazolidines. 4. Multiply-substituted aryl derivatives Chung Ho Park, David R. Brittelli, C. L. J. Wang, Frank D. Marsh, Walter A. Gregory, Mark A. Wuonola, Ronald J. McRipley, Virginia S. Eberly, Andrew M. Slee, and Martin Forbes pp 1156 - 1165; DOI: 10.1021/jm00084a022 |
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Tricarbonylchromium complexes of Hantzsch esters possess robust calcium antagonist activity Timothy L. Hubler, Scott B. Meikrantz, Thomas E. Bitterwolf, Nicholas R. Natale, David J. Triggle, and Yong Wha Kwon pp 1165 - 1168; DOI: 10.1021/jm00084a023 |
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Book Reviews pp 1168 - 1168; DOI: 10.1021/jm00084a600 |
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Oral hypoglycemic agents. Pyrimido[1,2-a]indoles and related compounds Ian A. Cliffe, Eric L. Lien, Howard L. Mansell, Kurt E. Steiner, Richard S. Todd, Alan C. White, and Robin M. Black pp 1169 - 1175; DOI: 10.1021/jm00085a001 |
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Antihyperglycemic activity of novel substituted 3H-1,2,3,5-oxathiadiazole 2-oxides John W. Ellingboe, Thomas R. Alessi, Terence M. Dolak, Thomas T. Nguyen, John D. Tomer, Frieda Guzzo, Jehan F. Bagli, and Michael L. McCaleb pp 1176 - 1183; DOI: 10.1021/jm00085a002 |
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Synthesis and antiulcer activity of novel 5-(2-ethenyl substituted)-3(2H)-furanones Steven W. Felman, Ivo Jirkovsky, Kevin A. Memoli, Luis Borella, Cheryl Wells, Jim Russell, and Jim Ward pp 1183 - 1190; DOI: 10.1021/jm00085a003 |
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Development of a series of phenyltetrazole leukotriene D4(LTD4) receptor antagonists Richard W. Harper, David K. Herron, Nancy G. Bollinger, J. Scott Sawyer, Ronald F. Baldwin, Carlos R. Roman, Lynn E. Rinkema, and Jerome H. Fleisch pp 1191 - 1200; DOI: 10.1021/jm00085a004 |
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Optimization of the quinoline and substituted benzyl moieties of a series of phenyltetrazole leukotriene D4 receptor antagonists J. Scott Sawyer, Ronald F. Baldwin, Lynn E. Rinkema, Carlos R. Roman, and Jerome H. Fleisch pp 1200 - 1209; DOI: 10.1021/jm00085a005 |
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Analogs of natural phloroglucinols as antagonists against both thromboxane A2 and leukotriene D4 Masahiro Tada, Kazuhiro Chiba, Takako Takakuwa, and Eri Kojima pp 1209 - 1212; DOI: 10.1021/jm00085a006 |
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Antimycobacterial activity of a series of pyrazinoic acid esters Michael H. Cynamon, Sally P. Klemens, Tso Sheng Chou, Rayomand H. Gimi, and John T. Welch pp 1212 - 1215; DOI: 10.1021/jm00085a007 |
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Synthesis, characterization, and anti-human immunodeficiency virus activity of water-soluble salts of polyoxotungstate anions with covalently attached organic groups Mark S. Weeks, Craig L. Hill, and Raymond F. Schinazi pp 1216 - 1221; DOI: 10.1021/jm00085a008 |
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Stereospecificity of amino acid side chains in deltorphin defines binding to opioid receptors Lawrence H. Lazarus, Severo Salvadori, Gianfranco Balboni, Roberto Tomatis, and William E. Wilson pp 1222 - 1227; DOI: 10.1021/jm00085a009 |
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Synthesis and biological activity of novel folic acid analogs: pteroyl-S-alkylhomocysteine sulfoximines Peter J. Harvison and Thomas I. Kalman pp 1227 - 1233; DOI: 10.1021/jm00085a010 |
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Cholesterol-lowering bile acid-binding agents: novel lipophilic polyamines Edward W. Thomas, Michele M. Cudahy, Charles H. Spilman, Dac M. Dinh, Tommie L. Watkins, and Thomas J. Vidmar pp 1233 - 1245; DOI: 10.1021/jm00085a011 |
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Low-molecular-weight proteins as carriers for renal drug targeting. Preparation of drug-protein conjugates and drug-spacer derivatives and their catabolism in renal cortex homogenates and lysosomal lysates Eric J. F. Franssen, Jaco Koiter, Caroline A. M. Kuipers, Andries P. Bruins, Frits Moolenaar, Dick De Zeeuw, Wim H. Kruizinga, Richard M. Kellogg, and Dirk K. F. Meijer pp 1246 - 1259; DOI: 10.1021/jm00085a012 |
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Potent and systemically active aminopeptidase N inhibitors designed from active-site investigation Marie Claude Fournie-Zaluski, Pascale Coric, Serge Turcaud, Luce Bruetschy, Evelyne Lucas, Florence Noble, and Bernard P. Roques pp 1259 - 1266; DOI: 10.1021/jm00085a013 |
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Cardiotonic agents. 7. Prodrug derivatives of 4-ethyl-1,3-dihydro-5-[4-(2-methyl-1H-imidazol-1-yl)benzoyl]-2H-imidazol-2-one Kenneth J. Shaw, Paul W. Erhardt, Alfred A. Hagedom, Cynthia A. Pease, William R. Ingebretsen, and Jay R. Wiggins pp 1267 - 1272; DOI: 10.1021/jm00085a014 |
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Synthesis and substance P antagonist activity of naphthimidazolium derivatives Kristine B. Lawrence, Bhaskar R. Venepalli, Kenneth C. Appell, Ramanuj Goswami, Margaret E. Logan, Bruce E. Tomczuk, and John M. Yanni pp 1273 - 1279; DOI: 10.1021/jm00085a015 |
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Synthesis and muscarinic activities of quinuclidin-3-yltriazole and -tetrazole derivatives Harry J. Wadsworth, Sarah M. Jenkins, Barry S. Orlek, Frederick Cassidy, Michael S. G. Clark, Frank Brown, Graham J. Riley, Diane Graves, Julie Hawkins, and Christopher B. Naylor pp 1280 - 1290; DOI: 10.1021/jm00085a016 |
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Muscarinic receptor subtype specificity of (N,N-dialkylamino)alkyl 2-cyclohexyl-2-phenylpropionates: cylexphenes (cyclohexyl-substituted aprophen analogs) Haim Leader, Richard K. Gordon, Jesse Baumgold, Victoria L. Boyd, Amy H. Newman, Ruthann M. Smejkal, and Peter K. Chiang pp 1290 - 1295; DOI: 10.1021/jm00085a017 |
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Synthesis of 3-(2-pyridylethyl)benzoxazolinone derivatives: potent analgesic and antiinflammatory compounds inhibiting prostaglandin E2 Cihat Safak, Hakki Erdogan, Erhan Palaska, Rumeysa Sunal, and Suna Duru pp 1296 - 1299; DOI: 10.1021/jm00085a018 |
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Development of 2,3-dihydro-6-(3-phenoxypropyl)-2-(2-phenylethyl)-5-benzofuranol (L-670,630) as a potent and orally active inhibitor of 5-lipoxygenase Cheuk K. Lau, Patrice C. Belanger, Claude Dufresne, John Scheigetz, Michel Therien, Brian Fitzsimmons, Robert N. Young, Anthony W. Ford-Hutchinson, Denis Riendeau, and et al. pp 1299 - 1318; DOI: 10.1021/jm00085a019 |
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Intriguing structure-activity relations underlie the potent inhibition of HIV protease by norstatine-based peptides Tim F. Tam, Julie Carriere, I. David MacDonald, Arlindo L. Castelhano, Diana H. Pliura, Nolan J. Dewdney, Everton M. Thomas, Chinh Bach, Jimmy Barnett, and et al. pp 1318 - 1320; DOI: 10.1021/jm00085a020 |
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Book Reviews pp 1321 - 1322; DOI: 10.1021/jm00085a600 |
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Analogs of the dioxolanes dexoxadrol and etoxadrol as potential phencyclidine-like agents. Synthesis and structure activity relationships Andrew Thurkauf, Mariena V. Mattson, Scott Richardson, Seid Mirsadeghi, Paul L. Ornstein, Ernest A. Harrison, Kenner C. Rice, Arthur E. Jacobson, and James A. Monn pp 1323 - 1329; DOI: 10.1021/jm00086a001 |
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Synthesis of 2-(p-chlorobenzyl)-3-aryl-6-methoxybenzofurans as selective ligands for antiestrogen-binding sites. Effects on cell proliferation and cholesterol synthesis Chin Chin Teo, Oi Lian Kon, Keng Yeow Sim, and Siu Choon Ng pp 1330 - 1339; DOI: 10.1021/jm00086a002 |
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2-Substituted 3-(aminooxy)propanamines as inhibitors of ornithine decarboxylase: synthesis and biological activity Jaroslav Stanek, Joerg Frei, Helmut Mett, Peter Schneider, and Urs Regenass pp 1339 - 1344; DOI: 10.1021/jm00086a003 |
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Generation of N-methyl-D-aspartate agonist and competitive antagonist pharmacophore models. Design and synthesis of phosphonoalkyl-substituted tetrahydroisoquinolines as novel antagonists Daniel F. Ortwine, Thomas C. Malone, Christopher F. Bigge, James T. Drummond, Christine Humblet, Graham Johnson, and Garry W. Pinter pp 1345 - 1370; DOI: 10.1021/jm00086a004 |
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Exploration of N-phosphonoalkyl-, N-phosphonoalkenyl-, and N-(phosphonoalkyl)phenyl-spaced .alpha.-amino acids as competitive N-methyl-D-aspartic acid antagonists Christopher F. Bigge, Graham Johnson, Daniel F. Ortwine, James T. Drummond, Daniel M. Retz, Laura J. Brahce, Linda L. Coughenour, Frank W. Marcoux, and Albert W. Probert pp 1371 - 1384; DOI: 10.1021/jm00086a005 |
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Pyrimido[1,6-a]benzimidazoles: a new class of DNA gyrase inhibitors C. Hubschwerlen, P. Pflieger, J. L. Specklin, K. Gubernator, H. Gmuender, P. Angehrn, and I. Kompis pp 1385 - 1392; DOI: 10.1021/jm00086a006 |
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Preparation and in vitro and in vivo evaluation of quinolones with selective activity against Gram-positive organisms Curt S. Cooper, Pamela L. Klock, Daniel T. W. Chu, Dwight J. Hardy, Robert N. Swanson, and Jacob J. Plattner pp 1392 - 1398; DOI: 10.1021/jm00086a007 |
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Synthesis and biological activity of open-chain analogs of 5,6,7,8-tetrahydrofolic acid-potential antitumor agents Eric C. Bigham, Stephen J. Hodson, W. Revill Mallory, David Wilson, David S. Duch, Gary K. Smith, and Robert Ferone pp 1399 - 1410; DOI: 10.1021/jm00086a008 |
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Inhibition of pig kidney L-aromatic amino acid decarboxylase by 2,3-methano-m-tyrosines Saeed Ahmad, Robert S. Phillips, and Charles H. Stammer pp 1410 - 1417; DOI: 10.1021/jm00086a009 |
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Anthracene-9,10-diones as potential anticancer agents. Synthesis, DNA-binding, and biological studies on a series of 2,6-disubstituted derivatives Mavis Agbandje, Terence C. Jenkins, Robert McKenna, Anthony P. Reszka, and Stephen Neidle pp 1418 - 1429; DOI: 10.1021/jm00086a010 |
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Syntheses, resolution, and structure-activity relationships of potent acetylcholinesterase inhibitors: 8-carbaphysostigmine analogs Yuhpyng L. Chen, Jann Nielsen, Kirk Hedberg, Audrey Dunaiskis, Shawn Jones, Lorena Russo, Jonathan Johnson, Jeffrey Ives, and Dane Liston pp 1429 - 1434; DOI: 10.1021/jm00086a011 |
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Synthesis and biological studies of unsaturated acyclonucleoside analogs of S-adenosyl-L-homocysteine hydrolase inhibitors Ahmad Hasan and Prem C. Srivastava pp 1435 - 1439; DOI: 10.1021/jm00086a012 |
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Synthesis and anti-HIV activity of 4'-azido- and 4'-methoxynucleosides Hans Maag, Robert M. Rydzewski, Mary Jane McRoberts, Diane Crawford-Ruth, Julien P. H. Verheyden, and Ernest J. Prisbe pp 1440 - 1451; DOI: 10.1021/jm00086a013 |
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Inhibitors of human purine nucleoside phosphorylase. Synthesis and biological activities of 8-amino-3-benzylhypoxanthine and related analogs Peter W. K. Woo, Catherine R. Kostlan, Jagadish C. Sircar, Mi K. Dong, and Richard B. Gilbertsen pp 1451 - 1457; DOI: 10.1021/jm00086a014 |
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Synthesis and antiviral activity of acyclic nucleosides with a 3(S),5-dihydroxypentyl or 4(R)-methoxy-3(S),5-dihydroxypentyl sidechain Frank Vandenriessche, Robert Snoeck, Gerard Janssen, Jos Hoogmartens, Arthur Van Aerschot, Erik De Clercq, and Piet Herdewijn pp 1458 - 1465; DOI: 10.1021/jm00086a015 |
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Stereoisomeric probes for the D1 dopamine receptor: synthesis and characterization of R-(+) and S-(-) enantiomers of 3-allyl-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine and its 6-bromo analog John L. Neumeyer, Nora S. Kula, Ross J. Baldessarini, and Nandkishore Baindur pp 1466 - 1471; DOI: 10.1021/jm00086a016 |
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Amide bond replacements incorporated into CCK-B selective "dipeptoids" Christopher I. Fincham, Michael Higginbottom, David R. Hill, David C. Horwell, John C. O'Toole, Giles S. Ratcliffe, David C. Rees, and Edward Roberts pp 1472 - 1484; DOI: 10.1021/jm00086a017 |
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Novel naphthalenic ligands with high affinity for the melatonin receptor S. Yous, J. Andrieux, H. E. Howell, P. J. Morgan, P. Renard, B. Pfeiffer, D. Lesieur, and B. Guardiola-Lemaitre pp 1484 - 1486; DOI: 10.1021/jm00086a018 |
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SC-53116: the first selective agonist at the newly identified serotonin 5-HT4 receptor subtype Daniel L. Flynn, Daniel L. Zabrowski, Daniel P. Becker, Roger Nosal, Clara I. Villamil, Gary W. Gullikson, Chafiq Moummi, and Dai C. Yang pp 1486 - 1489; DOI: 10.1021/jm00086a019 |
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Bis(maltolato)oxovanadium(IV) is a potent insulin mimic John H. McNeill, V. G. Yuen, H. R. Hoveyda, and Chris Orvig pp 1489 - 1491; DOI: 10.1021/jm00086a020 |
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Book Reviews pp 1492 - 1492; DOI: 10.1021/jm00086a600 |
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Endothelin: a new challenge Annette M. Doherty pp 1493 - 1508; DOI: 10.1021/jm00087a001 |
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Modeling of competitive phosphono amino acid NMDA receptor antagonists Jeffrey P. Whitten, Boyd L. Harrison, Herschel J. R. Weintraub, and Ian A. McDonald pp 1509 - 1514; DOI: 10.1021/jm00087a002 |
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Novel antagonists of the 5-HT3 receptor. Synthesis and structure-activity relationships of (2-alkoxybenzoyl)ureas Gerald Bradley, Terence J. Ward, Janet C. White, James Coleman, Ann Taylor, and Keith F. Rhodes pp 1515 - 1520; DOI: 10.1021/jm00087a003 |
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Phenylmorphans and analogs: opioid receptor subtype selectivity and effect of conformation on activity Mark Froimowitz, Chaim G. Pick, and Gavril W. Pasternak pp 1521 - 1525; DOI: 10.1021/jm00087a004 |
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(Aminoalkoxy)chromones. Selective .sigma. receptor ligands Ronald H. Erickson, Kenneth J. Natalie Jr., William Bock, Zhijian Lu, Farzaneh Farzin, Ronald G. Sherrill, David J. Meloni, Raymond J. Patch, Waclaw J. Rzesotarski, and et al. pp 1526 - 1535; DOI: 10.1021/jm00087a005 |
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Substitution on the Phe3 aromatic ring in cyclic .delta. opioid receptor-selective dermorphin/deltorphin tetrapeptide analogs: electronic and lipophilic requirements for receptor affinity Deborah L. Heyl and Henry I. Mosberg pp 1535 - 1541; DOI: 10.1021/jm00087a006 |
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Analogs of the muscarinic agent 2'-methylspiro[1-azabicyclo[2.2.2]octane-3,4'-[1,3]dioxolane]: synthesis and pharmacology Gunnar Nordvall, Staffan Sundquist, Gunilla Glas, Adolf Gogoll, Lisbeth Nilvebrant, and Uli Hacksell pp 1541 - 1550; DOI: 10.1021/jm00087a007 |
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Synthesis and in vitro characterization of novel amino terminally modified oxotremorine derivatives for brain muscarinic receptors David S. Garvey, James T. Wasicak, John Y. L. Chung, Youe Kong Shue, George M. Carrera, Paul D. May, Michael M. McKinney, David Anderson, Evelyn Cadman, and et al. pp 1550 - 1557; DOI: 10.1021/jm00087a008 |
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Structure-activity studies of a novel bicyclic oxytocin antagonist D. David Smith, Jirina Slaninova, and Victor J. Hruby pp 1558 - 1563; DOI: 10.1021/jm00087a009 |
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A new class of bradykinin antagonists: synthesis and in vitro activity of bissuccinimidoalkane peptide dimers John C. Cheronis, Eric T. Whalley, Khe T. Nguyen, Shad R. Eubanks, Lisa G. Allen, Matthew J. Duggan, Sharon D. Loy, Kathryn A. Bonham, and James K. Blodgett pp 1563 - 1572; DOI: 10.1021/jm00087a010 |
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Rationally designed dipeptoid analogs of cholecystokinin. A Free-Wilson/Fujita-Ban analysis of some .alpha.-methyltryptophan derivatives as cholecystokinin-B antagonists Michael Higginbottom, Clare Kneen, and Giles S. Ratcliffe pp 1572 - 1577; DOI: 10.1021/jm00087a011 |
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First use of the Taylor pteridine synthesis as a route to polyglutamate derivatives of antifolates. 46. Side chain modified 5-deazafolate and 5-deazatetrahydrofolate analogs as mammalian folylpolyglutamate synthetase and glycinamide ribonucleotide formyl transferase inhibitors: synthesis and in vitro biological evaluation Andre Rosowsky, Ronald A. Forsch, Valerie E. Reich, James H. Freisheim, and Richard G. Moran pp 1578 - 1588; DOI: 10.1021/jm00087a012 |
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Synthesis and evaluation of a new series of mechanism-based aromatase inhibitors D. Lesuisse, J. F. Gourvest, C. Hartmann, B. Tric, O. Benslimane, D. Philibert, and J. P. Vevert pp 1588 - 1597; DOI: 10.1021/jm00087a013 |
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Novel anthraquinone inhibitors of human leukocyte elastase and cathepsin G David E. Zembower, Chih Min Kam, James C. Powers, and Leon H. Zalkow pp 1597 - 1605; DOI: 10.1021/jm00087a014 |
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Inhibitors of human purine nucleoside phosphorylase. Synthesis of pyrrolo[3,2-d]pyrimidines, a new class of purine nucleoside phosphorylase inhibitors as potentially T-cell selective immunosuppressive agents. Description of 2,6-diamino-3,5-dihydro-7-(3-thienylmethyl)-4H-pyrrolo[3,2-d]pyrimidin-4-one (CI-972) Jagadish C. Sircar, Catherine R. Kostlan, Richard B. Gilbertsen, Mary K. Bennett, Mi K. Dong, and W. J. Cetenko pp 1605 - 1609; DOI: 10.1021/jm00087a015 |
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Inhibitors of acyl-CoA:cholesterol acyltransferase. 1. Identification and structure-activity relationships of a novel series of fatty acid anilide hypocholesterolemic agents Bruce D. Roth, C. John Blankley, Milton L. Hoefle, Ann Holmes, W. Howard Roark, Bharat K. Trivedi, Arnold D. Essenburg, Karen A. Kieft, Brian R. Krause, and Richard L. Stanfield pp 1609 - 1617; DOI: 10.1021/jm00087a016 |
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3-O-alkylascorbic acids as free radical quenchers. 3. Protective effect on coronary occlusion-reperfusion induced arrhythmias in anesthetized rats Yasunori Nihro, Satoshi Sogawa, Akihiro Izumi, Akihiro Sasamori, Tadamitsu Sudo, Tokutaro Miki, Hitoshi Matsumoto, and Toshio Satoh pp 1618 - 1623; DOI: 10.1021/jm00087a017 |
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Synthesis and antihypertensive activity of 3-[(substituted-carbonyl)amino]-2H-1-benzopyrans Frederick Cassidy, John M. Evans, Michael S. Hadley, Adele H. Haladij, Patricia E. Leach, and Geoffrey Stemp pp 1623 - 1627; DOI: 10.1021/jm00087a018 |
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Synthesis and in vitro evaluation of boronated uridine and glucose derivatives for boron neutron capture therapy. Werner Tjarks, Abul K. M. Anisuzzaman, Liang Liu, Albert H. Soloway, Rolf F. Barth, Douglas J. Perkins, and Dianne M. Adams pp 1628 - 1633; DOI: 10.1021/jm00087a019 |
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Synthesis and biological activity of 8a-phenyldecahydroquinolines as probes of PCP's binding conformation. A new PCP-like compound with increased in vivo potency Chinpiao Chen, Alan P. Kozikowski, Paul L. Wood, Ian J. Reynolds, Richard G. Ball, and Yuan Ping Pang pp 1634 - 1638; DOI: 10.1021/jm00087a020 |
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Antimalarial activity of new dihydroartemisinin derivatives. 5. Sugar analogs. Ai J. Lin, Liang Quan Li, Steven L. Andersen, and Daniel L. Klayman pp 1639 - 1642; DOI: 10.1021/jm00087a021 |
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Molecular recognition of amiloride analogs: a molecular electrostatic potential analysis. 1. Pyrazine ring modifications Carol A. Venanzi, Christopher Plant, and Thomas J. Venanzi pp 1643 - 1649; DOI: 10.1021/jm00087a022 |
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Analogs of platelet activating factor. 6. Mono- and bis-aryl phosphate antagonists of platelet activating factor A. Wissner, M. L. Carroll, K. E. Green, S. S. Kerwar, W. C. Pickett, R. E. Schaub, L. W. Torley, S. Wrenn, and C. A. Kohler pp 1650 - 1662; DOI: 10.1021/jm00087a023 |
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Antiandrogenic steroidal sulfonyl heterocycles. Utility of electrostatic complementarity in defining bioisosteric sulfonyl heterocycles John P. Mallamo, Garry M. Pilling, Joseph R. Wetzel, Paul J. Kowalczyk, Malcolm R. Bell, Rudolph K. Kullnig, Frederick H. Batzold, Paul E. Juniewicz, Richard C. Winneker, and Henry R. Luss pp 1663 - 1670; DOI: 10.1021/jm00088a001 |
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Definition and display of steric, hydrophobic, and hydrogen bonding properties of ligand binding sites in proteins using Lee and Richards accessible surface: validation of a high-resolution graphical tool for drug design Regine S. Bohacek and Colin McMartin pp 1671 - 1684; DOI: 10.1021/jm00088a002 |
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Synthesis and antiviral activity of a series of HIV-1 protease inhibitors with functionality tethered to the P1 or P1' phenyl design Wayne J. Thompson, Paula M. D. Fitzgerald, M. Katharine Holloway, Emilio A. Emini, Paul L. Darke, Brian M. McKeever, William A. Schleif, Julio C. Quintero, Joan A. Zugay, and et al. pp 1685 - 1701; DOI: 10.1021/jm00088a003 |
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HIV-1 protease inhibitors based on hydroxyethylene dipeptide isosteres: An investigation into the role of the P1' side chain on structure-activity Steven D. Young, Linda S. Payne, Wayne J. Thompson, Neil Gaffin, Terry A. Lyle, Susan F. Britcher, Samuel L. Graham, Thomas H. Schultz, Albert A. Deana, and et al. pp 1702 - 1709; DOI: 10.1021/jm00088a004 |
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1,2,3-Trisubstituted cyclopropanes as conformationally restricted peptide isosteres: application to the design and synthesis of novel renin inhibitors Stephen F. Martin, Richard E. Austin, Christopher J. Oalmann, William R. Baker, Stephen L. Condon, Ed DeLara, Saul H. Rosenberg, Kenneth P. Spina, Herman H. Stein, and et al. pp 1710 - 1721; DOI: 10.1021/jm00088a005 |
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Nonpeptide renin inhibitors employing a novel 3-aza (or oxa)-2,4-dialkyl glutaric acid moiety as a P2/P3 amide bond replacement William R. Baker, Anthony K. L. Fung, Hollis D. Kleinert, Herman H. Stein, Jacob J. Plattner, Yoek Lin Armiger, Stephen L. Condon, Jerome Cohen, David A. Egan, and et al. pp 1722 - 1734; DOI: 10.1021/jm00088a006 |
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C-Terminal modifications of nonpeptide renin inhibitors: improved oral bioavailability via modification of physicochemical properties Steven A. Boyd, Anthony K. L. Fung, William R. Baker, Robert A. Mantei, Yoek Lin Armiger, Herman H. Stein, Jerome Cohen, David A. Egan, Jennifer L. Barlow, and et al. pp 1735 - 1746; DOI: 10.1021/jm00088a007 |
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Carboxylic acid replacement structure-activity relationships in suosan type sweeteners. A sweet taste antagonist. 1 George W. Muller, J. Chris Culberson, Glenn Roy, Jeanette Ziegler, D. Eric Walters, Michael S. Kellogg, Susan S. Schiffman, and Zoe S. Warwick pp 1747 - 1751; DOI: 10.1021/jm00088a008 |
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Selective .beta.3-adrenergic agonists of brown adipose tissue and thermogenesis. 1. [4-[2-[(2-Hydroxy-3-phenoxypropyl)amino]ethoxy]phenoxy]acetates Ralph Howe, Balbir S. Rao, Brian R. Holloway, and Donald Stribling pp 1751 - 1759; DOI: 10.1021/jm00088a009 |
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Selective .beta.3-adrenergic agonists of brown adipose tissue and thermogenesis. 2. [4-[2-[(2-Hydroxy-3-phenoxypropyl)amino]ethoxy]phenoxy]acetamides Ralph Howe, Balbir S. Rao, Brian R. Holloway, and Donald Stribling pp 1759 - 1764; DOI: 10.1021/jm00088a010 |
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Quinolone antibacterial agents. Synthesis and structure-activity relationships of a series of amino acid prodrugs of racemic and chiral 7-(3-amino-1-pyrrolidinyl)quinolones. Highly soluble quinolone prodrugs with in vivo pseudomonas activity Joseph P. Sanchez, John M. Domagala, Carl L. Heifetz, Stephen R. Priebe, Josephine A. Sesnie, and Ashok K. Trehan pp 1764 - 1773; DOI: 10.1021/jm00088a011 |
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Structure-activity relationships of (+)-CC-1065 analogs in the inhibition of helicase-catalyzed unwinding of duplex DNA Daekyu Sun and Laurence H. Hurley pp 1773 - 1782; DOI: 10.1021/jm00088a012 |
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4'-Modified analogs of aristeromycin and neplanocin A: synthesis and inhibitory activity toward S-adenosyl-L-homocysteine hydrolase Michael S. Wolfe, Younha Lee, William J. Bartlett, David R. Borcherding, and Ronald T. Borchardt pp 1782 - 1791; DOI: 10.1021/jm00088a013 |
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3-(2-Carboxyindol-3-yl)propionic acid-based antagonists of the NMDA (N-methyl-D-aspartic acid) receptor associated glycine binding site Francesco G. Salituro, Boyd L. Harrison, Bruce M. Baron, Philip L. Nyce, Kenneth T. Stewart, John H. Kehne, H. Steven White, and Ian A. McDonald pp 1791 - 1799; DOI: 10.1021/jm00088a014 |
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Synthesis and antiviral activity of 1-cyclobutyl-5-(2-bromovinyl)uracil nucleoside analogs and related compounds. William A. Slusarchyk, Gregory S. Bisacchi, A. Kirk Field, Deborah R. Hockstein, Glenn A. Jacobs, Bridget McGeever-Rubin, Joseph A. Tino, A. V. Tuomari, Gregory A. Yamanaka, and et al. pp 1799 - 1806; DOI: 10.1021/jm00088a015 |
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Molecular modeling and crystallographic studies of 4-amino-N-phenylbenzamide anticonvulsants Norma E. C. Duke and Penelope W. Codding pp 1806 - 1812; DOI: 10.1021/jm00088a016 |
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Probes for the cocaine receptor. Potentially irreversible ligands for the dopamine transporter F. Ivy Carroll, Yigong Gao, Philip Abraham, Anita H. Lewin, Robert Lew, Amrat Patel, John W. Boja, and Michael J. Kuhar pp 1813 - 1817; DOI: 10.1021/jm00088a017 |
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Leukotriene B4 receptor antagonists: the LY255283 series of hydroxyacetophenones David K. Herron, Theodore Goodson, Nancy G. Bollinger, Dorothy Swanson-Bean, Ian G. Wright, Gilbert S. Staten, Alan R. Thompson, Larry L. Froelich, and William T. Jackson pp 1818 - 1828; DOI: 10.1021/jm00088a018 |
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Dual-action penems and carbapenems Alfred J. Corraz, Scott L. Dax, Norma K. Dunlap, Nafsika H. Georgopapadakou, Dennis D. Keith, David L. Pruess, Pamela L. Rossman, Rudolf Then, Joel Unowsky, and Chung Chen Wei pp 1828 - 1839; DOI: 10.1021/jm00088a019 |
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Synthetic modification of a novel microbial ionophore: exploration of anticoccidial structure-activity relationships E. A. Glazer, D. A. Koss, J. A. Olson, A. P. Ricketts, T. K. Schaaf, and R. J. Wiscount pp 1839 - 1844; DOI: 10.1021/jm00088a020 |
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Reversible inhibitors of the gastric (H+/K+)-ATPase. 2. 1-Arylpyrrolo[3,2-c]quinolines: effect of the 4-substituent Colin A. Leach, Thomas H. Brown, Robert J. Ife, David J. Keeling, Shiona M. Laing, Michael E. Parsons, Carolyn A. Price, and Kenneth J. Wiggall pp 1845 - 1852; DOI: 10.1021/jm00088a021 |
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Novel thiazolidine-2,4-diones as potent euglycemic agents. Bernard Hulin, David A. Clark, Steven W. Goldstein, Ruth E. McDermott, Paul J. Dambek, Werner H. Kappeler, Charles H. Lamphere, Diana M. Lewis, and James P. Rizzi pp 1853 - 1864; DOI: 10.1021/jm00088a022 |
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Affinity of human growth hormone-releasing factor (1-29)NH2 analogs for GRF binding sites in rat adenopituitary Pierrette Gaudreau, Luce Boulanger, and Thierry Abribat pp 1864 - 1869; DOI: 10.1021/jm00088a023 |
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Alanine series of ovine corticotropin releasing factor (oCRF): a structure-activity relationship study Wayne D. Kornreich, Robert Galyean, Jean Francois Hernandez, A. Grey Craig, Cynthia J. Donaldson, Gayle Yamamoto, Catherine Rivier, Wylie Vale, and Jean Rivier pp 1870 - 1876; DOI: 10.1021/jm00088a024 |
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Geiparvarin Analogs. 3. Synthesis and cytostatic activity of 3(2H)-furanone and 4,5-dihydro-3(2H)-furanone congeners of geiparvarin, containing a geraniol-like fragment in the side chain. Pier G. Baraldi, Stefano Manfredini, Daniele Simoni, Mojgan Aghazadeh Tabrizi, Jan Balzarini, and Erik De Clercq pp 1877 - 1882; DOI: 10.1021/jm00088a025 |
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Synthesis and anti-HIV activity of 9-[c-4,t-5-bis(hydroxymethyl)cyclopent-2-en-r-1-yl]-9H-adenine Nobuya Katagiri, Masahiro Nomura, Hiroshi Sato, Chikara Kaneko, Keisuke Yusa, and Takashi Tsuruo pp 1882 - 1886; DOI: 10.1021/jm00088a026 |
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Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 2. Tricyclic pyridobenzoxazepinones and dibenzoxazepinones Janice M. Klunder, Karl D. Hargrave, M. West, Ernest Cullen, Kollol Pal, Mark L. Behnke, Suresh R. Kapadia, Daniel W. McNeil, Joe C. Wu, and Grace C. Chow pp 1887 - 1897; DOI: 10.1021/jm00088a027 |
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Substrate specificity of isopenicillin N synthase George W. Huffman, Paul D. Gesellchen, Jan R. Turner, Robert B. Rothenberger, Harold E. Osborne, F. Dean Miller, Jerry L. Chapman, and Stephen W. Queener pp 1897 - 1914; DOI: 10.1021/jm00088a028 |
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Synthesis and pharmacological investigation of the enantiomers of muscarone and allo-muscarone Marco De Amici, Clelia Dallanoce, Carlo De Micheli, Enzo Grana, Annalisa Barbieri, Herbert Ladinsky, GiovanniBattista Schiavi, and Franco Zonta pp 1915 - 1920; DOI: 10.1021/jm00088a029 |
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Bioreductive fluorescent markers for hypoxic cells: a study of 2-nitroimidazoles with 1-substituents containing fluorescent, bridgehead-nitrogen, bicyclic systems Richard J. Hodgkiss, Richard W. Middleton, John Parrick, Harshad K. Rami, Peter Wardman, and George D. Wilson pp 1920 - 1926; DOI: 10.1021/jm00088a030 |
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The role of concepts in structure-activity relationship studies of opioid ligands Philip S. Portoghese pp 1927 - 1937; DOI: 10.1021/jm00089a001 |
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New thymidine triphosphate analog inhibitors of human immunodeficiency virus-1 reverse transcriptase. Qi Feng Ma, Ian C. Bathurst, Philip J. Barr, and George L. Kenyon pp 1938 - 1941; DOI: 10.1021/jm00089a002 |
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2-Carboxytetrahydroquinolines. Conformational and stereochemical requirements for antagonism of the glycine site on the N-methyl-D-aspartate (NMDA) receptor Robert W. Carling, Paul D. Leeson, Angela M. Moseley, Raymond Baker, Alan C. Foster, Sarah Grimwood, John A. Kemp, and George R. Marshall pp 1942 - 1953; DOI: 10.1021/jm00089a003 |
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4-Amido-2-carboxytetrahydroquinolines. Structure-activity relationships for antagonism at the glycine site of the NMDA receptor Paul D. Leeson, Robert W. Carling, Kevin W. Moore, Angela M. Moseley, Julian D. Smith, Graeme Stevenson, Tony Chan, Raymond Baker, Alan C. Foster, and et al. pp 1954 - 1968; DOI: 10.1021/jm00089a004 |
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Structure and molecular modeling of GABAA receptor antagonists Didier Rognan, Thierry Boulanger, Remy Hoffmann, Daniel P. Vercauteren, Jean Marie Andre, Francois Durant, and Camille Georges Wermuth pp 1969 - 1977; DOI: 10.1021/jm00089a005 |
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A nonpromoting phorbol from the Samoan medicinal plant Homalanthus nutans inhibits cell killing by HIV-1 Kirk R. Gustafson, John H. Cardellina II, James B. McMahon, Robert J. Gulakowski, Junichi Ishitoya, Zoltan Szallasi, Nancy E. Lewin, Peter M. Blumberg, Owen S. Weislow, and et al. pp 1978 - 1986; DOI: 10.1021/jm00089a006 |
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Asymmetric synthesis of 1,3-dioxolane-pyrimidine nucleosides and their anti-HIV activity. Hea O. Kim, Soon K. Ahn, Antonio J. Alves, J. Warren Beach, Lak S. Jeong, Bo G. Choi, Patrick Van Roey, Raymond F. Schinazi, and Chung K. Chu pp 1987 - 1995; DOI: 10.1021/jm00089a007 |
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Highly water-soluble lipophilic prodrugs of the anti-HIV nucleoside analog 2',3'-dideoxycytidine and its 3'-fluoro derivative Stephen G. Kerr and Thomas I. Kalman pp 1996 - 2001; DOI: 10.1021/jm00089a008 |
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Synthesis and biological evaluation of N.alpha.-(5-deaza-5,6,7,8-tetrahydropteroyl)-L-ornithine Shyam K. Singh, Sara C. Singer, Robert Ferone, Kathleen A. Waters, Robert J. Mullin, and John B. Hynes pp 2002 - 2006; DOI: 10.1021/jm00089a009 |
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Development of potent and selective CCK-A receptor agonists from Boc-CCK-4: tetrapeptides containing Lys(N.epsilon.)-amide residues Kazumi Shiosaki, Chun Wel Lin, Hana Kopecka, Richard A. Craig, Bruce R. Bianchi, Thomas R. Miller, David G. Witte, Michael Stashko, and Alex M. Nadzan pp 2007 - 2014; DOI: 10.1021/jm00089a010 |
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Studies on neurokinin antagonists. 1. The design of novel tripeptides possessing glutaminyl-D-tryptophylphenylalanine sequence as substance P antagonists Daijiro Hagiwara, Hiroshi Miyake, Hiroshi Morimoto, Masako Murai, Takashi Fujii, and Masaaki Matsuo pp 2015 - 2025; DOI: 10.1021/jm00089a011 |
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Benz[f]isoquinoline analogs as high-affinity .sigma. ligands Michael G. N. Russell, Raymond Baker, David C. Billington, Antony K. Knight, Derek N. Middlemiss, and Alison J. Noble pp 2025 - 2033; DOI: 10.1021/jm00089a012 |
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Spiropiperidines as high-affinity, selective .sigma. ligands. Mark S. Chambers, Raymond Baker, David C. Billington, Anthony K. Knight, D. N. Middlemiss, and Eric H. F. Wong pp 2033 - 2039; DOI: 10.1021/jm00089a013 |
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Cyclic RGD peptide analogs as antiplatelet antithrombotics Peter L. Barker, Sherron Bullens, Stuart Bunting, Daniel J. Burdick, Kathryn S. Chan, Tracy Deisher, Charles Eigenbrot, Thomas R. Gadek, Robin Gantzos, and et al. pp 2040 - 2048; DOI: 10.1021/jm00089a014 |
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Ester and amide derivatives of E64c as inhibitors of platelet calpains Zhenya Huang, Eleanor B. McGowan, and Thomas C. Detwiler pp 2048 - 2054; DOI: 10.1021/jm00089a015 |
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Synthesis and structure-activity relationships of a series of novel benzopyran-containing platelet activating factor antagonists Denise E. Guinn, James B. Summers, H. Robin Heyman, Richard G. Conway, David A. Rhein, Daniel H. Albert, Terry Magoc, and George W. Carter pp 2055 - 2061; DOI: 10.1021/jm00089a016 |
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Benzofuran bioisosteres of hallucinogenic tryptamines Zbigniew Tomaszewski, Michael P. Johnson, Xuemei Huang, and David E. Nichols pp 2061 - 2064; DOI: 10.1021/jm00089a017 |
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A novel probe for the cannabinoid receptor William A. Devane, Aviva Breuer, Tzviel Sheskin, Torbjoern U. C. Jaerbe, Moris S. Eisen, and Raphael Mechoulam pp 2065 - 2069; DOI: 10.1021/jm00089a018 |
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Enzymic synthesis and comparative biological evaluation of a phosphonate analog of the lipid A precursor Dieter Scholz, Karl Bednarik, Gerald Ehn, Wolfgang Neruda, Evelyne Janzek, Hans Loibner, Karin Briner, and Andrea Vasella pp 2070 - 2074; DOI: 10.1021/jm00089a019 |
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Synthesis and antiallergic activity of 11-(aminoalkylidene)-6,11-dihydrodibenz[b,e]oxepin derivatives Etsuo Ohshima, Shizuo Otaki, Hideyuki Sato, Toshiaki Kumazawa, Hiroyuki Obase, Akio Ishii, Hidee Ishii, Kenji Ohmori, and Noriaki Hirayama pp 2074 - 2084; DOI: 10.1021/jm00089a020 |
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Biological activities and quantitative structure-activity relationships of spiro[imidazolidine-4,4'(1'H)-quinazoline]-2,2',5(3'H)-triones as aldose reductase inhibitors Masafumi Yamagishi, Yoshihisa Yamada, Kenichi Ozaki, Masaaki Asao, Ryo Shimizu, Mamoru Suzuki, Mamoru Matsumoto, Yuzo Matsuoka, and Kazuo Matsumoto pp 2085 - 2094; DOI: 10.1021/jm00089a021 |
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Inhibitors of cholesterol biosynthesis. 6. trans-6-[2-(2-N-heteroaryl-3,5-disubstituted-pyrazol-4-yl)ethyl/ethenyl]tetrahydro-4-hydroxy-2H-pyran-2-ones D. R. Sliskovic, C. J. Blankley, B. R. Krause, R. S. Newton, J. A. Picard, W. H. Roark, B. D. Roth, C. Sekerke, M. K. Shaw, and R. L. Stanfield pp 2095 - 2103; DOI: 10.1021/jm00089a022 |
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Renin inhibitors containing C-termini derived from mercaptoheterocycles Wallace T. Ashton, Christine L. Cantone, Laura C. Meurer, Richard L. Tolman, William J. Greenlee, Arthur A. Patchett, Robert J. Lynch, Terry W. Schorn, John F. Strouse, and Peter K. S. Siegl pp 2103 - 2112; DOI: 10.1021/jm00089a023 |
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Synthesis of high-affinity fluorine-substituted ligands for the androgen receptor. Potential agents for imaging prostatic cancer by positron emission tomography Aijun Liu, Kathryn E. Carlson, and John A. Katzenellenbogen pp 2113 - 2129; DOI: 10.1021/jm00089a024 |
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Bisquinolines. 1. N,N-bis(7-chloroquinolin-4-yl)alkanediamines with potential against chloroquine-resistant malaria Jonathan L. Vennerstrom, William Y. Ellis, Arba L. Ager, Steven L. Andersen, Lucia Gerena, and Wilbur K. Milhous pp 2129 - 2134; DOI: 10.1021/jm00089a025 |
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Clinical analysis by proton spin-echo NMR. 2. Oxidation of intracellular glutathione as a consequence of penicillamine therapy in rheumatoid arthritis J. Reglinski, W. E. Smith, M. Brzeski, M. Marabani, and R. D. Sturrock pp 2134 - 2137; DOI: 10.1021/jm00089a026 |
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p-(Methylsulfinyl)phenyl nitrogen mustard as a novel bioreductive prodrug selective against hypoxic tumors Chul Hoon Kwon, Daria R. Blanco, and Nesrine Baturay pp 2137 - 2139; DOI: 10.1021/jm00089a027 |
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Cyclic pentapeptide endothelin antagonists with high ETA selectivity. Potency- and solubility-enhancing modifications Kiyofumi Ishikawa, Takehiro Fukami, Toshio Nagase, Kagari Fujita, Takashi Hayama, Kenji Niiyama, Toshiaki Mase, Masaki Ihara, and Mitsuo Yano pp 2139 - 2142; DOI: 10.1021/jm00089a028 |
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Book Reviews pp 2142 - 2144; DOI: 10.1021/jm00089a600 |
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3D database searching in drug design Yvonne C. Martin pp 2145 - 2154; DOI: 10.1021/jm00090a001 |
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Orally active aldose reductase inhibitors: indazoleacetic, oxopyridazineacetic, and oxopyridopyridazineacetic acid derivatives Banavara L. Mylari, William J. Zembrowski, Thomas A. Beyer, Charles E. Aldinger, and Todd W. Siegel pp 2155 - 2162; DOI: 10.1021/jm00090a002 |
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Structure-activity study of hCGRP8-37, a calcitonin gene-related peptide receptor antagonist Murielle Mimeault, Remi Quirion, Yvan Dumont, Serge St-Pierre, and Alain Fournier pp 2163 - 2168; DOI: 10.1021/jm00090a003 |
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Hydantoin bioisosteres. In vivo active spiro hydroxy acetic acid aldose reductase inhibitors Christopher A. Lipinski, Charles E. Aldinger, Thomas A. Beyer, Jon Bordner, Douglas F. Burdi, Donald L. Bussolotti, Philip B. Inskeep, and Todd W. Siegel pp 2169 - 2177; DOI: 10.1021/jm00090a004 |
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Synthesis of carbon-11 labeled iodinated cocaine derivatives and their distribution in baboon brain measured using positron emission tomography D. W. Yu, S. J. Gatley, A. P. Wolf, R. R. MacGregor, S. L. Dewey, J. S. Fowler, and D. J. Schlyer pp 2178 - 2183; DOI: 10.1021/jm00090a005 |
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Synthesis and muscarinic receptor activity of ester derivatives of 2-substituted 2-azabicyclo[2.2.1]heptan-5-ol and -6-ol F. Ivy Carroll, Phillip Abraham, Sanjay Chemburkar, Xu Chang He, S. Wayne Mascarella, Yong Wha Kwon, and David J. Triggle pp 2184 - 2191; DOI: 10.1021/jm00090a006 |
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(.+-.)-Carbocyclic 5'-nor-2'-deoxyguanosine and related purine derivatives: synthesis and antiviral properties Sharadbala D. Patil, Masakazu Koga, Stewart W. Schneller, Robert Snoeck, and Erik De Clercq pp 2191 - 2195; DOI: 10.1021/jm00090a007 |
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Chemistry and anti-HIV properties of 2'-fluoro-2',3'-dideoxyarabinofuranosylpyrimidines Maqbool A. Siddiqui, John S. Driscoll, Victor E. Marquez, Jeri S. Roth, Takuma Shirasaka, Hiroaki Mitsuya, Joseph J. Barchi, and James A. Kelley pp 2195 - 2201; DOI: 10.1021/jm00090a008 |
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Synthesis and thromboxane A2/prostaglandin H2 receptor antagonistic activity of phenol derivatives Shoji Fukumoto, Mitsuru Shiraishi, Zenichi Terashita, Yasuko Ashida, and Yoshiyuki Inada pp 2202 - 2209; DOI: 10.1021/jm00090a009 |
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Synthesis and aromatase inhibition of 3-cycloalkyl-substituted 3-(4-aminophenyl)piperidine-2,6-diones Rolf W. Hartmann, Christine Batzl, Thomas M. Pongratz, and Albrecht Mannschreck pp 2210 - 2214; DOI: 10.1021/jm00090a010 |
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Benzodiazepine receptor affinity and interaction of some N-(indol-3-ylglyoxylyl)amine derivatives Anna Maria Bianucci, Antonio Da Settimo, Federico Da Settimo, Giampaolo Primofiore, Claudia Martini, Gino Giannaccini, and Antonio Lucacchini pp 2214 - 2220; DOI: 10.1021/jm00090a011 |
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Synthesis and receptor binding properties of fluoro- and iodo-substituted high-affinity .sigma.-receptor ligands: identification of potential PET and SPECT .sigma.-receptor imaging agents Brian De Costa, Lilian Radesca, Celia Dominguez, Lisa Di Paolo, and Wayne D. Bowen pp 2221 - 2230; DOI: 10.1021/jm00090a012 |
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Iodoaminopotentidine and related compounds: a new class of ligands with high affinity and selectivity for the histamine H2 receptor Juergen Hirschfeld, Armin Buschauer, Sigurd Elz, Walter Schunack, Martial Ruat, Elisabeth Traiffort, and Jean Charles Schwartz pp 2231 - 2238; DOI: 10.1021/jm00090a013 |
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Synthesis, configuration, and calcium modulatory properties of enantiomerically pure 5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylates Ulrich Rose and Martin Draeger pp 2238 - 2243; DOI: 10.1021/jm00090a014 |
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Selective reversible and irreversible ligands for the .kappa. opioid receptor Chen Yu Cheng, Shou Chien Wu, Ling Wei Hsin, and S. William Tam pp 2243 - 2247; DOI: 10.1021/jm00090a015 |
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Active conformation of a tumor promoter, teleocidin. A molecular dynamics study Takatoshi Kawai, Tazuko Ichinose, Yasuyuki Endo, Koichi Shudo, and Akiko Itai pp 2248 - 2253; DOI: 10.1021/jm00090a016 |
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Nucleosides and nucleotides. 107. 2-(Cycloalkylalkynyl)adenosines: adenosine A2 receptor agonists with potent antihypertensive effects Toichi Abiru, Takanori Miyashita, Yohko Watanabe, Toyofumi Yamaguchi, Haruhiko Machida, and Akira Matsuda pp 2253 - 2260; DOI: 10.1021/jm00090a017 |
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Chemical and enzyme-mediated oxidation of the serotonergic neurotoxin 5,7-dihydroxytryptamine: mechanistic insights Tahereh Tabatabaie and Glenn Dryhurst pp 2261 - 2274; DOI: 10.1021/jm00090a018 |
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Novel functional M1 selective muscarinic agonists. Synthesis and structure-activity relationships of 3-(1,2,5-thiadiazolyl)-1,2,5,6-tetrahydro-1-methylpyridines Per Sauerberg, Preben H. Olesen, Susanne Nielsen, Svend Treppendahl, Malcolm J. Sheardown, Tage Honore, Charles H. Mitch, John S. Ward, Andrew J. Pike, and et al. pp 2274 - 2283; DOI: 10.1021/jm00090a019 |
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Nucleic acid related compounds. 74. Synthesis and biological activity of 2'(and 3')-deoxy-2'(and 3')-methylenenucleoside analogs that function as mechanism-based inhibitors of S-adenosyl-L-homocysteine hydrolase and/or ribonucleotide reductase Morris J. Robins, Vicente Samano, Weijian Zhang, Jan Balzarini, Erik De Clercq, Ronald T. Borchardt, Younha Lee, and Chong Sheng Yuan pp 2283 - 2293; DOI: 10.1021/jm00090a020 |
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Synthesis and evaluation of analogs of (Z)-1-(4-methoxyphenyl)-2-(3,4,5-trimethoxyphenyl)ethene as potential cytotoxic and antimitotic agents Mark Cushman, Dhanapalan Nagarathnam, D. Gopal, Hu Ming He, Chii M. Lin, and Ernest Hamel pp 2293 - 2306; DOI: 10.1021/jm00090a021 |
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2-Acetylpyridine thiocarbonohydrazones. Potent inactivators of herpes simplex virus ribonucleotide reductase Todd A. Blumenkopf, Joan A. Harrington, Cecilia S. Koble, Donald D. Bankston, Robert W. Morrison, Eric C. Bigham, Virgil L. Styles, and Thomas Spector pp 2306 - 2314; DOI: 10.1021/jm00090a022 |
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Structural studies on bio-active compounds. 20. Molecular modeling and crystallographic studies on methylbenzoprim, a potent inhibitor of dihydrofolate reductase Brian J. Denny, Neil S. Ringan, Carl H. Schwalbe, Peter A. Lambert, Michelle A. Meek, Roger J. Griffin, and Malcolm F. G. Stevens pp 2315 - 2320; DOI: 10.1021/jm00090a023 |
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Quinazoline antifolate thymidylate synthase inhibitors: difluoro-substituted benzene ring analogs Timothy J. Thornton, Ann L. Jackman, Peter R. Marsham, Brigid M. O'Connor, Joel A. M. Bishop, and A. Hilary Calvert pp 2321 - 2327; DOI: 10.1021/jm00090a024 |
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Structure-activity studies of potassium channel opening in pinacidil-type cyanoguanidines, nitroethenediamines, thioureas, and ureas Paul W. Manley and Ulrich Quast pp 2327 - 2340; DOI: 10.1021/jm00090a025 |
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7-Oxabicycloheptylprostanoic acids: potent, time-dependent cyclooxygenase inhibitors that induce a conformational change in the prostaglandin endoperoxide synthase protein Indrani Pal, Rebecca Odenwaller, and Lawrence J. Marnett pp 2340 - 2342; DOI: 10.1021/jm00090a026 |
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(E)-1,3-Dialkyl-7-methyl-8-(3,4,5-trimethoxystyryl)xanthines: potent and selective adenosine A2 antagonists Junichi Shimada, Fumio Suzuki, Hiromi Nonaka, Akio Ishii, and Shunji Ichikawa pp 2342 - 2345; DOI: 10.1021/jm00090a027 |
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Book Reviews pp 2346 - 2346; DOI: 10.1021/jm00090a600 |
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Synthesis and anti-HIV activity of isonucleosides Donna M. Huryn, Barbara C. Sluboski, Steve Y. Tam, Manfred Weigele, Iain Sim, Barry D. Anderson, Hiroaki Mitsuya, and Samuel Broder pp 2347 - 2354; DOI: 10.1021/jm00091a001 |
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Conformational analysis of dopamine D-2 receptor antagonists of the benzamide series in relation to a recently proposed D-2 receptor-interaction model Ingrid Pettersson and Tommy Liljefors pp 2355 - 2363; DOI: 10.1021/jm00091a002 |
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2-Alkynyl derivatives of adenosine and adenosine-5'-N-ethyluronamide as selective agonists at A2 adenosine receptors Gloria Cristalli, Alessandra Eleuteri, Sauro Vittori, Rosaria Volpini, Martin J. Lohse, and Karl Norbert Klotz pp 2363 - 2368; DOI: 10.1021/jm00091a003 |
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Structure-activity relationship studies of central nervous system (CNS) agents. 5. Effect of the hydrocarbon chain on the affinity of 4-substituted 1-(3-chlorophenyl)piperazines for 5-HT1A receptor sites Jerzy L. Mokrosz, Marzena Pietrasiewicz, Beata Duszynska, and Marek T. Cegla pp 2369 - 2374; DOI: 10.1021/jm00091a004 |
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Electrophilic opioid ligands. Oxygen-tethered .alpha.-methylene-.gamma.-lactone, acrylate, isothiocyanate, and epoxide derivatives of 6.beta.-naltrexol William E. Dasher, Peter Klein, and Wendel L. Nelson pp 2374 - 2384; DOI: 10.1021/jm00091a005 |
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Ring substituted and other conformationally constrained tyrosine analogs of [cyclic] [D-Pen2,D-Pen5]enkephalin with .delta.-opioid receptor selectivity Geza Toth, K. C. Russell, Geoffrey Landis, Thomas H. Kramer, Lei Fang, Richard Knapp, Peg Davis, Thomas F. Burks, Henry I. Yamamura, and Victor J. Hruby pp 2384 - 2391; DOI: 10.1021/jm00091a006 |
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Substituent variation in azabicyclic triazole- and tetrazole-based muscarinic receptor ligands Sarah M. Jenkins, Harry J. Wadsworth, Steven Bromidge, Barry S. Orlek, Paul A. Wyman, Graham J. Riley, and Julie Hawkins pp 2392 - 2406; DOI: 10.1021/jm00091a007 |
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Synthesis of 3-[(2,3-dihydro-1,1,3-trioxo-1,2-benzisothiazol-2-yl)alkyl] 1,4-dihydropyridine-3,5-dicarboxylate derivatives as calcium channel modulators Carlos E. Sunkel, Miguel Fau de Casa-Juana, Luis Santos, Antonio G. Garcia, Cristina R. Artalejo, Mercedes Villarroya, M. Antonia Gonzalez-Morales, Manuela G. Lopez, Javier Cillero, and et al. pp 2407 - 2414; DOI: 10.1021/jm00091a008 |
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Inhibition of N8-acetylspermidine deacetylase by active-site-directed metal coordinating inhibitors Tien L. Huang, Sasi A. Dredar, Victor A. Manneh, James W. Blankenship, and David S. Fries pp 2414 - 2418; DOI: 10.1021/jm00091a009 |
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1,3,6-Trisubstituted indoles as peptidoleukotriene antagonists: benefits of a second, polar, pyrrole substituent Frederick J. Brown, Laura A. Cronk, David Aharony, and David W. Snyder pp 2419 - 2439; DOI: 10.1021/jm00091a010 |
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Quantitative structure-activity relationships of benzamide derivatives for anti-leukotriene activities Satoru Goto, Zongru Guo, Yukako Futatsuishi, Hitoshi Hori, Zenei Taira, and Hiroshi Terada pp 2440 - 2445; DOI: 10.1021/jm00091a011 |
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Synthesis and antiulcer activity of N-substituted N'-[3-[3-(piperidinomethyl)phenoxy]propyl]ureas: histamine H2-receptor antagonists with potent mucosal protective activity Mitsutomo Miyashita, Toyomi Matsumoto, Hiroshi Matsukubo, Fujio Iinuma, Fukutaro Taga, Haruo Sekiguchi, Katsuhiro Hamada, Kyuya Okamura, and Keigo Nishino pp 2446 - 2451; DOI: 10.1021/jm00091a012 |
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Structure-activity relationship in the gastric cytoprotective effect of several sesquiterpene lactones Oscar S. Giordano, Mauricio J. Pestchanker, Eduardo Guerreiro, Jose R. Saad, Ricardo D. Enriz, Ana M. Rodriguez, Esteban A. Jauregui, Jorge Guzman, Alejandra O. M. Maria, and Graciela H. Wendel pp 2452 - 2458; DOI: 10.1021/jm00091a013 |
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Extraordinarily potent antimalarial compounds: new, structurally simple, easily synthesized, tricyclic 1,2,4-trioxanes. Gary H. Posner, Chang Ho Oh, Lucia Gerena, and Wilbur K. Milhous pp 2459 - 2467; DOI: 10.1021/jm00091a014 |
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NMR studies of an FK-506 analog, [U-carbon-13]ascomycin, bound to FK-506-binding protein Andrew M. Petros, Gerd Gemmecker, Placido Neri, Edward T. Olejniczak, David Nettesheim, Robert X. Xu, Earl G. Gubbins, Harriet Smith, and Stephen W. Fesik pp 2467 - 2473; DOI: 10.1021/jm00091a015 |
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Mixed-inhibitor-prodrug as a new approach toward systemically active inhibitors of enkephalin-degrading enzymes Marie Claude Fournie-Zaluski, Pascal Coric, Serge Turcaud, Evelyne Lucas, Florence Noble, Raphael Maldonado, and Bernard P. Roques pp 2473 - 2481; DOI: 10.1021/jm00091a016 |
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New triazine derivatives as potent modulators of multidrug resistance Alain Dhainaut, Gilbert Regnier, Ghanem Atassi, Alain Pierre, Stephane Leonce, Laurence Kraus-Berthier, and Jean Francois Prost pp 2481 - 2496; DOI: 10.1021/jm00091a017 |
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Novel sulfonamides as potential, systemically active antitumor agents Hiroshi Yoshino, Norihiro Ueda, Jun Niijima, Hiroyuki Sugumi, Yoshihiko Kotake, Nozomu Koyanagi, Kentaro Yoshimatsu, Makoto Asada, Tatsuo Watanabe, and et al. pp 2496 - 2497; DOI: 10.1021/jm00091a018 |
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Isopropyl and phenyl esters of 3.beta.-(4-substituted phenyl)tropan-2.beta.-carboxylic acids. Potent and selective compounds for the dopamine transporter F. Ivy Carroll, Philip Abraham, Anita H. Lewin, Karol A. Parham, John W. Boja, and Michael J. Kuhar pp 2497 - 2500; DOI: 10.1021/jm00091a019 |
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Book Reviews pp 2500 - 2500; DOI: 10.1021/jm00091a600 |
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5-Lipoxygenase: properties, pharmacology, and the quinolinyl(bridged)aryl class of inhibitors John H. Musser and Anthony F. Kreft pp 2501 - 2524; DOI: 10.1021/jm00092a001 |
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A series of potent HIV-1 protease inhibitors containing a hydroxyethyl secondary amine transition state isostere: synthesis, enzyme inhibition, and antiviral activity Thomas J. Tucker, William C. Lumma Jr., Linda S. Payne, Jenny M. Wai, S. Jane De Solms, Elizabeth A. Giuliani, Paul L. Darke, Jill C. Heimbach, Joan A. Zugay, and et al. pp 2525 - 2533; DOI: 10.1021/jm00092a002 |
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Synthesis and x-ray crystallographic analysis of quinazolinone cholecystokinin/gastrin receptor ligands Melvin J. Yu, Jefferson R. McCowan, Norman R. Mason, Jack B. Deeter, and Laurane G. Mendelsohn pp 2534 - 2542; DOI: 10.1021/jm00092a003 |
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Comparative molecular field analysis of anticoccidial triazines James W. McFarland pp 2543 - 2550; DOI: 10.1021/jm00092a004 |
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Preferred antagonist binding state of the N-methyl-D-aspartate receptor: synthesis, pharmacology, and computer modeling of (phosphonomethyl)phenylalanine derivatives Agnes Dorville, Isabelle McCort-Tranchepain, Dominique Vichard, William Sather, Rachid Maroun, Philippe Ascher, and Bernard P. Roques pp 2551 - 2562; DOI: 10.1021/jm00092a005 |
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Structure-activity relationships of a series of 2-amino-4-thiazole-containing renin inhibitors William C. Patt, Harriet W. Hamilton, Michael D. Taylor, Michael J. Ryan, David G. Taylor Jr., Cleo J. C. Connolly, Annette M. Doherty, Sylvester R. Klutchko, Ila Sircar, and et al. pp 2562 - 2572; DOI: 10.1021/jm00092a006 |
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Rationally designed "dipeptoid" analogs of CCK. Acid mimics of the potent and selective non-peptide CCK-B receptor antagonist (CI-988) Martin J. Drysdale, Martyn C. Pritchard, and David C. Horwell pp 2573 - 2581; DOI: 10.1021/jm00092a007 |
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Highly potent and selective heptapeptide antagonists of the neurokinin NK-2 receptor Andrew B. McElroy, Stephen P. Clegg, Martyn J. Deal, George B. Ewan, Russell M. Hagan, Simon J. Ireland, Christopher C. Jordan, Barry Porter, Barry C. Ross, and et al. pp 2582 - 2591; DOI: 10.1021/jm00092a008 |
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The discovery of (2S,3S)-cis-2-(diphenylmethyl)-N-[(2-methoxyphenyl)methyl]-1-azabicyclo[2.2.2]octan-3-amine as a novel, nonpeptide substance P antagonist John A. Lowe, III, Susan E. Drozda, R. Michael Snider, Kelly P. Longo, Stevin H. Zorn, Jean Morrone, Elisa R. Jackson, Stafford McLean, Dianne K. Bryce, and et al. pp 2591 - 2600; DOI: 10.1021/jm00092a009 |
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Methoxytetrahydropyrans. A new series of selective and orally potent 5-lipoxygenase inhibitors Graham C. Crawley, Robert I. Dowell, Philip N. Edwards, Stephen J. Foster, Rodger M. McMillan, Edward R. H. Walker, David Waterson, T. Geoffrey C. Bird, Pierre Bruneau, and Jean Marc Girodeau pp 2600 - 2609; DOI: 10.1021/jm00092a010 |
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Benzazepinone calcium channel blockers. 5. Effects on antihypertensive activity associated with N1 and aromatic substituents Jagabandhu Das, David M. Floyd, S. David Kimball, Keith J. Duff, Michael W. Lago, John Krapcho, Ronald E. White, Richard E. Ridgewell, Mary T. Obermeier, and et al. pp 2610 - 2617; DOI: 10.1021/jm00092a011 |
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Studies on antidiabetic agents. 11. Novel thiazolidinedione derivatives as potent hypoglycemic and hypolipidemic agents Takashi Sohda, Katsutoshi Mizuno, Yu Momose, Hitoshi Ikeda, Takeshi Fujita, and Kanji Meguro pp 2617 - 2626; DOI: 10.1021/jm00092a012 |
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Side chain modified 5-deazatolate and 5-deazatetrahydrotolate analogs as mammalian folylpolyglutamate synthetase and glycinamide ribonucleotide formyltransferase inhibitors: synthesis and in vitro biological evaluation. 47. N-[4-[[(3,4-Dihydro-4-oxo-1,2,3-benzotriazin-6-yl)methyl]amino]benzoyl-L-glutamic acid, a novel a-ring analog of 2-desamino-5,8-dideazafolic acid Andre Rosowsky, Ronald A. Forsch, and Richard G. Moran pp 2626 - 2630; DOI: 10.1021/jm00092a013 |
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Synthesis and structure-activity relationships of cephalosporins with C-3' catechol-containing residues J. C. Arnould, A. Bertrandie, T. G. C. Bird, D. Boucherot, F. Jung, J. J. Lohmann, A. Olivier, J. P. Bailey, W. Bell, and G. M. Davies pp 2631 - 2642; DOI: 10.1021/jm00092a014 |
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Pharmacokinetics of catechol cephalosporins. The effect of incorporating substituents into the catechol moiety on pharmacokinetics in a marmoset model T. G. C. Bird, J. C. Arnould, A. Bertrandie, and F. H. Jung pp 2643 - 2651; DOI: 10.1021/jm00092a015 |
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Novel inhibitors of prolyl 4-hydroxylase. 3. Inhibition by the substrate analog N-oxaloglycine and its derivatives C. Jane Cunliffe, Trevor J. Franklin, Neil J. Hales, and George B. Hill pp 2652 - 2658; DOI: 10.1021/jm00092a016 |
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Nonpeptide angiotensin II receptor antagonists: synthetic and computational chemistry of N-[[4-[2-(2H-tetrazol-5-yl)-1-cycloalken-1-yl]phenyl]methyl]imidazole derivatives and their in vitro activity Ho Shen Lin, Ashraff A. Rampersaud, Karen Zimmerman, Mitchell I. Steinberg, and Donald B. Boyd pp 2658 - 2667; DOI: 10.1021/jm00092a017 |
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Metabolism of 5-hydroxytryptamine by brain synaptosomes and microsomes in the presence of cysteine and glutathione Satendra Singh and Glenn Dryhurst pp 2667 - 2672; DOI: 10.1021/jm00092a018 |
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Inhibitors of blood platelet cAMP phosphodiesterase. 2. Structure-activity relationships associated with 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-ones substituted with functionalized side chains Nicholas A. Meanwell, Bradley C. Pearce, Herbert R. Roth, Edward C. R. Smith, Donald L. Wedding, J. J. Kim Wright, John O. Buchanan, Urzula M. Baryla, Marianne Gamberdella, and et al. pp 2672 - 2687; DOI: 10.1021/jm00092a019 |
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Inhibitors of blood platelet cAMP phosphodiesterase. 3. 1,3-Dihydro-2H-imidazo[4,5-b]quinolin-2-one derivatives with enhanced aqueous solubility Nicholas A. Meanwell, Ronald D. Dennis, Herbert R. Roth, Michael J. Rosenfeld, Edward Smith, J. J. Kim Wright, John O. Buchanan, Catherine L. Brassard, Marianne Gamberdella, and et al. pp 2688 - 2696; DOI: 10.1021/jm00092a020 |
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Acetazolamide-like carbonic anhydrase inhibitors with topical ocular hypotensive activity Simonetta Antonaroli, Armandodoriano Bianco, Mario Brufani, Luciano Cellai, Giuseppe Lo Baido, Edoardo Potier, Luciano Bonomi, Sergio Perfetti, Anna Ida Fiaschi, and Giorgio Segre pp 2697 - 2703; DOI: 10.1021/jm00092a021 |
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Synthesis of the acridone alkaloids, glyfoline and congeners. Structure-activity relationship studies of cytotoxic acridones Tsann Long Su, Bernd Kohler, Ting Chao Chou, Moon Woo Chun, and Kyoichi A. Watanabe pp 2703 - 2710; DOI: 10.1021/jm00092a022 |
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1-(5'-Fluoro-6'-hydroxy-5',6'-dihydrouracil-5'-yl)-5-fluorouracil, a novel N(1)-C(5)-linked dimer that releases 5-fluorouracil by radiation activation under hypoxic conditions Seiichi Nishimoto, Hiroshi Hatta, Hiroyuki Ueshima, and Tsutomu Kagiya pp 2711 - 2712; DOI: 10.1021/jm00092a023 |
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3[4-[1-(6-Fluorobenzo[b]thiophen-3-yl)-4-piperazinyl]butyl]-2,5,5-trimethyl-4-thiazolidinone: a new atypical antipsychotic agent for the treatment of schizophrenia Nicholas J. Hrib, John G. Jurcak, Deborah E. Bregna, Robert W. Dunn, Harry M. Geyer, III, Harold B. Hartman, Joachim E. Roehr, Kendra L. Rogers, Douglas K. Rush, and et al. pp 2712 - 2715; DOI: 10.1021/jm00092a024 |
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Book Reviews pp 2715 - 2716; DOI: 10.1021/jm00092a600 |
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Antitumor agents. 134. New shiraiachrome A and calphostin C-related perylene derivatives as cytotoxic and antiviral agents and inhibitors of protein kinase C Hui Kang Wang, Jing Xi Xie, Jer Jang Chang, Kou Maou Hwang, Su Ying Liu, Lawrence M. Ballas, Jack B. Jiang, and Kuo Hsiung Lee pp 2717 - 2721; DOI: 10.1021/jm00093a001 |
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3'-Spiro nucleosides, a new class of specific human immunodeficiency virus type 1 inhibitors: synthesis and antiviral activity of [2', 5'-bis-O-(tert-butyldimethylsilyl)-.beta.-D-xylo- and -ribofuranose]-3'-spiro-5''-[4''-amino-1'', 2''-oxathiole 2'', 2''-dioxide] (TSAO) pyrimidine nucleosides Maria Jose Camarasa, Maria Jesus Perez-Perez, Ana San-Felix, Jan Balzarini, and Erik De Clercq pp 2721 - 2727; DOI: 10.1021/jm00093a002 |
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Potential prodrug derivatives of 2',3'-didehydro-2',3'-dideoxynucleosides. Preparations and antiviral activities Khairuzzaman B. Mullah, T. Sudhakar Rao, Jan Balzarini, Erik De Clercq, and Wesley G. Bentrude pp 2728 - 2735; DOI: 10.1021/jm00093a003 |
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HIV inhibitory natural products. Part 7. The calanolides, a novel HIV-inhibitory class of coumarin derivatives from the tropical rainforest tree, Calophyllum lanigerum Yoel Kashman, Kirk R. Gustafson, Richard W. Fuller, John H. Cardellina, James B. McMahon, Michael J. Currens, Robert W. Buckheit, Stephen H. Hughes, Gordon M. Cragg, and Michael R. Boyd pp 2735 - 2743; DOI: 10.1021/jm00093a004 |
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HIV-1 neutralization and tumor cell proliferation inhibition in vitro by simplified analogs of pyrido[4,3,2-mn]thiazolo[5,4-b]acridine marine alkaloids Irach B. Taraporewala, James W. Cessac, Tran C. Chanh, Angel V. Delgado, and Raymond F. Schinazi pp 2744 - 2752; DOI: 10.1021/jm00093a005 |
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A molecular-modeling study of the interactions between the antiestrogen drug tamoxifen and several derivatives, and the calcium-binding protein calmodulin Karen J. Edwards, Charles A. Laughton, and Stephen Neidle pp 2753 - 2761; DOI: 10.1021/jm00093a006 |
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Quinoline antifolate thymidylate synthase inhibitors: variation of the C2- and C4-substituents Peter Warner, Andrew J. Barker, Ann L. Jackman, Kenneth D. Burrows, Neal Roberts, Joel A. M. Bishop, Brigid M. O'Connor, and Leslie R. Hughes pp 2761 - 2768; DOI: 10.1021/jm00093a007 |
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Inhibition of collagenase by aranciamycin and aranciamycin derivatives. Mikael Bols, Lise Binderup, Jytte Hansen, and Poul Rasmussen pp 2768 - 2771; DOI: 10.1021/jm00093a008 |
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Inhibitors of human renin with C-termini derived from amides and esters of .alpha.-mercaptoalkanoic acids Wallace T. Ashton, Christine L. Cantone, Richard L. Tolman, William J. Greenlee, Robert J. Lynch, Terry W. Schorn, John F. Strouse, and Peter K. S. Siegl pp 2772 - 2781; DOI: 10.1021/jm00093a009 |
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New potent mitomycin derivatives: synthesis and antitumor activity of 7,7-(ethylenedioxy)mitomycins Yutaka Kanda, Hitoshi Arai, Tadashi Ashizawa, Makoto Morimoto, and Masaji Kasai pp 2781 - 2786; DOI: 10.1021/jm00093a010 |
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Amide, urea, and carbamate analogs of the muscarinic agent [4-[[N-(3-chlorophenyl)carbamoyl]oxy]-2-butynyl]trimethylammonium chloride Bjoern M. Nilsson, Hugo M. Vargas, and Uli Hacksell pp 2787 - 2798; DOI: 10.1021/jm00093a011 |
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Synthesis and anticonvulsant activity of enaminones Ivan O. Edafiogho, Christine N. Hinko, Hyejung Chang, Jacqueline A. Moore, Dianna Mulzac, Jesse M. Nicholson, and K. R. Scott pp 2798 - 2805; DOI: 10.1021/jm00093a012 |
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N-Methylated analogs of Ac[Nle28,31]CCK(26-33): synthesis, activity, and receptor selectivity D. Ron, C. Gilon, M. Hanani, A. Vromen, Z. Selinger, and M. Chorev pp 2806 - 2811; DOI: 10.1021/jm00093a013 |
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Enantiomeric N-substituted N-normetazocines: a comparative study of affinities at .sigma., PCP, and .mu. opioid receptors F. I. Carroll, P. Abraham, K. Parham, X. Bai, X. Zhang, G. A. Brine, S. W. Mascarella, B. R. Martin, E. L. May, C. Sauss, L. Di Paolo, P. Wallace, J. M. Walker, and W.D. Bowen pp 2812 - 2818; DOI: 10.1021/jm00093a014 |
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Stereoisomers of ketoconazole: preparation and biological activity David M. Rotstein, Denis J. Kertesz, Keith A. M. Walker, and David C. Swinney pp 2818 - 2825; DOI: 10.1021/jm00093a015 |
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Probes for narcotic receptor mediated phenomena. 18. Epimeric 6.alpha.- and 6.beta.-iodo-3,14-dihydroxy-17-(cyclopropylmethyl)-4,5.alpha.-epoxymorphinans as potential ligands for opioid receptor single photon emission computed tomography: synthesis, evaluation, and radiochemistry of [125I]-6.beta.-iodo-3,14-dihydroxy-17-(cyclopropylmethyl)-4,5.alpha.-epoxymorphinan Brian R. De Costa, Michael J. Iadarola, Richard B. Rothman, Karen F. Berman, Clifford George, Amy H. Newman, Artin Mahboubi, Arthur E. Jacobson, and Kenner C. Rice pp 2826 - 2835; DOI: 10.1021/jm00093a016 |
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Structural requirements for neuropeptide Y18-36-evoked hypotension: a systematic study R. D. Feinstein, J. H. Boublik, D. Kirby, M. A. Spicer, A. G. Craig, K. Malewicz, N. A. Scott, M. R. Brown, and J. E. Rivier pp 2836 - 2843; DOI: 10.1021/jm00093a017 |
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Preparation and structure-activity relationships of simplified analogs of the antifungal agent cilofungin: a total synthesis approach Robert A. Zambias, Milton L. Hammond, James V. Heck, Ken Bartizal, Charlotte Trainor, George Abruzzo, Dennis M. Schmatz, and Karl M. Nollstadt pp 2843 - 2855; DOI: 10.1021/jm00093a018 |
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2-Substituted 1-azabicycloalkanes, a new class of non-opiate antinociceptive agents John R. Carson, Richard J. Carmosin, Jeffry L. Vaught, Joseph F. Gardocki, Michael J. Costanzo, Robert B. Raffa, and Harold R. Almond pp 2855 - 2863; DOI: 10.1021/jm00093a019 |
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New antiinflammatory agents. 2. 5-Phenyl-3H-imidazo[4,5-c][1,8]naphthyridin-4(5H)-ones: a new class of nonsteroidal antiinflammatory agents with potent activity like glucocorticoids Fumio Suzuki, Takeshi Kuroda, Tadafumi Tamura, Soichiro Sato, Kenji Ohmori, and Shunji Ichikawa pp 2863 - 2870; DOI: 10.1021/jm00093a020 |
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Quenched molecular dynamics simulations of tuftsin and proposed cyclic analogs Stephen D. O'Connor, Paul E. Smith, Fahad Al-Obeidi, and B. Montgomery Pettitt pp 2870 - 2881; DOI: 10.1021/jm00093a021 |
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Nucleosides and nucleotides. 112. 2-(1-Hexyn-1-yl)adenosine-5'-uronamides: a new entry of selective A2 adenosine receptor agonists with potent antihypertensive activity Hiroshi Homma, Yohko Watanabe, Toichi Abiru, Toshihiko Murayama, Yasuharu Nomura, and Akira Matsuda pp 2881 - 2890; DOI: 10.1021/jm00093a022 |
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Anti-HIV-I activity of linked lexitropsins Wuyi Wang and J. William Lown pp 2890 - 2897; DOI: 10.1021/jm00093a023 |
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Fluoronaphthyridines as antibacterial agents. 6. Synthesis and structure-activity relationships of new chiral 7-(1-, 3-, 4-, and 6-methyl-2,5-diazabicyclo[2.2.1]heptan-2-yl)naphthyridine analogs of 7-[(1R,4R)-2,5-diazabicyclo[2.2.1]heptan-2-yl]-1-(1,1-dimethylethyl)-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid. Influence of the configuration on blood pressure in dogs. A quinolone-class effect Philippe Remuzon, Daniel Bouzard, Chantal Guiol, and Jean Pierre Jacquet pp 2898 - 2909; DOI: 10.1021/jm00093a024 |
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Synthesis and antihistaminic activity of some thiazolidin-4-ones M. Vittoria Diurno, Orazio Mazzoni, Eugenio Piscopo, Antonio Calignano, Federico Giordano, and Adele Bolognese pp 2910 - 2912; DOI: 10.1021/jm00093a025 |
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Probing the molecular basis of resistance to pyrimethamine by site-directed mutagenesis Carston R. Wagner and Stephen J. Benkovic pp 2912 - 2915; DOI: 10.1021/jm00093a026 |
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Use of affinity capillary electrophoresis to measure binding constants of ligands to proteins Yen Ho Chu, Luis Z. Avila, Hans A. Biebuyck, and George M. Whitesides pp 2915 - 2917; DOI: 10.1021/jm00093a027 |
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Book Reviews pp 2917 - 2918; DOI: 10.1021/jm00093a600 |
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Synthesis and biological activity of CCK heptapeptide analogs. Effects of conformational constraints and standard modifications on receptor subtype selectivity, functional activity in vitro, and appetite suppression in vivo Mark W. Holladay, Michael J. Bennett, Michael D. Tufano, C. W. Lin, Karen E. Asin, David G. Witte, Thomas R. Miller, Bruce R. Bianchi, A. L. Nikkel, and et al. pp 2919 - 2928; DOI: 10.1021/jm00094a001 |
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Analogs of the .delta. opioid receptor selective cyclic peptide [cyclic][2-D-penicillamine,5-D-penicillamine]-enkephalin: 2',6'-dimethyltyrosine and Gly3-Phe4 amide bond isostere substitutions Nizal S. Chandrakumar, Awilda Stapelfeld, Patrick M. Beardsley, Oscar T. Lopez, Bridget Drury, Elizabeth Anthony, Michael A. Savage, L. Neil Williamson, and Melvin Reichman pp 2928 - 2938; DOI: 10.1021/jm00094a002 |
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Design and synthesis of some substrate analog inhibitors of phospholipase A2 and investigations by NMR and molecular modeling into the binding interactions in the enzyme-inhibitor complex Colin Bennion, Stephen Connolly, Nigel P. Gensmantel, Catherine Hallam, Clive G. Jackson, William U. Primrose, Gordon C. K. Roberts, David H. Robinson, and Pritpal K. Slaich pp 2939 - 2951; DOI: 10.1021/jm00094a003 |
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Molecular determinants of the platelet aggregation inhibitory activity of carbamoylpiperidines Zixia Feng, Ramachander Gollamudi, Elwood O. Dillingham, Stephen E. Bond, Beverly A. Lyman, William P. Purcell, Robert J. Hill, and Walter A. Korfmacher pp 2952 - 2958; DOI: 10.1021/jm00094a004 |
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Synthesis and antiviral activity of methyl derivatives of 9-[2-(phosphonomethoxy)ethyl]guanine Kuo Long Yu, Joanne J. Bronson, Hyekyung Yang, Amy Patick, Masud Alam, Vera Brankovan, Roelf Datema, Michael J. M. Hitchcock, and John C. Martin pp 2958 - 2969; DOI: 10.1021/jm00094a005 |
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Substituted 1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinolines: a novel class of very potent antinociceptive agents with varying degrees of selectivity for .kappa. and .mu. opioid receptors Vittorio Vecchietti, Geoffrey D. Clarke, Roberto Colle, Giulio Dondio, Giuseppe Giardina, Giuseppe Petrone, and Massimo Sbacchi pp 2970 - 2978; DOI: 10.1021/jm00094a006 |
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Quantitative structure-activity relationships of N2-phenylguanines as inhibitors of Herpes simplex virus thymidine kinases Joseph Gambino, Federico Focher, Catherine Hildebrand, Giovanni Maga, Timothy Noonan, Silvio Spadari, and George Wright pp 2979 - 2983; DOI: 10.1021/jm00094a007 |
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DNA-directed alkylating agents. 5. Acridinecarboxamide derivatives of (1,2-diaminoethane)dichloroplatinum(II) Ho H. Lee, Brian D. Palmer, Bruce C. Baguley, Michael Chin, W. David McFadyen, Geoffrey Wickham, Deborah Thorsbourne-Palmer, Laurence P. G. Wakelin, and William A. Denny pp 2983 - 2987; DOI: 10.1021/jm00094a008 |
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TSAO analogs. Stereospecific synthesis and anti-HIV-1 activity of 1-[2',5'-bis-O-(tert-butyldimethylsilyl)-.beta.-D-ribofuranosyl]-3'-spiro-5''-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide)pyrimidine and pyrimidine-modified nucleosides Maria Jesus Perez-Perez, Ana San-Felix, Jan Balzarini, Erik De Clercq, and Maria Jose Camarasa pp 2988 - 2995; DOI: 10.1021/jm00094a009 |
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Template-directed design of a DNA-DNA crosslinker based upon a bis-tomaymycin-duplex adduct Jeh Jeng Wang, G. Craig Hill, and Laurence H. Hurley pp 2995 - 3002; DOI: 10.1021/jm00094a010 |
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Synthesis and antifolate evaluation of 10-ethyl-5-methyl-5,10-dideazaaminopterin and an alternative synthesis of 10-ethyl-10-deazaaminopterin (edatrexate) J. R. Piper, C. A. Johnson, G. M. Otter, and F. M. Sirotnak pp 3002 - 3006; DOI: 10.1021/jm00094a011 |
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A pentahalogenated monoterpene from the red alga Portieria hornemannii produces a novel cytotoxicity profile against a diverse panel of human tumor cell lines Richard W. Fuller, John H. Cardellina, Yoko Kato, Linda S. Brinen, Jon Clardy, Kenneth M. Snader, and Michael R. Boyd pp 3007 - 3011; DOI: 10.1021/jm00094a012 |
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Sulfonylureas: a new class of cancer chemotherapeutic agents Fariborz Mohamadi, Michael M. Spees, and Gerald B. Grindey pp 3012 - 3016; DOI: 10.1021/jm00094a013 |
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Side-chain derivatives of biologically active nucleosides. Part 1. Side-chain analogs of 3'-azido-3'-deoxythymidine (AZT) Johann Hiebl, Erich Zbiral, Jan Balzarini, and Erik De Clercq pp 3016 - 3023; DOI: 10.1021/jm00094a014 |
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Dispiro-1,2,4,5-tetraoxanes: a new class of antimalarial peroxides Jonathan L. Vennerstrom, Hong Ning Fu, William Y. Ellis, Arba L. Ager, James K. Wood, Steven L. Andersen, Lucia Gerena, and Wilbur K. Milhous pp 3023 - 3027; DOI: 10.1021/jm00094a015 |
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Thieno[2,3-b]furan-2-sulfonamides as topical carbonic anhydrase inhibitors George D. Hartman, Wasyl Halczenko, John D. Prugh, Robert L. Smith, Michael F. Sugrue, Pierre Mallorga, Stuart R. Michelson, William C. Randall, Harvey Schwam, and John M. Sondey pp 3027 - 3033; DOI: 10.1021/jm00094a016 |
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PgH2 analogs as potential antiplatelet derivatives Dimitri Komiotis, Chang T. Lim, J. P. Dieter, G. C. Le Breton, and D. L. Venton pp 3033 - 3039; DOI: 10.1021/jm00094a017 |
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Improved brain delivery of AZT using a glycosyl phosphotriester prodrug Abdelkader Namane, Catherine Gouyette, Marie Paule Fillion, Gilles Fillion, and Huynh Dinh Tam pp 3039 - 3044; DOI: 10.1021/jm00094a018 |
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Oxygen isosteric derivatives of 3-(3-hydroxyphenyl)-N-n-propylpiperidine Roberto Perrone, Francesco Berardi, Marcello Leopoldo, Vincenzo Tortorella, Marcello D. Lograno, Eugenia Daniele, and Stefano Govoni pp 3045 - 3049; DOI: 10.1021/jm00094a019 |
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2,3-Epoxy-10-aza-10,11-dihydrosqualene, a high-energy intermediate analog inhibitor of 2,3-oxidosqualene cyclase Maurizio Ceruti, Gianni Balliano, Franca Viola, Giorgio Grosa, Flavio Rocco, and Luigi Cattel pp 3050 - 3058; DOI: 10.1021/jm00094a020 |
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Novel indolodioxanes with antihypertensive effects: potent ligands for the 5-HT1A receptor Michael D. Ennis, Mark E. Baze, Martin W. Smith, Charles F. Lawson, Robert B. McCall, Robert A. Lahti, and Montford F. Piercey pp 3058 - 3066; DOI: 10.1021/jm00094a021 |
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Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure Fumio Suzuki, Junichi Shimada, Hideaki Mizumoto, Akira Karasawa, Kazuhiro Kubo, Hiromi Nonaka, Akio Ishii, and Takashi Kawakita pp 3066 - 3075; DOI: 10.1021/jm00094a022 |
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5'-Azido-.DELTA.8-THC: a novel photoaffinity label for the cannabinoid receptor Avgui Charalambous, Guo Yan, Devin B. Houston, Allyn C. Howlett, David R. Compton, Billy R. Martin, and Alexandros Makriyannis pp 3076 - 3079; DOI: 10.1021/jm00094a023 |
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Penicillin derived C2-symmetric dimers as novel inhibitors of HIV-1 proteinase David C. Humber, Nicholas Cammack, Jonathan A. V. Coates, Kevin N. Cobley, David C. Orr, Richard Storer, Gordon G. Weingarten, and Malcolm P. Weir pp 3080 - 3081; DOI: 10.1021/jm00094a024 |
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Disodium (R,R)-5-[2-[[2-(3-chlorophenyl)-2-hydroxyethyl]amino]propyl]-1,3-benzodioxole-2,2-dicarboxylate (CL 316,243). A potent .beta.-adrenergic agonist virtually specific for .beta.3 receptors. A promising antidiabetic and antiobesity agent Jonathan D. Bloom, Minu D. Dutia, Bernard D. Johnson, Allan Wissner, Michael G. Burns, Elwood E. Largis, Jo Alene Dolan, and Thomas H. Claus pp 3081 - 3084; DOI: 10.1021/jm00094a025 |
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Conformational preferences of the .kappa.-selective opioid agonist U50488. A combined molecular mechanics and nuclear magnetic resonance study Mark Froimowitz, Christine M. DiMeglio, and Alexandros Makriyannis pp 3085 - 3094; DOI: 10.1021/jm00095a001 |
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Mapping the binding site of tissue kallikrein: preparation and testing of all possible substrate analog inhibitors homologous with the sequence of kininogen between Ser386 and Gln392 Milind S. Deshpande and James Burton pp 3094 - 3102; DOI: 10.1021/jm00095a002 |
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Synthesis and pharmacological evaluation of enantiomerically pure 4-deoxy-4-fluoromuscarines Pierfrancesco Bravo, Giuseppe Resnati, Piero Angeli, Massimo Frigerio, Fiorenza Viani, Alberto Arnone, Gabriella Marucci, and Franco Cantalamessa pp 3102 - 3110; DOI: 10.1021/jm00095a003 |
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NMDA antagonist activity of (.+-.)-(2SR,4RS)-4-(1H-tetrazol-5-ylmethyl)piperidine-2-carboxylic acid residues with the (-)-2R,4S-isomer Paul L. Ornstein, Darryle D. Schoepp, M. Brian Arnold, Noel D. Jones, Jack B. Deeter, David Lodge, and J. David Leander pp 3111 - 3115; DOI: 10.1021/jm00095a004 |
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1,4-Dihydropyridines as antagonists of platelet activating factor. 1. Synthesis and structure-activity relationships of 2-(4-heterocyclyl)phenyl derivatives Kelvin Cooper, M. Jonathan Fray, M. John Parry, Kenneth Richardson, and John Steele pp 3115 - 3129; DOI: 10.1021/jm00095a005 |
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Syntheses and affinities of novel organometallic-labeled estradiol derivatives: a structure-affinity relationship Hani El Amouri, Anne Vessieres, Dominique Vichard, Siden Top, Michel Gruselle, and Gerard Jaouen pp 3130 - 3135; DOI: 10.1021/jm00095a006 |
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Synthetic nonpsychotropic cannabinoids with potent antiinflammatory, analgesic, and leukocyte antiadhesion activities Sumner H. Burstein, Charlene A. Audette, Aviva Breuer, William A. Devane, Sharona Colodner, Sharon A. Doyle, and Raphael Mechoulam pp 3135 - 3141; DOI: 10.1021/jm00095a007 |
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Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine Matthew J. Valli, Yunzhao Tang, J. W. Kosh, James M. Chapman, and J. Walter Sowell pp 3141 - 3147; DOI: 10.1021/jm00095a008 |
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Novel 1-(pyridylphenyl)-1-phenyl-2-imidazolylethanols with topical antiinflammatory activity Stephen W. Wright, Richard R. Harris, Robert J. Collins, Ronald L. Corbett, Alicia M. Green, Eric A. Wadman, and Douglas G. Batt pp 3148 - 3155; DOI: 10.1021/jm00095a009 |
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.omega.-[(.omega.-Arylalkyl)aryl]alkanoic acids: a new class of specific LTA4 hydrolase inhibitors Richard Labaudiniere, Gerd Hilboll, Alicia Leon-Lomeli, Hans Heiner Lautenschlaeger, Michael Parnham, Peter Kuhl, and Norbert Dereu pp 3156 - 3169; DOI: 10.1021/jm00095a010 |
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.omega.-[(.omega.-Arylalkyl)thienyl]alkanoic acids: from specific LTA4 hydrolase inhibitors to LTB4 receptor antagonists Richard Labaudiniere, Gerd Hilboll, Alicia Leon-Lomeli, Bernard Terlain, Francoise Cavy, Michael Parnham, Peter Kuhl, and Norbert Dereu pp 3170 - 3179; DOI: 10.1021/jm00095a011 |
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Benzothiazole hydroxy ureas as inhibitors of 5-lipoxygenase: use of the hydroxyurea moiety as a replacement for hydroxamic acid Michael N. Greco, William E. Hageman, Eugene T. Powell, Joseph J. Tighe, and Francis J. Persico pp 3180 - 3183; DOI: 10.1021/jm00095a012 |
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Studies on neurokinin antagonists. 2. Design and structure-activity relationships of novel tripeptide substance P antagonists, N.alpha.-[N.alpha.-(N.alpha.-acetyl-L-threonyl)-N1-formyl-D-tryptophyl]-N-methyl-N-(phenylmethyl)-L-phenylalaninamide and its related compounds Daijiro Hagiwara, Hiroshi Miyake, Hiroshi Morimoto, Masako Murai, Takashi Fujii, and Masaaki Matsuo pp 3184 - 3191; DOI: 10.1021/jm00095a013 |
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3'-Azido-3',5'-dideoxythymidine-5'-methylphosphonic acid diphosphate: synthesis and HIV-1 reverse transcriptase inhibition. G. A. Freeman, J. L. Rideout, W. H. Miller, and J. E. Reardon pp 3192 - 3196; DOI: 10.1021/jm00095a014 |
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S-(5'-Deoxy-5'-adenosyl)-1-ammonio-4-(methylsulfonio)-2-cyclopentene: a potent, enzyme-activated irreversible inhibitor of S-adenosylmethionine decarboxylase Yongqian Wu and Patrick M. Woster pp 3196 - 3201; DOI: 10.1021/jm00095a015 |
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Application of neural networks: quantitative structure-activity relationships of the derivatives of 2,4-diamino-5-(substituted-benzyl)pyrimidines as DHFR inhibitors Sung Sau So and W. Graham Richards pp 3201 - 3207; DOI: 10.1021/jm00095a016 |
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N-(5,5-diacetoxypent-1-yl)doxorubicin: a new intensely potent doxorubicin analog Abdallah Cherif and David Farquhar pp 3208 - 3214; DOI: 10.1021/jm00095a017 |
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Hypoxia-selective antitumor agents. 5. Synthesis of water-soluble nitroaniline mustards with selective cytotoxicity for hypoxic mammalian cells Brian D. Palmer, William R. Wilson, Stephen Cliffe, and William A. Denny pp 3214 - 3222; DOI: 10.1021/jm00095a018 |
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Antiviral and antitumor structure-activity relationship studies on tetracyclic eudistomines Jan H. Van Maarseveen, Pedro H. H. Hermkens, Erik De Clercq, Jan Balzarini, Hans W. Scheeren, and Chris G. Kruse pp 3223 - 3230; DOI: 10.1021/jm00095a019 |
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Synthesis and antiviral evaluation of N-carboxamidine-substituted analogs of 1-.beta.-D-ribofuranosyl-1,2,4-triazole-3-carboxamidine hydrochloride. Bjarne Gabrielsen, Michael J. Phelan, Luis Barthel-Rosa, Cathy See, John W. Huggins, Deborah F. Kefauver, Thomas P. Monath, Michael A. Ussery, Gwendolyn N. Chmurny, and et al. pp 3231 - 3238; DOI: 10.1021/jm00095a020 |
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Histamine H2-receptor agonists. Synthesis, in vitro pharmacology, and qualitative structure-activity relationships of substituted 4- and 5-(2-aminoethyl)thiazoles John C. Eriks, Henk Van der Goot, Geert Jan Sterk, and Hendrik Timmerman pp 3239 - 3246; DOI: 10.1021/jm00095a021 |
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Synthesis, characterization, and Ca2+ antagonistic activity of diltiazem metabolites Rongshi Li, Patrick S. Farmer, Mei Xie, Michael A. Quilliam, Stephen Pleasance, Susan E. Howlett, and Pollen K. F. Yeung pp 3246 - 3253; DOI: 10.1021/jm00095a022 |
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Dihydropyrimidine calcium channel blockers. 4. Basic 3-substituted-4-aryl-1,4-dihydropyrimidine-5-carboxylic acid esters. Potent antihypertensive agents George C. Rovnyak, Karnail S. Atwal, Anders Hedberg, S. David Kimball, Suzanne Moreland, Jack Z. Gougoutas, Brian C. O'Reilly, Joseph Schwartz, and Mary F. Malley pp 3254 - 3263; DOI: 10.1021/jm00095a023 |
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Conformationally restrained, chiral (phenylisopropyl)amino-substituted pyrazolo[3,4-d]pyrimidines and purines with selectivity for adenosine A1 and A2 receptors Norton P. Peet, Nelsen L. Lentz, Shyam Sunder, Mark W. Dudley, and Ann Marie L. Ogden pp 3263 - 3269; DOI: 10.1021/jm00095a024 |
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Urea and 2-imidazolidone derivatives of the muscarinic agents oxotremorine and N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide Bjoern M. Nilsson, Hugo M. Vargas, and Uli Hacksell pp 3270 - 3279; DOI: 10.1021/jm00095a025 |
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New vitamin D3 derivatives with unexpected antiproliferative activity: 1-(hydroxymethyl)-25-hydroxyvitamin D3 homologs Gary H. Posner, Todd D. Nelson, Kathryn Z. Guyton, and Thomas W. Kensler pp 3280 - 3287; DOI: 10.1021/jm00095a026 |
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Pyridazines. 63. Novel thiosemicarbazones derived from formyl- and acyldiazines: synthesis, effects on cell proliferation, and synergism with antiviral agents Johnny Easmon, Gottfried Heinisch, Wolfgang Holzer, and Brigitte Rosenwirth pp 3288 - 3296; DOI: 10.1021/jm00095a027 |
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4-Methyl-3-(arylsulfonyl)furoxans: a new class of potent inhibitors of platelet aggregation R. Calvino, R. Fruttero, D. Ghigo, A. Bosia, G. P. Pescarmona, and A. Gasco pp 3296 - 3300; DOI: 10.1021/jm00095a028 |
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Design of a functional hexapeptide antagonist of endothelin Wayne L. Cody, Annette M. Doherty, John X. He, Patricia L. DePue, Stephen T. Rapundalo, Gary A. Hingorani, Terry C. Major, Robert L. Panek, David T. Dudley, and et al. pp 3301 - 3303; DOI: 10.1021/jm00095a029 |
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Time-dependent inhibition of human placental aromatase with a 2,19-methyleneoxy-bridged androstenedione Norton P. Peet, Joseph P. Burkhart, C. Lee Wright, and J. O'Neal Johnston pp 3303 - 3306; DOI: 10.1021/jm00095a030 |
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Book Reviews pp 3306 - 3306; DOI: 10.1021/jm00095a600 |
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Novel 5-HT3 antagonists. Isoquinolinones and 3-aryl-2-pyridones Toshiaki Matsui, Tsuneyuki Sugiura, Hisao Nakai, Sadahiko Iguchi, Satoshi Shigeoka, Hideo Takada, Yoshihiko Odagaki, Yuhki Nagao, Yasuyuki Ushio, and et al. pp 3307 - 3319; DOI: 10.1021/jm00096a001 |
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Synthesis and excitatory amino acid pharmacology of a series of heterocyclic-fused quinoxalinones and quinazolinones Loretta A. McQuaid, Edward C. R. Smith, Kimberly K. South, Charles H. Mitch, Darryle D. Schoepp, Rebecca A. True, David O. Calligaro, Patrick J. O'Malley, David Lodge, and Paul L. Ornstein pp 3319 - 3324; DOI: 10.1021/jm00096a002 |
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Synthesis and pharmacological studies of N-substituted 6-[(2-aminoethyl)amino]-1,3-dimethyl-2,4(1H,3H)-pyrimidinediones, novel class III antiarrhythmic agents Tsutomu Katakami, Tatsuro Yokoyama, Michihiko Miyamoto, Haruki Mori, Nobuya Kawauchi, Tadahito Nobori, Kunio Sannohe, Tatsuo Kaiho, and Joji Kamiya pp 3325 - 3330; DOI: 10.1021/jm00096a003 |
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Synthesis of a homologous series of ketomethylene arginyl pseudodipeptides and application to low molecular weight hirudin-like thrombin inhibitors John DiMaio, Bernard Gibbs, Jean Lefebvre, Yasuo Konishi, Debra Munn, Shi Yi Yue, and Wilfried Hornberger pp 3331 - 3341; DOI: 10.1021/jm00096a004 |
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Determination of the absolute configuration of the active amlodipine enantiomer as (-)-S: a correction Siegfried Goldmann, Juergen Stoltefuss, and Liborius Born pp 3341 - 3344; DOI: 10.1021/jm00096a005 |
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Synthesis and functional evaluation of a peptide derivative of 1-.beta.-D-arabinofuranosylcytosine Zoltan Balajthy, Janos Aradi, Ildiko T. Kiss, and Pal Elodi pp 3344 - 3349; DOI: 10.1021/jm00096a006 |
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cis-Bis(pyridine)platinum(II) organoamides with unexpected growth inhibition properties and antitumor activity Lorraine K. Webster, Glen B. Deacon, David P. Buxton, Brian L. Hillcoat, Alison M. James, Ian A. G. Roos, Robin J. Thomson, Laurence P. G. Wakelin, and Tracey L. Williams pp 3349 - 3353; DOI: 10.1021/jm00096a007 |
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Synthesis and antibronchospastic activity of 8-alkoxy- and 8-(alkylamino)imidazo[1,2-a]pyrazines Pierre A. Bonnet, Alain Michel, Florence Laurent, Claire Sablayrolles, Eliane Rechencq, Jean C. Mani, Maurice Boucard, and Jean P. Chapat pp 3353 - 3358; DOI: 10.1021/jm00096a008 |
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Synthesis and chemical characterization of N-substituted phenoxazines directed toward reversing vinca alkaloid resistance in multidrug-resistant cancer cells Kuntebommanahalli N. Thimmaiah, Julie K. Horton, Ramakrishnan Seshadri, Mervyn Israel, Janet A. Houghton, Franklin C. Harwood, and Peter J. Houghton pp 3358 - 3364; DOI: 10.1021/jm00096a009 |
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Synthesis and biological activity of ketomethylene pseudopeptide analogs as thrombin inhibitors Leifeng Cheng, Christopher A. Goodwin, Michael F. Schully, Vijay V. Kakkar, and Goran Claeson pp 3364 - 3369; DOI: 10.1021/jm00096a010 |
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3',3'-Difluoro-3'-deoxythymidine: comparison of anti-HIV activity to 3'-fluoro-3'-deoxythymidine Donald E. Bergstrom, Andrew W. Mott, Erik De Clercq, Jan Balzarini, and Daniel J. Swartling pp 3369 - 3372; DOI: 10.1021/jm00096a011 |
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The synthesis and antiviral properties of (.+-.)-5'-noraristeromycin and related purine carbocyclic nucleosides. A new lead for anti-human cytomegalovirus agent design Sharadbala D. Patil, Stewart W. Schneller, Mitsuaki Hosoya, Robert Snoeck, Graciela Andrei, Jan Balzarini, and Erik De Clercq pp 3372 - 3377; DOI: 10.1021/jm00096a012 |
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Antitumor imidazotetrazines. 25. Crystal structure of 8-carbamoyl-3-methylimidazo[5,1-d]-1,2,3,5-tetrazin-4(3H)-one (temozolomide) and structural comparisons with the related drugs mitozolomide and DTIC P. R. Lowe, C. E. Sansom, C. H. Schwalbe, M. F. G. Stevens, and A. S. Clark pp 3377 - 3382; DOI: 10.1021/jm00096a013 |
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Energy aspects of oil/water partition leading to the novel hydrophobic parameters for the analysis of quantitative structure-activity relationships Yong Zhong Da, Katsuhiko Ito, and Hideaki Fujiwara pp 3382 - 3387; DOI: 10.1021/jm00096a014 |
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The synthesis and biological evaluation of dihydroeptastatin, a novel inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase Elisabeth A. Bone, Alan H. Davidson, Christopher N. Lewis, and Richard S. Todd pp 3388 - 3393; DOI: 10.1021/jm00096a015 |
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Non-prostanoid thromboxane A2 receptor antagonists with a dibenzoxepin ring system. 1 Etsuo Ohshima, Hitoshi Takami, Hideyuki Sato, Hiroyuki Obase, Ichiro Miki, Akio Ishii, Akira Karasawa, and Kazuhiro Kubo pp 3394 - 3402; DOI: 10.1021/jm00096a016 |
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Non-prostanoid thromboxane A2 receptor antagonists with a dibenzoxepin ring system. 2 Etsuo Ohshima, Hitoshi Takami, Hideyuki Sato, Shinichiro Mohri, Hiroyuki Obase, Ichiro Miki, Akio Ishii, Shiro Shirakura, Akira Karasawa, and Kazuhiro Kubo pp 3402 - 3413; DOI: 10.1021/jm00096a017 |
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Reversible inhibitors of the gastric (H+/K+)-ATPase. 3. 3-Substituted-4-(phenylamino)quinolines Robert J. Ife, Thomas H. Brown, David J. Keeling, Colin A. Leach, Malcolm L. Meeson, Michael E. Parsons, David R. Reavill, Colin J. Theobald, and Kenneth J. Wiggall pp 3413 - 3422; DOI: 10.1021/jm00096a018 |
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3-Phenyl-4-hydroxyquinolin-2(1H)-ones: potent and selective antagonists at the strychnine-insensitive glycine site on the N-methyl-D-aspartate receptor complex Loretta A. McQuaid, Edward C. R. Smith, David Lodge, Etienne Pralong, James H. Wikel, David O. Calligaro, and Patrick J. O'Malley pp 3423 - 3425; DOI: 10.1021/jm00096a019 |
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Specific inhibition of HIV-1 protease by boronated porphyrins Dianne L. DeCamp, Lilia M. Babe, Rafael Salto, Jeanne L. Lucich, Myoung Seo Koo, Stephen B. Kahl, and Charles S. Craik pp 3426 - 3428; DOI: 10.1021/jm00096a020 |
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Antimalarial drugs. 64. Synthesis and antimalarial properties of 1-imino derivatives of 7-chloro-3-substituted-3,4-dihydro-1,9(2H,10H)-acridinediones and related structures Stephen J. Kesten, Margaret J. Degnan, Jocelyn Hung, Dennis J. McNamara, Daniel F. Ortwine, Susan E. Uhlendorf, and Leslie M. Werbel pp 3429 - 3447; DOI: 10.1021/jm00097a001 |
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Modeling of G-protein-coupled receptors: application to dopamine, adrenaline, serotonin, acetylcholine, and mammalian opsin receptors Susanne Trumpp-Kallmeyer, Jan Hoflack, Anne Bruinvels, and Marcel Hibert pp 3448 - 3462; DOI: 10.1021/jm00097a002 |
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Acyclic analogs of lipid A: synthesis and biological activities. Murty A. R. C. Bulusu, Peter Waldstaetten, Johannes Hildebrandt, Eberhard Schuetze, and Gerhard Schulz pp 3463 - 3469; DOI: 10.1021/jm00097a003 |
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Synthesis and antibacterial activity of 1-(substituted pyrrolyl)-7-(substituted amino)-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids Jianhui Liu and Huiyuan Guo pp 3469 - 3473; DOI: 10.1021/jm00097a004 |
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Development, synthesis, and biological evaluation of (-)-trans-(2S,5S)-2-[3-[(2-oxopropyl)sulfonyl]-4-n-propoxy-5-(3-hydroxypropoxy)-phenyl]-5-(3,4,5-trimethoxyphenyl)tetrahydrofuran, a potent orally active platelet-activating factor (PAF) antagonist and its water-soluble prodrug phosphate ester N. N. Girotra, T. Biftu, M. M. Ponpipom, J. J. Acton, A. W. Alberts, T. N. Bach, R. G. Ball, R. L. Bugianesi, J. C. Chabala, and et al. pp 3474 - 3482; DOI: 10.1021/jm00097a005 |
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Nonprostanoid prostacyclin mimetics. 2. 4,5-diphenyloxazole derivatives. Nicholas A. Meanwell, Michael J. Rosenfeld, Ashok K. Trehan, J. J. Kim Wright, Catherine L. Brassard, John O. Buchanan, Marianne E. Federici, J. Stuart Fleming, Marianne Gamberdella, and et al. pp 3483 - 3497; DOI: 10.1021/jm00097a006 |
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Nonprostanoid prostacyclin mimetics. 3. Structural variations of the diphenyl heterocycle moiety Nicholas A. Meanwell, Michael J. Rosenfeld, Ashok K. Trehan, Jeffrey L. Romine, J. J. Kim Wright, Catherine L. Brassard, John O. Buchanan, Marianne E. Federici, J. Stuart Fleming, Marianne Gamberdella, George B. Zavoico, and Steven M. Seiler pp 3498 - 3512; DOI: 10.1021/jm00097a007 |
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Excitatory amino acid receptor ligands. Synthesis and biological activity of 3-isoxazolol amino acids structurally related to homoibotenic acid Inge T. Christensen, Bjarke Ebert, Ulf Madsen, Birgitte Nielsen, Lotte Brehm, and Povl Krogsgaard-Larsen pp 3512 - 3519; DOI: 10.1021/jm00097a008 |
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Flavones. 3. Synthesis, biological activities, and conformational analysis of isoflavone derivatives and related compounds Edwin S. C. Wu, James T. Loch, Bruce H. Toder, Alfonso R. Borrelli, Daniel Gawlak, Lesley A. Radov, and Nigel P. Gensmantel pp 3519 - 3525; DOI: 10.1021/jm00097a009 |
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Renin inhibitors containing new P1-P1' dipeptide mimetics with heterocycles in P1' Peter Raddatz, Alfred Jonczyk, Klaus Otto Minck, Friedrich Rippmann, Christine Schittenhelm, and Claus Jochen Schmitges pp 3525 - 3536; DOI: 10.1021/jm00097a010 |
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6-Alkyl-12-formylindolo[2,1-a]isoquinolines. Syntheses, estrogen receptor binding affinities, and stereospecific cytostatic activity Thomas Polossek, Reinhard Ambros, Silvia Von Angerer, Gert Brandl, Albrecht Mannschreck, and Erwin Von Angerer pp 3537 - 3547; DOI: 10.1021/jm00097a011 |
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6-Substituted decahydroisoquinoline-3-carboxylic acids as potent and selective conformationally constrained NMDA receptor antagonists Paul L. Ornstein, Darryle D. Schoepp, M. Brian Arnold, Nancy K. Augenstein, David Lodge, John D. Millar, John Chambers, Jack Campbell, Jonathan W. Paschal, and et al. pp 3547 - 3560; DOI: 10.1021/jm00097a012 |
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Carboxamide group conformation in the nicotinamide and thiazole-4-carboxamide rings: implications for enzyme binding Hong Li and Barry M. Goldstein pp 3560 - 3567; DOI: 10.1021/jm00097a013 |
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5,5-Disubstituted hydantoins: syntheses and anti-HIV activity Robert N. Comber, Robert C. Reynolds, Joyce D. Friedrich, Roupen A. Manguikian, Robert W. Buckheit, Jackie W. Truss, William M. Shannon, and John A. Secrist pp 3567 - 3572; DOI: 10.1021/jm00097a014 |
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2-Nitroimidazole dual-function bioreductive drugs: studies on the effects of regioisomerism and side-chain structural modifications on differential cytotoxicity and radiosensitization by aziridinyl and oxiranyl derivatives Matthew A. Naylor, Michael D. Threadgill, Paul Webb, Ian J. Stratford, Miriam A. Stephens, E. Martin Fielden, and Gerald E. Adams pp 3573 - 3578; DOI: 10.1021/jm00097a015 |
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7,8-Dihydro-8-ethyl-2-(3-noradamantyl)-4-propyl-1H-imidazo[2,1-i]purin-5(4H)-one: a potent and water-soluble adenosine A1 antagonist Fumio Suzuki, Junichi Shimada, Hiromi Nonaka, Akio Ishii, Shizuo Shiozaki, Shunji Ichikawa, and Eikichi Ono pp 3578 - 3581; DOI: 10.1021/jm00097a016 |
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N-(1-Oxododecyl)-4.alpha.,10-dimethyl-8-aza-trans-decal-3.beta.-ol: a potent competitive inhibitor of 2,3-oxidosqualene cyclase M. Woods Wannamaker, Philip P. Waid, William A. Van Sickle, James R. McCarthy, Pamela K. Wilson, Gerald L. Schatzman, and William R. Moore pp 3581 - 3583; DOI: 10.1021/jm00097a017 |
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Fatty acid amides: scooting mode-based discovery of tight-binding competitive inhibitors of secreted phospholipases A2 Mahendra K. Jain, Farideh Ghomashchi, Bao Zhu Yu, Timothy Bayburt, Dennis Murphy, David Houck, James Brownell, John C. Reid, James E. Solowiej, and et al. pp 3584 - 3586; DOI: 10.1021/jm00097a018 |
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Book Reviews pp 3586 - 3586; DOI: 10.1021/jm00097a600 |
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A half century in medicinal chemistry with major emphasis on pain-relieving drugs and their antagonists Everette L. May pp 3587 - 3594; DOI: 10.1021/jm00098a001 |
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Hypocholesterolemic activity of synthetic and natural tocotrienols. Bradley C. Pearce, Rex A. Parker, Michael E. Deason, Asaf A. Qureshi, and J. J. Kim Wright pp 3595 - 3606; DOI: 10.1021/jm00098a002 |
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Novel positive inotropic agents: synthesis and biological activities of 6-(3-amino-2-hydroxypropoxy)-2(1H)-quinolinone derivatives Takafumi Fujioka, Shuji Teramoto, Toyoki Mori, Tetsumi Hosokawa, Takumi Sumida, Michiaki Tominaga, and Youichi Yabuuchi pp 3607 - 3612; DOI: 10.1021/jm00098a003 |
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Synthesis and biological activity of trans-(.+-.)-N-methyl-2-(3-pyridyl)-2-tetrahydrothiopyrancarbothioamide 1-oxide (RP 49356) and analogs: a new class of potassium channel opener Thomas J. Brown, Robert F. Chapman, David C. Cook, Terance W. Hart, Iain M. McLay, Roy Jordan, Jonathan S. Mason, Malcolm N. Palfreyman, Roger J. A. Walsh, and et al. pp 3613 - 3624; DOI: 10.1021/jm00098a004 |
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1-(2-Aminoethyl)-3-methyl-8,9-dihydropyrano[3,2-e]indole: a rotationally restricted phenolic analog of the neurotransmitter serotonin and agonist selective for serotonin (5-HT2-type) receptors John E. Macor, Carol B. Fox, Celeste Johnson, B. Kenneth Koe, Lorraine A. Lebel, and Stevin H. Zorn pp 3625 - 3632; DOI: 10.1021/jm00098a005 |
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Antiallergic and cytoprotective activity of new N-phenylbenzamido acid derivatives. Francesco Makovec, Walter Peris, Laura Revel, Roberto Giovanetti, Daniele Redaelli, and Lucio C. Rovati pp 3633 - 3640; DOI: 10.1021/jm00098a006 |
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N1-Hydroxylated derivatives of chlorpropamide and its analogs as inhibitors of aldehyde dehydrogenase in vivo Melinda J. C. Lee, James A. Elberling, and Herbert T. Nagasawa pp 3641 - 3647; DOI: 10.1021/jm00098a007 |
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Prodrugs of nitroxyl as inhibitors of aldehyde dehydrogenase Melinda J. C. Lee, Herbert T. Nagasawa, James A. Elberling, and Eugene G. DeMaster pp 3648 - 3652; DOI: 10.1021/jm00098a008 |
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Truncated, branched, and/or cyclic analogs of neuropeptide Y: importance of the pancreatic peptide fold in the design of specific Y2 receptor ligands M. T. Reymond, L. Delmas, S. C. Koerber, M. R. Brown, and J. E. Rivier pp 3653 - 3659; DOI: 10.1021/jm00098a009 |
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Comparative molecular field analysis of polyhalogenated dibenzo-p-dioxins, dibenzofurans, and biphenyls Chris L. Waller and James D. McKinney pp 3660 - 3666; DOI: 10.1021/jm00098a010 |
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Synthesis and antitumor activity of 3- and 5-hydroxy-4-methylpyridine-2-carboxaldehyde thiosemicarbazones Yuqiang Wang, Mao Chin Liu, Tai Shun Lin, and Alan C. Sartorelli pp 3667 - 3671; DOI: 10.1021/jm00098a011 |
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Synthesis and antitumor activity of amino derivatives of pyridine-2-carboxaldehyde thiose micarbazone Mao Chin Liu, Tai Chun Lin, and Alan C. Sartorelli pp 3672 - 3677; DOI: 10.1021/jm00098a012 |
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5,10-Methylenetetrahydro-5-deazafolic acid and analogs: synthesis and biological activities Aleem Gangjee, Jasmin Patel, Roy L. Kisliuk, and Yvette Gaumont pp 3678 - 3685; DOI: 10.1021/jm00098a013 |
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Antimitotic agents: structure-activity studies with some pyridine derivatives Carroll Temple, Gregory A. Rener, William R. Waud, and Patricia E. Noker pp 3686 - 3690; DOI: 10.1021/jm00098a014 |
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Novel 1,2,4-oxadiazoles and 1,2,4-thiadiazoles as dual 5-lipoxygenase and cyclooxygenase inhibitors Paul C. Unangst, Gary P. Shrum, David T. Connor, Richard D. Dyer, and Denis J. Schrier pp 3691 - 3698; DOI: 10.1021/jm00098a015 |
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Conformational analysis of the aromatase inhibitor 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione (rogletimide) and discovery of potent 5-alkyl derivatives Raymond McCague and Martin G. Rowlands pp 3699 - 3704; DOI: 10.1021/jm00098a016 |
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Aliphatic propargylamines: potent, selective, irreversible monoamine oxidase B inhibitors Peter H. Yu, Bruce A. Davis, and Alan A. Boulton pp 3705 - 3713; DOI: 10.1021/jm00098a017 |
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Discovery of a novel class of orally active, non-peptide angiotensin II antagonists B. De, M. Winn, T. M. Zydowsky, D. J. Kerkman, J. F. DeBernardis, J. Lee, S. Buckner, R. Warner, M. Brune, and et al. pp 3714 - 3717; DOI: 10.1021/jm00098a018 |
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(R)-2-(3-mercapto-2(S)-methyl-1-oxopropoxy)-3-(methylthio)propanoic acid (FPL 66564), the first ultra-short-acting angiotensin converting enzyme inhibitor Andrew J. G. Baxter, Richard D. Carr, Stephen C. Eyley, Lynne Fraser-Rae, Catherine Hallam, Steve T. Harper, Paul A. Hurved, Sarah J. King, and Premji Meghani pp 3718 - 3720; DOI: 10.1021/jm00098a019 |
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Book Reviews pp 3721 - 3724; DOI: 10.1021/jm00098a600 |
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A general method for the preparation of internally quenched fluorogenic protease substrates using solid-phase peptide synthesis Linda L. Maggiora, Clark W. Smith, and Zhong Yin Zhang pp 3727 - 3730; DOI: 10.1021/jm00099a001 |
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Inhibition of human leukocyte elastase. 4. Selection of a substituted cephalosporin (L-658,758) as a topical aerosol Paul E. Finke, Shrenik K. Shah, Bonnie M. Ashe, Richard G. Ball, Thomas J. Blacklock, Robert J. Bonney, Karen A. Brause, Gilbert O. Chandler, Meredith Cotton, and et al. pp 3731 - 3744; DOI: 10.1021/jm00099a002 |
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Orally active .beta.-lactam inhibitors of human leukocyte elastase-1. Activity of 3,3-diethyl-2-azetidinones Shrenik K. Shah, Conrad P. Dorn Jr., Paul E. Finke, Jeffrey J. Hale, William K. Hagmann, Karen A. Brause, Gilbert O. Chandler, Amy L. Kissinger, Bonnie M. Ashe, and et al. pp 3745 - 3754; DOI: 10.1021/jm00099a003 |
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Highly potent, orally active diester macrocyclic human renin inhibitors Ann E. Weber, Mark G. Steiner, Philip A. Krieter, Adria E. Colletti, James R. Tata, Thomas A. Halgren, Richard G. Ball, John J. Doyle, Terry W. Schorn, and et al. pp 3755 - 3773; DOI: 10.1021/jm00099a004 |
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Analogs of Ac-CCK-7 incorporating dipeptide mimics in place of Met28-Gly29 Jefferson W. Tilley, Waleed Danho, Shian Jan Shiuey, Irina Kulesha, Joseph Swistok, Raymond Makofske, Joseph Michalewsky, Joseph Triscari, David Nelson, and et al. pp 3774 - 3783; DOI: 10.1021/jm00099a005 |
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Synthesis and evaluation of 2-pyridinone derivatives as HIV-1 specific reverse transcriptase inhibitors. 1. Phthalimidoalkyl and -alkylamino analogs Jacob M. Hoffman, John S. Wai, Craig M. Thomas, Rhonda B. Levin, Julie A. O'Brien, and Mark E. Goldman pp 3784 - 3791; DOI: 10.1021/jm00099a006 |
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Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 2. Analogs of 3-aminopyridin-2(1H)-one Walfred S. Saari, John S. Wai, Thorsten E. Fisher, Craig M. Thomas, Jacob M. Hoffman, Clarence S. Rooney, Anthony M. Smith, James H. Jones, Dona L. Bamberger, and et al. pp 3792 - 3802; DOI: 10.1021/jm00099a007 |
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New hydroxyethylamine HIV protease inhibitors that suppress viral replication Daniel H. Rich, J. V. N. Vara Prasad, Chong Qing Sun, Jeremy Green, Richard Mueller, Kathryn Houseman, Debra MacKenzie, and Miroslav Malkovsky pp 3803 - 3812; DOI: 10.1021/jm00099a008 |
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3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 9. The synthesis and biological evaluation of novel simvastatin analogs George D. Hartman, Wasyl Halczenko, Mark E. Duggan, Jill S. Imagire, Robert L. Smith, Steven M. Pitzenberger, Susan L. Fitzpatrick, Alfred W. Alberts, Rick Bostedor, and et al. pp 3813 - 3821; DOI: 10.1021/jm00099a009 |
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4-Substituted thiophene- and furan-2-sulfonamides as topical carbonic anhydrase inhibitors George D. Hartman, Wasyl Halczenko, Robert L. Smith, Michael F. Sugrue, Pierre J. Mallorga, Stuart R. Michelson, William C. Randall, Harvey Schwam, and John M. Sondey pp 3822 - 3831; DOI: 10.1021/jm00099a010 |
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Development of a novel series of styrylquinoline compounds as high-affinity leukotriene D4 receptor antagonists: synthetic and structure-activity studies leading to the discovery of (.+-.)-3-[[[3-[2-(7-chloro-2-quinolinyl)-(E)-ethenyl]phenyl][[3-(dimethylamino)-3-oxopropyl]thio]methyl]thio]propionic acid R. Zamboni, M. Belley, E. Champion, L. Charette, R. DeHaven, R. Frenette, J. Y. Gauthier, T. R. Jones, S. Leger, and et al. pp 3832 - 3844; DOI: 10.1021/jm00099a011 |
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Synthesis and hypoglycemic activity of substituted 8-(1-piperazinyl)imidazo[1,2-a]pyrazines Laura C. Meurer, Richard L. Tolman, Edward W. Chapin, Richard Saperstein, Pasquale P. Vicario, Matthew M. Zrada, and Malcolm MacCoss pp 3845 - 3857; DOI: 10.1021/jm00099a012 |
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Imidazole-5-acrylic acids: potent nonpeptide angiotensin II receptor antagonists designed using a novel peptide pharmacophore model R. M. Keenan, J. Weinstock, J. A. Finkelstein, R. G. Franz, D. E. Gaitanopoulos, G. R. Girard, D. T. Hill, T. M. Morgan, J. M. Samanen, and et al. pp 3858 - 3872; DOI: 10.1021/jm00099a013 |
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Synthesis and biological activity of 13-epi-avermectins: potent anthelmintic agents with an increased margin of safety Timothy A. Blizzard, Gaye M. Margiatto, Helmut Mrozik, Wesley L. Shoop, Robert A. Frankshun, and Michael H. Fisher pp 3873 - 3878; DOI: 10.1021/jm00099a014 |
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Affinity probes for the avermectin binding proteins Peter T. Meinke, Susan P. Rohrer, Edward C. Hayes, James M. Schaeffer, Michael H. Fisher, and Helmut Mrozik pp 3879 - 3884; DOI: 10.1021/jm00099a015 |
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Differences in hydration and association of helical Boc-Val-Ala-Leu-Aib-Val-Ala-Leu-(Val-Ala-Leu-Aib)2-OMe.cntdot.xH2O in two crystalline polymorphs Isabella L. Karle, Judith L. Flippen-Anderson, Muppalla Sukumar, and Padmanabhan Balaram pp 3885 - 3889; DOI: 10.1021/jm00099a016 |
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Stabilization of the N-terminal residues of luteinizing hormone-releasing hormone agonists and the effect on pharmacokinetics Fortuna Haviv, Timothy D. Fitzpatrick, Charles J. Nichols, Rolf E. Swenson, Eugene N. Bush, Gilbert Diaz, A. Nguyen, Hugh N. Nellans, Daniel J. Hoffman, and et al. pp 3890 - 3894; DOI: 10.1021/jm00099a017 |
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Potent V2/V1a vasopressin antagonists with C-terminal ethylenediamine-linked retro-amino acids Maurice Manning, Jozef Przybylski, Zbigniew Grzonka, Eleonora Nawrocka, Bernard Lammek, Aleksandra Misicka, Ling Ling Cheng, W. Y. Chan, Nga Ching Wo, and Wilbur H. Sawyer pp 3895 - 3904; DOI: 10.1021/jm00099a018 |
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Development of a novel class of cyclic hexapeptide oxytocin antagonists based on a natural product Peter D. Williams, Mark G. Bock, Roger D. Tung, Victor M. Garsky, Debra S. Perlow, Jill M. Erb, G. F. Lundell, Norman P. Gould, Willie L. Whitter, and et al. pp 3905 - 3918; DOI: 10.1021/jm00099a019 |
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Orally active, nonpeptide oxytocin antagonists Ben E. Evans, James L. Leighton, Kenneth E. Rittle, Kevin F. Gilbert, George F. Lundell, Norman P. Gould, Doug W. Hobbs, Robert M. DiPardo, Daniel F. Veber, Douglas J. Pettibone, Bradley V. Clineschmidt, Paul S. Anderson, and Roger M. Freidinger pp 3919 - 3927; DOI: 10.1021/jm00099a020 |
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Growth hormone-releasing factor analogs with hydrophobic residues at position 19. Effects on growth hormone releasing activity in vitro and in vivo, stability in blood plasma in vitro, and secondary structure Alan R. Friedman, Avneet K. Ichhpurani, William M. Moseley, Glenn R. Alaniz, William H. Claflin, Diane L. Cleary, Mark D. Prairie, William C. Krueger, Lawrence A. Frohman, and et al. pp 3928 - 3933; DOI: 10.1021/jm00099a021 |
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Enzymic semisynthesis of a superpotent analog of human growth hormone-releasing factor Jacob Bongers, Theodore Lambros, Wen Liu, Mushtaq Ahmad, Robert M. Campbell, Arthur M. Felix, and Edgar P. Heimer pp 3934 - 3941; DOI: 10.1021/jm00099a022 |
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Potent gonadotropin releasing hormone antagonists with low histamine-releasing activity John J. Nestor, Ram Tahilramani, Teresa L. Ho, Jessie C. Goodpasture, Brian H. Vickery, and Pierre Ferrandon pp 3942 - 3948; DOI: 10.1021/jm00099a023 |
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A new class of high affinity ligands for the neurokinin A NK2 receptor: .psi.(CH2NR) reduced peptide bond analogs of neurokinin A4-10 Scott L. Harbeson, Scott A. Shatzer, Tieu Binh Le, and Stephen H. Buck pp 3949 - 3955; DOI: 10.1021/jm00099a024 |
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Conformationally restricted deltorphin analogs Peter W. Schiller, Grazyna Weltrowska, Thi M. D. Nguyen, Brian C. Wilkes, Nga N. Chung, and Carole Lemieux pp 3956 - 3961; DOI: 10.1021/jm00099a025 |
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Investigation of conformational specificity at GPIIb/IIIa: evaluation of conformationally constrained RGD peptides Catherine E. Peishoff, Fadia E. Ali, John W. Bean, Raul Calvo, Cynthia A. D'Ambrosio, Drake S. Eggleston, Tammy Page Kline, Paul F. Koster, S. M. Hwang, and et al. pp 3962 - 3969; DOI: 10.1021/jm00099a026 |
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Design and synthesis of a C7 mimetic for the predicted .gamma.-turn conformation found in several constrained RGD antagonists James F. Callahan, John W. Bean, Joelle L. Burgess, Drake S. Eggleston, Shing Mei Hwang, Kenneth D. Kopple, Paul F. Koster, Andrew Nichols, Catherine E. Peishoff, and et al. pp 3970 - 3972; DOI: 10.1021/jm00099a027 |
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4-Oxospiro[benzopyran-2,4'-piperidines] as class III antiarrhythmic agents. Pharmacological studies on 3,4-dihydro-1'-[2-(benzofurazan-5-yl)ethyl]-6-methanesulfonamidospiro[(2H)-1-benzopyran-2,4'-piperidin]-4-one (L-691,121) Jason M. Elliott, Harold G. Selnick, David A. Claremon, John J. Baldwin, Susan A. Buhrow, John W. Butcher, Charles N. Habecker, Stella W. King, Joseph J. Lynch Jr., and et al. pp 3973 - 3976; DOI: 10.1021/jm00099a028 |
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Editorial - A Tribute to Ralph F. Hirschmann Daniel H. Rich pp 3725 - 3726; DOI: 10.1021/jm00099a600 |
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N-substituted pyrazino[2,3-c][1,2,6]thiadiazine 2,2-dioxides. A new class of diuretics Pilar Goya, Juan A. Paez, Ibon Alkorta, Emilio Carrasco, Manuel Grau, Francisca Anton, Sebastian Julia, and Martin Martinez-Ripoll pp 3977 - 3983; DOI: 10.1021/jm00100a001 |
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6-Hydroxy-3-propyl-2,3,4,5-tetrahydro-1H-3-benzazepine and analogs: new centrally acting 5-HT1a receptor agonists Haakan Wikstroem, Bengt Andersson, Thomas Elebring, Soeren Lagerkvist, Gerd Hallnemo, Ingrid Pettersson, Per Aake Jovall, Kjell Svensson, Agneta Ekman, and Arvid Carlsson pp 3984 - 3990; DOI: 10.1021/jm00100a002 |
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Synthesis and biological evaluation of 5'-sulfamoylated purinyl carbocyclic nucleosides Eileen M. Peterson, Jay Brownell, and Robert Vince pp 3991 - 4000; DOI: 10.1021/jm00100a003 |
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Predictive binding of .beta.-carboline inverse agonists and antagonists via the CoMFA/GOLPE approach Michael S. Allen, Anthony J. LaLoggia, Linda J. Dorn, Michael J. Martin, Gabriele Costantino, Timothy J. Hagen, Konrad F. Koehler, Phil Skolnick, and James M. Cook pp 4001 - 4010; DOI: 10.1021/jm00100a004 |
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Novel functional M1 selective muscarinic agonists. 2. Synthesis and structure-activity relationships of 3-pyrazinyl-1,2,5,6-tetrahydro-1-methylpyridines. Construction of a molecular model for the M1 pharmacophore John S. Ward, Leander Merritt, V. J. Klimkowski, M. L. Lamb, C. H. Mitch, F. P. Bymaster, B. Sawyer, H. E. Shannon, Preben H. Olesen, and et al. pp 4011 - 4019; DOI: 10.1021/jm00100a005 |
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Synthesis and dopaminergic activity of some 3-(1,2,3,6-tetrahydro-1-pyridylalkyl)indoles. A novel conformational model to explain structure-activity relationships Henning Boettcher, Gerhard Barnickel, Hans Heinrich Hausberg, Anton F. Haase, Christoph A. Seyfried, and Volker Eiermann pp 4020 - 4026; DOI: 10.1021/jm00100a006 |
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New nonpeptide angiotensin II receptor antagonists. 2. Synthesis, biological properties, and structure-activity relationships of 2-alkyl-4-(biphenylylmethoxy)quinoline derivatives Robert H. Bradbury, Christopher P. Allott, Michael Dennis, Eric Fisher, John S. Major, Brian B. Masek, Alec A. Oldham, Robert J. Pearce, Neil Rankine, and et al. pp 4027 - 4038; DOI: 10.1021/jm00100a007 |
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Effects of alkyl substitutions of xanthine skeleton on bronchodilation Ryosuke Sakai, Kayo Konno, Yasunori Yamamoto, Fujiko Sanae, Kenzo Takagi, Takaaki Hasegawa, Nobuhiko Iwasaki, Masato Kakiuchi, Hideo Kato, and Kenichi Miyamoto pp 4039 - 4044; DOI: 10.1021/jm00100a008 |
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New bronchodilators. 1. 1,5-Substituted 1H-imidazo[4,5-c]quinolin-4(5H)-ones Fumio Suzuki, Takeshi Kuroda, Yoshisuke Nakasato, Haruhiko Manabe, Kenji Ohmori, Shigeto Kitamura, Shunji Ichikawa, and Tetsuji Ohno pp 4045 - 4053; DOI: 10.1021/jm00100a009 |
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Synthesis and antibacterial activity of a series of basic amides of teicoplanin and deglucoteicoplanin with polyamines Adriano Malabarba, Romeo Ciabatti, Jurgen Kettenring, Roberto Scotti, Gianpaolo Candiani, Rosa Pallanza, Marisa Berti, and Beth P. Goldstein pp 4054 - 4060; DOI: 10.1021/jm00100a010 |
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Synthesis, chemical, and biological properties of vinylogous hydroxamic acids: dual inhibitors of 5-lipoxygenase and IL-1 biosynthesis Stephen W. Wright, Richard R. Harris, Janet S. Kerr, Alicia M. Green, Donald J. Pinto, Elaine M. Bruin, Robert J. Collins, Roberta L. Dorow, Lisa R. Mantegna, and et al. pp 4061 - 4068; DOI: 10.1021/jm00100a011 |
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Copyrine alkaloids: synthesis, spectroscopic characterization, and antimycotic/antimycobacterial activity of A- and B-ring-functionalized sampangines John R. Peterson, Jordan K. Zjawiony, Shihchih Liu, Charles D. Hufford, Alice M. Clark, and Robin D. Rogers pp 4069 - 4077; DOI: 10.1021/jm00100a012 |
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Inhibition of hog liver folylpolyglutamate synthetase by 5-substituted 5,8-dideaza analogs of folic acid bearing a terminal L-ornithine residue John B. Hynes, Shyam K. Singh, Oliver Fetzer, and Barry Shane pp 4078 - 4085; DOI: 10.1021/jm00100a013 |
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.delta. Opioid antagonist activity and binding studies of regioisomeric isothiocyanate derivatives of naltrindole: evidence for .delta. receptor subtypes P. S. Portoghese, M. Sultana, W. L. Nelson, P. Klein, and A. E. Takemori pp 4086 - 4091; DOI: 10.1021/jm00100a014 |
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Condensation of muscimol or thiomuscimol with aminopyridazines yields GABA-A antagonists Anita Melikian, Gilbert Schlewer, Jean Pierre Chambon, and Camille Georges Wermuth pp 4092 - 4097; DOI: 10.1021/jm00100a015 |
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(R)-(-)- and (S)-(+)-Adenallene: synthesis, absolute configuration, enantioselectivity of antiretroviral effect, and enzymic deamination. Sreenivasulu Megati, Zafrir Goren, James V. Silverton, Joel Orlina, Hisao Nishimura, Takuma Shirasaki, Hiroaki Mitsuya, and Jiri Zemlicka pp 4098 - 4104; DOI: 10.1021/jm00100a016 |
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Molecular yardsticks. Rigid probes to define the spatial dimensions of the benzodiazepine receptor binding site Michael J. Martin, Mark L. Trudell, Hernando Diaz Arauzo, Michael S. Allen, Anthony J. LaLoggia, Li Deng, Christopher A. Schultz, Yun Chou Tan, Yingzhi Bi, and et al. pp 4105 - 4117; DOI: 10.1021/jm00100a017 |
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(Pyridylcyanomethyl)piperazines as orally active PAF antagonists Elena Carceller, Carmen Almansa, Manuel Merlos, Marta Giral, Javier Bartroli, Julian Garcia-Rafanell, and Javier Forn pp 4118 - 4134; DOI: 10.1021/jm00100a018 |
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Synthesis and evaluation of 3-substituted 17-methylmorphinan analogs as potential anticonvulsant agents Amy Hauck Newman, Kathryn Bevan, Norman Bowery, and Frank C. Tortella pp 4135 - 4142; DOI: 10.1021/jm00100a019 |
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Synthesis and biological activity of N6-(p-sulfophenyl)alkyl and N6-sulfoalkyl derivatives of adenosine: water-soluble and peripherally selective adenosine agonists. Kenneth A. Jacobson, Olga Nikodijevic, Xiao Duo Ji, Deborah A. Berkich, David Eveleth, Reginald L. Dean, Kenichiro Hiramatsu, Neal F. Kassell, Philip J. M. Van Galen, and et al. pp 4143 - 4149; DOI: 10.1021/jm00100a020 |
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Guanidinophenyl-substituted enol lactones as selective, mechanism-based inhibitors of trypsin-like serine proteases Roopa Rai and John A. Katzenellenbogen pp 4150 - 4159; DOI: 10.1021/jm00100a021 |
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Structural modifications of camptothecin and effects on topoisomerase I inhibition Robert T. Crow and Donald M. Crothers pp 4160 - 4164; DOI: 10.1021/jm00100a022 |
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Synthesis of novel MPTP analogs as potential monoamine oxidase B (MAO-B) inhibitors Amit S. Kalgutkar and Neal Castagnoli pp 4165 - 4174; DOI: 10.1021/jm00100a023 |
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The first mechanism-based inactivators for angiotensin-converting enzyme Soumitra S. Ghosh, Odile Said-Nejad, Juliatiek Roestamadji, and Shahriar Mobashery pp 4175 - 4179; DOI: 10.1021/jm00100a024 |
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Adenosine deaminase inhibitors. Synthesis and biological evaluation of C1' and nor-C1' derivatives of (+)-erythro-9-[2(S)-hydroxy-3(R)-nonyl]adenine Geraldine C. B. Harriman, Anne F. Poirot, Elie Abushanab, Rose Marie Midgett, and Johanna D. Stoeckler pp 4180 - 4184; DOI: 10.1021/jm00100a025 |
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Synthesis and conformational properties of the lanthionine-bridged opioid peptide [D-AlaL2,AlaL5]enkephalin as determined by NMR and computer simulations Alexander Polinsky, Michael G. Cooney, Anna Toy-Palmer, George Osapay, and Murray Goodman pp 4185 - 4194; DOI: 10.1021/jm00100a026 |
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Conformationally constrained tachykinin analogs: potent and highly selective neurokinin NK-2 receptor agonists Martyn J. Deal, Russell M. Hagan, Simon J. Ireland, Christopher C. Jordan, Andrew B. McElroy, Barry Porter, Barry C. Ross, Michaela Stephens-Smith, and Peter Ward pp 4195 - 4204; DOI: 10.1021/jm00100a027 |
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Fluoronaphthyridines and -quinolones as antibacterial agents. 5. Synthesis and antimicrobial activity of chiral 1-tert-butyl-6-fluoro-7-substituted-naphthyridones P. Di Cesare, D. Bouzard, M. Essiz, J. P. Jacquet, B. Ledoussal, J. R. Kiechel, P. Remuzon, R. E. Kessler, J. Fung-Tomc, and J. Desiderio pp 4205 - 4213; DOI: 10.1021/jm00100a028 |
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L-Thymidine is phosphorylated by herpes simplex virus type 1 thymidine kinase and inhibits viral growth Silvio Spadari, Giovanni Maga, Federico Focher, Giovanni Ciarrocchi, Roberto Manservigi, Federico Arcamone, Massimo Capobianco, Antonio Carcuro, Francesco Colonna, and et al. pp 4214 - 4220; DOI: 10.1021/jm00100a029 |
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Isobenzofurans as conformationally constrained miconazole analogs with improved antifungal potency Raymond G. Lovey, Arthur J. Elliott, James J. Kaminski, David Loebenberg, Raulo M. Parmegiani, D. F. Rane, Viyyoor M. Girijavallabhan, Russel E. Pike, Henry Guzik, and et al. pp 4221 - 4229; DOI: 10.1021/jm00100a030 |
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Synthesis of biologically active taxol analogs with modified phenylisoserine side chains Gunda I. Georg, Zacharia S. Cheruvallath, Richard H. Himes, Magdalena R. Mejillano, and Charles T. Burke pp 4230 - 4237; DOI: 10.1021/jm00100a031 |
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Structure-activity studies on benzhydrol-containing nipecotic acid and guvacine derivatives as potent, orally-active inhibitors of GABA uptake Michael R. Pavia, Sandra J. Lobbestael, David Nugiel, Daniel R. Mayhugh, Vlad E. Gregor, Charles P. Taylor, Roy D. Schwarz, Laura Brahce, and Mark G. Vartanian pp 4238 - 4248; DOI: 10.1021/jm00100a032 |
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Analogs of CCK incorporating conformationally constrained replacements for Asp32 Jefferson W. Tilley, Waleed Danho, Vincent Madison, David Fry, Joseph Swistok, Raymond Makofske, Joseph Michalewsky, Allan Schwartz, Sally Weatherford, and et al. pp 4249 - 4252; DOI: 10.1021/jm00100a033 |
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4-[2-[Methyl(2-phenethyl)amino]-2-oxoethyl]-8-(phenylmethoxy)-2-naphthalenecarboxylic acid: a high affinity, competitive, orally active leukotriene B4 receptor antagonist Fu Chih Huang, Wan Kit Chan, James D. Warus, Mathew M. Morrissette, Kevin J. Moriarty, Michael N. Chang, Jeffrey J. Travis, Laurie S. Mitchell, George W. Nuss, and Charles A. Sutherland pp 4253 - 4255; DOI: 10.1021/jm00100a034 |
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Book Reviews pp 4256 - 4258; DOI: 10.1021/jm00100a600 |
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Novel non-crossresistant diaminoanthraquinones as potential chemotherapeutic agents Jack B. Jiang, Mary George Johnson, Jean M. Defauw, Tracey M. Beine, Lawrence M. Ballas, William P. Janzen, Carson R. Loomis, Jan Seldin, Divann Cofield, and et al. pp 4259 - 4263; DOI: 10.1021/jm00101a001 |
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Synthesis and evaluation of novel spermidine derivatives as targeted cancer chemotherapeutic agents Peter A. Stark, Brian D. Thrall, Gary G. Meadows, and Mahmoud M. Abdel-Monem pp 4264 - 4269; DOI: 10.1021/jm00101a002 |
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Gonadotropin-releasing hormone antagonists with N.omega.-triazolylornithine, -lysine, or -p-aminophenylalanine residues at positions 5 and 6 Jean Rivier, John Porter, Carl Hoeger, Paula Theobald, A. Grey Craig, John Dykert, Anne Corrigan, Marilyn Perrin, William A. Hook, and et al. pp 4270 - 4278; DOI: 10.1021/jm00101a003 |
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Cysteine protease inhibition by azapeptide esters Joe Magrath and Robert H. Abeles pp 4279 - 4283; DOI: 10.1021/jm00101a004 |
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Design and synthesis of novel FKBP inhibitors James R. Hauske, Peter Dorff, Susan Julin, Joseph DiBrino, Robin Spencer, and Rebecca Williams pp 4284 - 4296; DOI: 10.1021/jm00101a005 |
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Effect of conformational mobility and hydrogen-bonding interactions on the selectivity of some guanidinoaryl-substituted mechanism-based inhibitors of trypsin-like serine proteases Roopa Rai and John A. Katzenellenbogen pp 4297 - 4305; DOI: 10.1021/jm00101a006 |
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.omega.-[(4-Phenyl-2-quinolyl)oxy]alkanoic acid derivatives: a new family of potent LTB4 antagonists Richard Labaudiniere, Wolfram Hendel, Bernard Terlain, Francoise Cavy, Olivier Marquis, and Norbert Dereu pp 4306 - 4314; DOI: 10.1021/jm00101a007 |
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.omega.-[(4,6-Diphenyl-2-pyridyl)oxy]alkanoic acid derivatives: a new family of potent and orally active LTB4 antagonists Richard Labaudiniere, Norbert Dereu, Francoise Cavy, Marie Christine Guillet, Olivier Marquis, and Bernard Terlain pp 4315 - 4324; DOI: 10.1021/jm00101a008 |
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Opioid agonist and antagonist activities of morphindoles related to naltrindole P. S. Portoghese, D. L. Larson, M. Sultana, and A. E. Takemori pp 4325 - 4329; DOI: 10.1021/jm00101a009 |
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Effect of modification of the basic residues of dynorphin A-(1-13) amide on opioid receptor selectivity and opioid activity Kristin R. Snyder, Sandra C. Story, Mia E. Heidt, Thomas F. Murray, Gary E. DeLander, and Jane V. Aldrich pp 4330 - 4333; DOI: 10.1021/jm00101a010 |
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Synthesis and biological evaluation of conformationally restricted 2-(1-pyrrolidinyl)-N-[2-(3,4-dichlorophenyl)ethyl]-N-methylethylenediamines as .sigma. receptor ligands. 1. Pyrrolidine, piperidine, homopiperidine, and tetrahydroisoquinoline classes Brian R. De Costa, Celia Dominguez, Xiao Shu He, Wanda Williams, Lilian Radesca, and Wayne Bowen pp 4334 - 4343; DOI: 10.1021/jm00101a011 |
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Novel piperidine .sigma. receptor ligands as potential antipsychotic drugs Paul J. Gilligan, Gary A. Cain, Thomas E. Christos, Leonard Cook, Spencer Drummond, Alexander L. Johnson, Ahmed A. Kergaye, John F. McElroy, Kenneth W. Rohrbach, and et al. pp 4344 - 4361; DOI: 10.1021/jm00101a012 |
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Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 2. Synthesis and biological activity of 8-(benzenesulfonamido)-7-(3-pyridinyl)octanoic acid and related compounds Alan J. Main, Robert Goldstein, David Cohen, Patricia Furness, and Warren Lee pp 4362 - 4365; DOI: 10.1021/jm00101a013 |
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Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 3. Pyridinylalkyl-substituted 8-[(arylsulfonyl)amino]octanoic acids Alan J. Main, Shripad S. Bhagwat, Clay Boswell, Robert Goldstein, Candido Gude, David Cohen, Patricia Furness, Warren Lee, and Marissa Louzan pp 4366 - 4372; DOI: 10.1021/jm00101a014 |
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Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 4. 8-[[(4-Chlorophenyl)sulfonyl]amino]-4-[3-(3-pyridinyl)propyl]octanoic acid and analogs Shripad S. Bhagwat, Candido Gude, Clay Boswell, Nicolina Contardo, David S. Cohen, Ronald Dotson, Janice Mathis, Warren Lee, Patricia Furness, and Harry Zoganas pp 4373 - 4383; DOI: 10.1021/jm00101a015 |
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Acyl-CoA: cholesterol O-acyl transferase (ACAT) inhibitors. 1. 2-(Alkylthio)-4,5-diphenyl-1H-imidazoles as potent inhibitors of ACAT Neil V. Harris, Andrew W. Bridge, Raymond C. Bush, Edward C. J. Coffee, Donald I. Dron, Mark F. Harper, Michael J. Ashton, David J. Lythgoe, Christopher Smith, and et al. pp 4384 - 4392; DOI: 10.1021/jm00101a016 |
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Low molecular weight, non-peptide fibrinogen receptor antagonists Leo Alig, Albrecht Edenhofer, Paul Hadvary, Marianne Huerzeler, Dietmar Knopp, Marcel Mueller, Beat Steiner, Arnold Trzeciak, and Thomas Weller pp 4393 - 4407; DOI: 10.1021/jm00101a017 |
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Synthesis and pharmacological characterization of 2-(4-chloro-3-hydroxyphenyl)ethylamine and N,N-dialkyl derivatives as dopamine receptor ligands Francesco Claudi, Gianfabio Giorgioni, Antonio Di Stefano, Maria Pia Abbracchio, Anna Maria Paoletti, and Walter Balduini pp 4408 - 4414; DOI: 10.1021/jm00101a018 |
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Synthesis and antimuscarinic properties of some N-substituted 5-(aminomethyl)-3,3-diphenyl-2(3H)-furanones Carl Kaiser, Ciro J. Spagnuolo, Theodore C. Adams, Vicki H. Audia, Andrea C. Dupont, Holia Hatoum, Valerie C. Lowe, Judith C. Prosser, Bonnie L. Sturm, and Lalita Noronha-Blob pp 4415 - 4424; DOI: 10.1021/jm00101a019 |
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Thiophene systems. 14. Synthesis and antihypertensive activity of novel 7-(cyclic amido)-6-hydroxythieno[3,2-b]pyrans and related compounds as new potassium channel activators Pauline J. Sanfilippo, James J. McNally, Jeffery B. Press, Louis J. Fitzpatrick, Maud J. Urbanski, Laurence B. Katz, Edward Giardino, Robert Falotico, Joseph Salata, and et al. pp 4425 - 4433; DOI: 10.1021/jm00101a020 |
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Synthesis, absolute configuration, stereoselectivity, and receptor selectivity of (.alpha.R,.beta.S)-.alpha.,.beta.-dimethylhistamine. A novel highly potent histamine H3 receptor agonist Ralph Lipp, Jean Michel Arrang, Monique Garbarg, Peter Luger, Jean Charles Schwartz, and Walter Schunack pp 4434 - 4441; DOI: 10.1021/jm00101a021 |
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Synthesis and biological activity of 4-(diphenylmethyl)-.alpha.-[(4-quinolinyloxy)methyl]-1-piperazineethanol and related compounds Ila Sircar, Steve J. Haleen, Sandra E. Burke, and Hubert Barth pp 4442 - 4449; DOI: 10.1021/jm00101a022 |
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A dideazatetrahydrofolate analog lacking a chiral center at C-6: N-[4-[2-(2-amino-3,4-dihydro-4-oxo-7H-pyrrolo[2,3-d]pyrimidin-5yl)ethyl[benzoyl]-L-glutamic acid is an inhibitor of thymidylate synthase Edward C. Taylor, Dietmar Kuhnt, Chuan Shih, Sharon M. Rinzel, Gerald B. Grindey, Julio Barredo, Mehrdad Jannatipour, and Richard G. Moran pp 4450 - 4454; DOI: 10.1021/jm00101a023 |
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Cardiotonic agents. Synthesis and cardiovascular properties of novel 2-arylbenzimidazoles and azabenzimidazoles Timur Gungor, Andre Fouquet, Jean Marie Teulon, Daniel Provost, Michele Cazes, and Alix Cloarec pp 4455 - 4463; DOI: 10.1021/jm00101a024 |
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2-(Aminomethyl)chromans that inhibit iron-dependent lipid peroxidation and protect against central nervous system trauma and ischemia E. Jon Jacobsen, Fred J. VanDoornik, Donald E. Ayer, Kenneth L. Belonga, J. Mark Braughler, Edward D. Hall, and David J. Houser pp 4464 - 4472; DOI: 10.1021/jm00101a025 |
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Design, synthesis, and biological evaluation of novel 4-substituted 1-methyl-1,2,3,6-tetrahydropyridine analogs of MPTP Zhiyang Zhao, Deepak Dalvie, Noreen Naiman, Kay Castagnoli, and Neal Castagnoli pp 4473 - 4478; DOI: 10.1021/jm00101a026 |
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Diamine ligand release from the cisplatin analog [meso-1,2-bis(2,6-dichloro-4-hydroxyphenyl)ethylenediamine]dichloroplatinum(II) in cell culture medium Patrick J. Bednarski, Barbara Truembach, Nicole A. Kratochwil, and Helmut Schoenenberger pp 4479 - 4485; DOI: 10.1021/jm00101a027 |
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Structural features of substituted purine derivatives compatible with depletion of human O6-alkylguanine-DNA alkyltransferase Robert C. Moschel, Mark G. McDougall, M. Eileen Dolan, Linda Stine, and Anthony E. Pegg pp 4486 - 4491; DOI: 10.1021/jm00101a028 |
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Iodinated tomoxetine derivatives as selective ligands for serotonin and norepinephrine uptake sites Sumalee Chumpradit, Mei Ping Kung, Chitchanum Panyachotipun, Vichukorn Prapansiri, Catherine Foulon, Brian P. Brooks, Stephen A. Szabo, Shanaz Tejani-Butt, Alan Frazer, and Hank F. Kung pp 4492 - 4497; DOI: 10.1021/jm00101a029 |
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Incorporation of a novel conformationally restricted tyrosine analog into a cyclic, .delta. opioid receptor selective tetrapeptide (JOM-13) enhances .delta. receptor binding affinity and selectivity Henry I. Mosberg and Heather B. Kroona pp 4498 - 4500; DOI: 10.1021/jm00101a030 |
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Carbohydrate materials bearing neuraminidase-resistant C-glycosides of sialic acid strongly inhibit the in vitro infectivity of influenza virus Jon O. Nagy, Peng Wang, James H. Gilbert, Mary E. Schaefer, Tara G. Hill, Matthew R. Callstrom, and Mark D. Bednarski pp 4501 - 4502; DOI: 10.1021/jm00101a031 |
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Synthesis and serotonergic pharmacology of the enantiomers of 3-[(N-methylpyrrolidin-2-yl)methyl]-5-methoxy-1H-indole: discovery of stereogenic differentiation in the aminoethyl side chain of the neurotransmitter serotonin John E. Macor, James Blake, Carol B. Fox, Celeste Johnson, B. Kenneth Koe, Lorraine A. Lebel, Jean M. Morrone, Kevin Ryan, Anne W. Schmidt, and et al. pp 4503 - 4505; DOI: 10.1021/jm00101a032 |
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Book Reviews pp 4506 - 4508; DOI: 10.1021/jm00101a600 |
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Synthesis and structure-activity relationship of 6-substituted purine derivatives as novel selective positive inotropes Jeffery B. Press, Robert Falotico, Zoltan G. Hajos, Rebecca Anne Sawyers, Ramesh M. Kanojia, Louella Williams, Barbara Haertlein, Jack A. Kauffman, Constance Lakas-Weiss, and Joseph J. Salata pp 4509 - 4515; DOI: 10.1021/jm00102a001 |
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Synthesis and biological characterization of .alpha.-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogs as potential atypical antipsychotic agents Joseph P. Yevich, James S. New, Walter G. Lobeck, Pierre Dextraze, Edith Bernstein, Duncan P. Taylor, Frank D. Yocca, Michael S. Eison, and Davis L. Temple pp 4516 - 4525; DOI: 10.1021/jm00102a002 |
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Anticancer activity in murine and human tumor cell lines of bis(platinum) complexes incorporating straight-chain aliphatic diamine linker groups Alan J. Kraker, James D. Hoeschele, William L. Elliott, H. D. Hollis Showalter, Anthony D. Sercel, and Nicholas P. Farrell pp 4526 - 4532; DOI: 10.1021/jm00102a003 |
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Pyrrolobenzodiazepines and related systems. 2. Synthesis and biological properties of isonoraptazepine derivatives Silvio Massa, Marino Artico, Antonello Mai, Federico Corelli, Maurizio Botta, Andrea Tafi, Gian Carlo Pantaleoni, Raffaele Giorgi, Maria Francesca Coppolino, and et al. pp 4533 - 4541; DOI: 10.1021/jm00102a004 |
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Synthesis and structure-activity relationships of acetylcholinesterase inhibitors: 1-benzyl-4-(2-phthalimidoethyl)piperidine, and related derivatives Hachiro Sugimoto, Yutaka Tsuchiya, Hiroyuki Sugumi, Kunizo Higurashi, Norio Karibe, Yoichi Iimura, Atsushi Sasaki, Shin Araki, Yoshiharu Yamanishi, and Kiyomi Yamatsu pp 4542 - 4548; DOI: 10.1021/jm00102a005 |
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Synthesis and enzymic activity of some new purine ring system analogs of adenosine 3'5'-cyclic monophosphate Gyula Sagi, Kornelia Szucs, Gyorgy Vereb, and Laszlo Otvos pp 4549 - 4556; DOI: 10.1021/jm00102a006 |
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2-(N'-alkylidenehydrazino)adenosines: potent and selective coronary vasodilators Kazunori Niiya, Ray A. Olsson, Robert D. Thompson, Scott K. Silvia, and Masayuki Ueeda pp 4557 - 4561; DOI: 10.1021/jm00102a007 |
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2-(N'-aralkylidenehydrazino)adenosines: potent and selective coronary vasodilators. Kazunori Niiya, Robert D. Thompson, Scott K. Silvia, and Ray A. Olsson pp 4562 - 4566; DOI: 10.1021/jm00102a008 |
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3'-C-Branched 2'-deoxy-5-methyluridines: synthesis, enzyme inhibition, and antiviral properties I. I. Fedorov, E. M. Kaz'mina, N. A. Novicov, G. V. Gurskaya, A. V. Bochkarev, M. V. Yas'ko, L. S. Viktorova, M. K. Kukhanova, Jan Balzarini, and et al. pp 4567 - 4575; DOI: 10.1021/jm00102a009 |
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Synthesis and antiviral activity of some new S-adenosyl-L-homocysteine derivatives Pawel Serafinowski, Erwin Dorland, Kenneth R. Harrap, Jan Balzarini, and Erik De Clercq pp 4576 - 4583; DOI: 10.1021/jm00102a010 |
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Dihydroxynitrobenzaldehydes and hydroxymethoxynitrobenzaldehydes: synthesis and biological activity as catechol-O-methyltransferase inhibitors Rosa A. Perez, Eldiberto Fernandez-Alvarez, Ofelia Nieto, and F. Javier Piedrafita pp 4584 - 4588; DOI: 10.1021/jm00102a011 |
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O3-(2-Carbomethoxyallyl) ethers of opioid ligands derived from oxymorphone, naltrexone, etorphine, diprenorphine, norbinaltorphimine, and naltrindole. Unexpected O3-dealkylation in the opioid radioligand displacement assay Peter Klein and Wendel L. Nelson pp 4589 - 4594; DOI: 10.1021/jm00102a012 |
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Structure-activity relationships of imidazo[4,5-f]quinoline partial structures and analogs. Discovery of pyrazolo[3,4-f]quinoline derivatives as potent immunostimulants Mikel P. Moyer, Frederick H. Weber, and Jonathan L. Gross pp 4595 - 4601; DOI: 10.1021/jm00102a013 |
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Quisqualic acid analogs: synthesis of .beta.-heterocyclic 2-aminopropanoic acid derivatives and their activity at a novel quisqualate-sensitized site Nalin Subasinghe, Marvin Schulte, Robert J. Roon, James F. Koerner, and Rodney L. Johnson pp 4602 - 4607; DOI: 10.1021/jm00102a014 |
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DL-Tetrazol-5-ylglycine, a highly potent NMDA agonist: its synthesis and NMDA receptor efficacy W. H. W. Lunn, Darryle D. Schoepp, David O. Calligaro, R. T. Vasileff, L. J. Heinz, Craig R. Salhoff, and Patrick J. O'Malley pp 4608 - 4612; DOI: 10.1021/jm00102a015 |
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Novel spirosuccinimides with incorporated isoindolone and benzisothiazole 1,1-dioxide moieties as aldose reductase inhibitors and antihyperglycemic agents Jay Wrobel, Arlene Dietrich, Shiela A. Woolson, Jane Millen, Michael McCaleb, Maria C. Harrison, Thomas C. Hohman, Janet Sredy, and Donald Sullivan pp 4613 - 4627; DOI: 10.1021/jm00102a016 |
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Antirhinoviral activity of heterocyclic analogs of Win 54954 Thomas R. Bailey, Guy D. Diana, Paul J. Kowalczyk, Vahan Akullian, Michael A. Eissenstat, David Cutcliffe, John P. Mallamo, Philip M. Carabateas, and Daniel C. Pevear pp 4628 - 4633; DOI: 10.1021/jm00102a017 |
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Potential antitumor agents. 21. Structure determination and antitumor activity of imidazo[2,1-b]thiazole guanylhydrazones Aldo Andreani, Mirella Rambaldi, Alessandra Locatelli, Rosaria Bossa, Alessandra Fraccari, and Iraklis Galatulas pp 4634 - 4637; DOI: 10.1021/jm00102a018 |
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N-Terminal alkylated derivatives of [D-Pro10]dynorphin A-(1-11) are highly selective for .kappa.-opioid receptors Heekyung Choi, Thomas F. Murray, Gary E. DeLander, Valerie Caldwell, and Jane V. Aldrich pp 4638 - 4639; DOI: 10.1021/jm00102a019 |
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Non-peptide fibrinogen receptor antagonists. 1. Discovery and design of exosite inhibitors George D. Hartman, Melissa S. Egbertson, Wasyl Halczenko, William L. Laswell, Mark E. Duggan, Robert L. Smith, Adel M. Naylor, Patricia D. Manno, Robert J. Lynch, and et al. pp 4640 - 4642; DOI: 10.1021/jm00102a020 |
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Book Reviews pp 4643 - 4650; DOI: 10.1021/jm00102a600 |
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Para-substituted Phe3 deltorphin analogs: enhanced selectivity of halogenated derivatives for .sigma. opioid receptor sites Severo Salvadori, Clementina Bianchi, Lawrence H. Lazarus, Valeria Scaranari, Martti Attila, and Roberto Tomatis pp 4651 - 4657; DOI: 10.1021/jm00103a001 |
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NMR studies on YSPTSPSY: implications for the design of DNA bisintercalators Margaret M. Harding pp 4658 - 4664; DOI: 10.1021/jm00103a002 |
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A novel orally active inhibitor of IL-1 generation: synthesis and structure-activity relationships of 3-(4-hydroxy-1-naphthalenyl)-2-propenoic acid derivatives Masayuki Tanaka, Kenichi Chiba, Makoto Okita, Toshihiko Kaneko, Katsuya Tagami, Shigeki Hibi, Yasushi Okamoto, Hiroshi Shirota, Masaki Goto, and et al. pp 4665 - 4675; DOI: 10.1021/jm00103a003 |
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Computer-aided mapping of the .beta.-adrenoceptor I: Explanation for effect of para substitution on blocking activity at the .beta.-1-adrenoceptor Jonathan B. Ball, Tracy L. Nero, Dimitri Iakovidis, Lun Tung, Graham Jackman, and William J. Louis pp 4676 - 4682; DOI: 10.1021/jm00103a004 |
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Radiosynthesis, cerebral distribution, and binding of [125I]-1-(p-iodophenyl)-3-(1-adamantyl)guanidine, a ligand for .sigma. binding sites Alane S. Kimes, Alan A. Wilson, Ursula Scheffel, Bruce G. Campbell, and Edythe D. London pp 4683 - 4689; DOI: 10.1021/jm00103a005 |
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Conformationally restricted analogs of disoxaril: a comparison of the activity against human rhinovirus type 14 and 1A John P. Mallamo, Guy D. Diana, Daniel C. Pevear, Frank J. Dutko, Michael S. Chapman, Kyung H. Kim, Iwona Minor, Marcos Oliveira, and Michael G. Rossmann pp 4690 - 4695; DOI: 10.1021/jm00103a006 |
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Synthesis and biological evaluation of novel potent antagonists of the bombesin/gastrin releasing peptide receptor Michael Mokotoff, Kaijun Ren, Lan K. Wong, Ann V. LeFever, and Ping C. Lee pp 4696 - 4703; DOI: 10.1021/jm00103a007 |
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Synthesis, configuration, and activity of isomeric 2-phenyl-2-(N-piperidinyl)bicyclo[3.1.0]hexanes at phencyclidine and .sigma. binding sites Brian R. De Costa, Mariena V. Mattson, Clifford George, and Joannes T. M. Linders pp 4704 - 4712; DOI: 10.1021/jm00103a008 |
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Synthesis and antiviral activity of deoxy analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) as potent and selective anti-HIV-1 agents Hiromichi Tanaka, Hideaki Takashima, Masaru Ubasawa, Kouichi Sekiya, Issei Nitta, Masanori Baba, Shiro Shigeta, Richard T. Walker, Erik De Clercq, and Tadashi Miyasaka pp 4713 - 4719; DOI: 10.1021/jm00103a009 |
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Bioisosteric replacement of the .alpha.-amino carboxylic acid functionality in 2-amino-5-phosphonopentanoic acid yields unique 3,4-diamino-3-cyclobutene-1,2-dione containing NMDA antagonists William A. Kinney, Nancy E. Lee, Deanna T. Garrison, Edward J. Podlesny, Joanne T. Simmonds, Donna Bramlett, Ronald R. Notvest, Dianne M. Kowal, and Rene P. Tasse pp 4720 - 4726; DOI: 10.1021/jm00103a010 |
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Studies on pyridonecarboxylic acids. 1. Synthesis and antibacterial evaluation of 7-substituted-6-halo-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acids Jun Segawa, Masahiko Kitano, Kenji Kazuno, Masato Matsuoka, Ichiro Shirahase, Masakuni Ozaki, Masato Matsuda, Yoshifumi Tomii, and Masahiro Kise pp 4727 - 4738; DOI: 10.1021/jm00103a011 |
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Structural alterations in desferrioxamine compatible with iron clearance in animals Raymond J. Bergeron, Zhi Rong Liu, James S. McManis, and Jan Wiegand pp 4739 - 4744; DOI: 10.1021/jm00103a012 |
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Fluoroquinolones: relationships between structural variations, mammalian cell cytotoxicity and antimicrobial activity Mark J. Suto, John M. Domagala, Gregory E. Roland, Gail B. Mailloux, and Michael A. Cohen pp 4745 - 4750; DOI: 10.1021/jm00103a013 |
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Dihydropyrimidine angiotensin II receptor antagonists Karnail S. Atwal, Syed Z. Ahmed, J. Eileen Bird, Carol L. Delaney, Kenneth E. J. Dickinson, Francis N. Ferrara, Anders Hedberg, Arthur V. Miller, Suzanne Moreland, and et al. pp 4751 - 4763; DOI: 10.1021/jm00103a014 |
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Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against hydrogen-bonding and provides an esterase-resistant, high-affinity cocaine Alan P. Kozikowski, Marinella Roberti, Li Xiang, John S. Bergmann, Patrick M. Callahan, Kathryn A. Cunningham, and Kenneth M. Johnson pp 4764 - 4766; DOI: 10.1021/jm00103a015 |
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Potent inhibitory effect of a series of modified cyclodextrin sulfates on the replication of HIV-1 in vitro. [Erratum to document cited in CA115(17):174059j] Tamon Moriya, Hironori Kurita, Kazuo Matsumoto, Toru Otake, Haruyo Mori, Motoko Morimoto, Noboru Ueba, and Nobuharu Kunita pp 4767 - 4767; DOI: 10.1021/jm00103a016 |
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Structure and DNA binding activity of analogs of 1,5-bis(4-amidinophenoxy)pentane (pentamidine). [Erratum to document cited in CA116(9):75694b] Michael Cory, Richard R. Tidwell, and Terri A. Fairley pp 4767 - 4767; DOI: 10.1021/jm00103a017 |
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Quantitative structure-activity relationship. QSAR, analyses of the substituted indanone and benzylpiperidine rings of a series of indanone-benzylpiperidine inhibitors of acetylcholinesterase. [Erratum to document cited in CA116(9):83138p] Mario G. Cardozo, Youichi Iimura, Hachiro Sugimoto, Yoshiharu Yamanishi, and A. J. Hopfinger pp 4767 - 4767; DOI: 10.1021/jm00103a018 |
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Synthesis and antibacterial activity of new tetracyclic quinolone antibacterials. [Erratum to document cited in CA116(5):41380f] Masahiro Taguchi, Hirosato Kondo, Yoshimasa Inoue, Yoshihiro Kawahata, Yoshikau Jinbo, Fumio Sakamoto, and Goro Tsukamoto pp 4767 - 4767; DOI: 10.1021/jm00103a019 |
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CoMFA analysis of the interactions of antipicornavirus compounds in the binding pocket of human rhinovirus-14. [Erratum to document cited in CA116(15):143280r] Guy D. Diana, Paul Kowalczyk, Adi M. Treasurywala, Richard C. Oglesby, Daniel C. Pevear, and Frank J. Dutko pp 4768 - 4768; DOI: 10.1021/jm00103a020 |
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Conformational analyses and molecular-shape comparisons of a series of indanone-benzylpiperidine inhibitors of acetylcholinesterase. [Erratum to document cited in CA116(11):98893e] Mario G. Cardozo, Takatoshi Kawai, Youichi Iimura, Hachiro Sugimoto, Yoshiharu Yamanishi, and A. J. Hopfinger pp 4768 - 4768; DOI: 10.1021/jm00103a021 |
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The discovery of (2S,3S)-cis-2-(diphenylmethyl)-N-[(2-methoxyphenyl)methyl]-1-azabicyclo[2.2.2]octan-3-amine as a novel, nonpeptide substance P antagonist. [Erratum to document cited in CA117(5):48289n] John A. Lowe, III, Susan E. Drozda, R. Michael Snider, Kelly P. Longo, Stevin H. Zorn, Jean Morrone, Elisa R. Jackson, Stafford McLean, Dianne K. Bryce, and et al. pp 4768 - 4768; DOI: 10.1021/jm00103a022 |
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Editorial - Reinstatement of Notes as a Manuscript Class Philip S, Portoghese. pp 4769 - 4769; DOI: 10.1021/jm00104a601 |
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2-(Aminoalkyl)-5-nitropyrazolo[3,4,5-kl]acridines, a new class of anticancer agents David B. Capps, James Dunbar, Suzanne R. Kesten, Joan Shillis, Leslie M. Werbel, Jacqueline Plowman, and Donald L. Ward pp 4770 - 4778; DOI: 10.1021/jm00104a001 |
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Analogs of platelet activating factor. 7. Bis-aryl amide and bis-aryl urea receptor antagonists of PAF Allan Wissner, Marion L. Carroll, Bernard D. Johnson, Suresh S. Kerwar, Walter C. Pickett, Robert E. Schaub, Lawrence W. Torley, Michael P. Trova, and Constance A. Kohler pp 4779 - 4789; DOI: 10.1021/jm00104a002 |
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Synthesis and physiochemical properties of sulfamate derivatives as topical antiglaucoma agents Young S. Lo, Joseph C. Nolan, Thomas H. Maren, William J. Welstead, David F. Gripshover, and Dwight A. Shamblee pp 4790 - 4794; DOI: 10.1021/jm00104a003 |
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Inhibition of human leukocyte elastase by N-substituted peptides containing .alpha.,.alpha.-difluorostatone residues at P1 Jerry W. Skiles, Clara Miao, Ronald Sorcek, Stephen Jacober, Philip W. Mui, Grace Chow, Steve M. Weldon, Genus Possanza, Mark Skoog, and et al. pp 4795 - 4808; DOI: 10.1021/jm00104a004 |
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Antimitotic agents: ring analogs and derivatives of ethyl [(S)-5-amino-1,2-dihydro-2-methyl-3-phenylpyrido[3,4-b]pyrazin-7-yl]carbamate Carroll Temple and Gregory A. Rener pp 4809 - 4812; DOI: 10.1021/jm00104a005 |
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Selective, centrally acting serotonin 5-HT2 antagonists. 1. 2- and 6-Substituted 1-phenyl-3-(4-piperidinyl)-1H-indoles Jens Perregaard, Kim Andersen, John Hyttel, and Connie Sanchez pp 4813 - 4822; DOI: 10.1021/jm00104a006 |
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Selective, centrally acting serotonin 5-HT2 antagonists. 2. Substituted 3-(4-fluorophenyl)-1H-indoles Kim Andersen, Jens Perregaard, Joern Arn, Joern Bay Nielsen, and Mikael Begtrup pp 4823 - 4831; DOI: 10.1021/jm00104a007 |
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Hypoxia-selective antitumor agents. 6. 4-(Alkylamino)nitroquinolines: a new class of hypoxia-selective cytotoxins William A. Denny, Graham J. Atwell, Peter B. Roberts, Robert F. Anderson, Maruta Boyd, Colin J. L. Lock, and William R. Wilson pp 4832 - 4841; DOI: 10.1021/jm00104a008 |
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The conformation of 6-methoxyerythromycin A in water determined by proton NMR spectroscopy Wayne E. Steinmetz, Richard Bersch, Jeffrey Towson, and David Pesiri pp 4842 - 4845; DOI: 10.1021/jm00104a009 |
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Potential anti-AIDS naphthalenesulfonic acid derivatives. Synthesis and inhibition of HIV-1 induced cytopathogenesis and HIV-1 and HIV-2 reverse transcriptase activities Ghee T. Tan, Anura Wickramasinghe, Sandeep Verma, Rajendra Singh, Stephen H. Hughes, John M. Pezzuto, Masanori Baba, and Prem Mohan pp 4846 - 4853; DOI: 10.1021/jm00104a010 |
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N-Methylcarbamate derivatives of ellipticine and olivacine with cytotoxic activity against four human lung cancer cell lines John C. Ruckdeschel, Sandeep P. Modi, Wageeh El-Hamouly, Enrico Portuese, and Sydney Archer pp 4854 - 4857; DOI: 10.1021/jm00104a011 |
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Novel cAMP PDE III inhibitors: 1,6-naphthyridin-2(1H)-ones Baldev Singh, George Y. Lesher, Kevin C. Pluncket, Edward D. Pagani, Donald C. Bode, Ross G. Bentley, Mary J. Connell, Linda T. Hamel, and Paul J. Silver pp 4858 - 4865; DOI: 10.1021/jm00104a012 |
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New bronchodilators. 3. Imidazo[4,5-c][1,8]naphthyridin-4(5H)-ones Fumio Suzuki, Takeshi Kuroda, Takashi Kawakita, Haruhiko Manabe, Shigeto Kitamura, Kenji Ohmori, Michio Ichimura, Hiroshi Kase, and Shunji Ichikawa pp 4866 - 4874; DOI: 10.1021/jm00104a013 |
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ATP-citrate-lyase as a target for hypolipidemic intervention. Sulfoximine and 3-hydroxy-.beta.-lactam containing analogs of citric acid as potential tight-binding inhibitors Roland E. Dolle, David McNair, Mark J. Hughes, Lawrence I. Kruse, Drake Eggelston, Barbara A. Saxty, Timothy N. C. Wells, and Pieter H. E. Groot pp 4875 - 4884; DOI: 10.1021/jm00104a014 |
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.alpha.-Halo [(phenylphosphinyl)methyl]phosphonates as specific inhibitors of Na+-gradient-dependent Na+-phosphate cotransport across renal brush border membrane Charles E. McKenna, Phuong Truc T. Pham, Mark E. Rassier, and Thomas P. Dousa pp 4885 - 4892; DOI: 10.1021/jm00104a015 |
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5-HT3 receptor antagonists. 1. New quinoline derivatives Hiroaki Hayashi, Yoshikazu Miwa, Ichiro Miki, Shunji Ichikawa, Nobuyuki Yoda, Akio Ishii, Motomichi Kono, and Fumio Suzuki pp 4893 - 4902; DOI: 10.1021/jm00104a016 |
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Ketanserin analogs: structure-affinity relationships for 5-HT2 and 5-HT1C serotonin receptor binding Jeff L. Herndon, Abd Ismaiel, Stacy P. Ingher, M. Teitler, and Richard A. Glennon pp 4903 - 4910; DOI: 10.1021/jm00104a017 |
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Discovery of a potent substance P antagonist: recognition of the key molecular determinant Manoj C. Desai, Sheri L. Lefkowitz, Peter F. Thadeio, Kelly P. Longo, and R. Michael Snider pp 4911 - 4913; DOI: 10.1021/jm00104a018 |
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Book Reviews pp 4918 - 4922; DOI: 10.1021/jm00104a600 |
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Potent inhibitors of platelet aggregation based upon the Arg-Gly-Asp-Phe sequence of fibrinogen. A proposal on the nature of the binding interaction between the Asp-carboxylate of RGDX mimetics and the platelet GP IIb-IIIa receptor Jeffery A. Zablocki, Masateru Miyano, Shashidhar N. Rao, Susan Panzer-Knodle, Nancy Nicholson, and Larry Feigen pp 4914 - 4917; DOI: 10.1021/jm00104a019 |
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Editorial - Reinstatement of Notes as a Manuscript Class pp 4769 - 4769; DOI: 10.1021/jm00103a601 |