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Design and synthesis of novel cyclic RGD-containing peptides as highly potent and selective integrin .alpha.IIb.beta.3 antagonists Soan Cheng, William S. Craig, Daniel Mullen, Juerg F. Tschopp, Doug Dixon, and Michael D. Pierschbacher pp 1 - 8; DOI: 10.1021/jm00027a001 |
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TcO(PnAO-1-(2-nitroimidazole)) [BMS-181321], a new technetium-containing nitroimidazole complex for imaging hypoxia: synthesis, characterization, and xanthine oxidase-catalyzed reduction Karen E. Linder, Yee Wai Chan, John E. Cyr, Mary F. Malley, David P. Nowotnik, and Adrian D. Nunn pp 9 - 17; DOI: 10.1021/jm00027a002 |
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Novel potassium channel openers: synthesis and pharmacological evaluation of new N-(substituted-3-pyridyl)-N'-alkylthioureas and related compounds Tadahiro Takemoto, Masahiro Eda, Mitsuyoshi Hihara, Takehiro Okada, Hiroshi Sakashita, Miyuki Eiraku, Sumio Matzno, Maki Gohda, Hajime Ebisu, and et al. pp 18 - 25; DOI: 10.1021/jm00027a003 |
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6,6-Disubstituted hex-5-enoic acid derivatives as combined thromboxane A2 receptor antagonists and synthetase inhibitors Rainer Soyka, Armin Heckel, Josef Nickl, Wolfgang Eisert, Thomas H. Mueller, and Hans Weisenberger pp 26 - 39; DOI: 10.1021/jm00027a004 |
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The structural basis of camptothecin interactions with human serum albumin: impact on drug stability Thomas G. Burke and Zihou Mi pp 40 - 46; DOI: 10.1021/jm00027a005 |
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FTIR spectral study of intramolecular hydrogen bonding in thromboxane A2 receptor agonist (U-46619), prostaglandin (PG)E2, PGD2, PGF2.alpha., prostacyclin receptor agonist (carbacyclin) and their related compounds in dilute carbon tetrachloride solution: structure-activity relationships Mamoru Takasuka, Morio Kishi, and Masumi Yamakawa pp 47 - 56; DOI: 10.1021/jm00027a006 |
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Studies on antiulcer drugs. 7. 2-Guanidino-4-pyridylthiazoles as histamine H2-receptor antagonists with potent gastroprotective effects against nonsteroidal antiinflammatory drug-induced injury Yousuke Katsura, Yoshikazu Inoue, Tetsuo Tomishi, Hirohumi Ishikawa, and Hisashi Takasugi pp 57 - 66; DOI: 10.1021/jm00027a007 |
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Synthesis and DNA-sequence selectivity of a series of mono- and difunctional 9-aminoacridine nitrogen mustards Kurt W. Kohn, Ann Orr, Patrick M. O'Connor, Lynn James Guziec, and Frank S. Guziec pp 67 - 72; DOI: 10.1021/jm00027a008 |
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S-Glucosylated hydantoins as new antiviral agents Ahmed A. El-Barbary, Ahmed I. Khodair, Erik B. Pedersen, and Claus Nielsen pp 73 - 77; DOI: 10.1021/jm00027a009 |
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Structure-activity studies of benzimidazole-based DNA-cleaving agents. Comparison of benzimidazole, pyrrolobenzimidazole, and tetrahydropyridobenzimidazole analogs Edward B. Skibo, Imadul Islam, Matthew J. Heileman, and William G. Schulz pp 78 - 92; DOI: 10.1021/jm00027a010 |
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Enhancement of iron excretion via monoanionic 3-hydroxypyrid-4-ones John Josef Molenda, Mark M. Jones, and Mark A. Basinger pp 93 - 98; DOI: 10.1021/jm00027a011 |
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Mixed 5-HT1A/D-2 activity of a new model of arylpiperazines: 1-aryl-4-[3-(1,2-dihydronaphthalen-4-yl)-n-propyl]piperazines. 1. Synthesis and structure-activity relationships Roberto Perrone, Francesco Berardi, Nicola A. Colabufo, Vincenzo Tortorella, Francesco Fiorentini, Vincenzo Olgiati, Ermes Vanotti, and Stefano Govoni pp 99 - 104; DOI: 10.1021/jm00027a012 |
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Synthesis and structure activity relationships of cis- and trans-2,3,4,4a,9,9a-hexahydro-1H-indeno[2,1-c]pyridines for 5-HT receptor subtypes Michael D. Meyer, John F. DeBernardis, and Arthur A. Hancock pp 105 - 112; DOI: 10.1021/jm00027a013 |
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Conformational analysis of 5-lipoxygenase inhibitors: role of the substituents in chiral recognition and on the active conformations of the (methoxyalkyl)thiazole and methoxytetrahydropyran series Christine Lambert-van der Brempt, Pierre Bruneau, Maryannick A. Lamorlette, and Stephen J. Foster pp 113 - 124; DOI: 10.1021/jm00027a014 |
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5-Aryl-3-(alkylthio)-4H-1,2,4-triazoles as selective antagonists of strychnine-induced convulsions and potential antispastic agents John M. Kane, Michael A. Staeger, Christopher R. Dalton, Francis P. Miller, Mark W. Dudley, Ann Marie L. Ogden, John H. Kehne, Herbert J. Ketteler, Timothy C. McCloskey, and et al. pp 125 - 132; DOI: 10.1021/jm00027a015 |
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Photoactivatable 2-[(4'-azido)tetrafluorophenyl]-5-tert-butyl-1,3-dithiane bissulfone and related compounds as candidate irreversible probes for the GABA-gated chloride channels Isabelle Kapfer, Jon E. Hawkinson, John E. Casida, and Maurice P. Goeldner pp 133 - 140; DOI: 10.1021/jm00027a016 |
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Design of cyclic deltorphins and dermenkephalins with a disulfide bridge leads to analogs with high selectivity for .delta.-opioid receptors Aleksandra Misicka, Andrzej W. Lipkowski, Robert Horvath, Peg Davis, Henry I. Yamamura, Frank Porreca, and Victor J. Hruby pp 141 - 145; DOI: 10.1021/jm00027a017 |
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Cyclic enkephalin analogs with exceptional potency at peripheral .delta. opioid receptors Hubert Bartosz-Bechowski, Peg Davis, Teresa Zalewska, Jirina Slaninova, Frank Porreca, Henry I. Yamamura, and Victor J. Hruby pp 146 - 150; DOI: 10.1021/jm00027a018 |
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Interaction of tetrahydrostilbazoles with monoamine oxidase A and B Sergey O. Sablin, Matthew J. Krueger, Thomas P. Singer, Sergey O. Bachurin, Anil B. Khare, Simon M. N. Efange, and Sergey E. Tkachenko pp 151 - 157; DOI: 10.1021/jm00027a019 |
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Synthesis of novel N-phosphonoalkyl dipeptide inhibitors of human collagenase John Bird, Rachel C. De Mello, Gregory P. Harper, David J. Hunter, Eric H. Karran, Roger E. Markwell, Anette J. Miles-Williams, Shahzad S. Rahman, and Robert W. Ward pp 158 - 169; DOI: 10.1021/jm00027a020 |
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Design and synthesis of bifunctional isothiocyanate analogs of sulforaphane: correlation between structure and potency as inducers of anticarcinogenic detoxication enzymes Gary H. Posner, C.-G. Cho, Julianne V. Green, Yuesheng Zhang, and Paul Talalay pp 170 - 176; DOI: 10.1021/jm00027a021 |
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Sulfinosine congeners: synthesis and antitumor activity in mice of certain N9-alkylpurines and purine ribonucleosides Naeem B. Hanna, Birendra K. Bhattacharya, Roland K. Robins, Thomas L. Avery, and Ganapathi R. Revankar pp 177 - 183; DOI: 10.1021/jm00027a022 |
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Glycylcyclines. 1. A new generation of potent antibacterial agents through modification of 9-aminotetracyclines P.-E. Sum, Ving J. Lee, Raymond T. Testa, Joseph J. Hlavka, George A. Ellestad, Jonathan D. Bloom, Yakov Gluzman, and Francis P. Tally pp 184 - 188; DOI: 10.1021/jm00027a023 |
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Isoenzyme-specific glutathione-S-transferase inhibitors: design and synthesis Matthew H. Lyttle, Michael D. Hocker, Hon C. Hui, Colby G. Caldwell, Decius T. Aaron, Asa Engqvist-Goldstein, Jeffrey E. Flatgaard, and Karin E. Bauer pp 189 - 194; DOI: 10.1021/jm00027a024 |
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New hexahydroxybiphenyl derivatives as inhibitors of protein kinase C Yoshiki Kashiwada, Li Huang, Lawrence M. Ballas, Jack B. Jiang, William P. Janzen, and K.-H. Lee pp 195 - 200; DOI: 10.1021/jm00027a025 |
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Adenosine deaminase inhibitors: synthesis and structure-activity relationships of 2-hydroxy-3-nonyl derivatives of azoles Gloria Cristalli, Alessandra Eleuteri, Rosaria Volpini, Sauro Vittori, Emido Camaioni, and Giulio Lupidi pp 201 - 205; DOI: 10.1021/jm00027a026 |
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A recombinant human stromelysin catalytic domain identifying tryptophan derivatives as human stromelysin inhibitors Qi Zhuang Ye, Linda L. Johnson, Ian Nordan, Donald Hupe, and Lynn Hupe pp 206 - 209; DOI: 10.1021/jm00027a027 |
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Molecular electrostatic potential of D1 and D2 dopamine agonists Ibon Alkorta and Hugo O. Villar pp 210 - 213; DOI: 10.1021/jm00027a028 |
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Book Reviews pp 214 - 214; DOI: 10.1021/jm00027a600 |
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Design and synthesis of peptidomimetic inhibitors of HIV-1 protease and renin. Evidence for improved transport Amos B. Smith, III, Ralph Hirschmann, Alexander Pasternak, Ryouichi Akaishi, Mark C. Guzman, David R. Jones, Terence P. Keenan, Paul A. Sprengeler, Paul L. Darke, and et al. pp 215 - 218; DOI: 10.1021/jm00028a001 |
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Estrone sulfamates: potent inhibitors of estrone sulfatase with therapeutic potential Nicola M. Howarth, Atul Purohit, Michael J. Reed, and Barry V. L. Potter pp 219 - 221; DOI: 10.1021/jm00028a002 |
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Synthesis and Antifungal Activity of Novel Cationic Pneumocandin Bo Derivatives F. Aileen Bouffard, Robert A. Zambias, James F. Dropinski, James M. Balkovec, Milton L. Hammond, George K. Abruzzo, Kenneth F. Bartizal, Jean A. Marrinan, Myra B. Kurtz, and et al. pp 222 - 225; DOI: 10.1021/jm00028a003 |
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Novel amidine-containing peptidyl phosphonates as irreversible inhibitors for blood coagulation and related serine proteases Jozef Oleksyszyn, Bogdan Boduszek, Chih-Min Kam, and James C. Powers pp 226 - 231; DOI: 10.1021/jm00028a004 |
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Total synthesis and biological properties of novel antineoplastic (chloromethyl)furanoindolines: an asymmetric hydroboration mediated synthesis of the alkylation subunits Fariborz Mohamadi, Michael M. Spees, Gilbert S. Staten, Philip Marder, Julia K. Kipka, David A. Johnson, Dale L. Boger, and Hamideh Zarrinmayeh pp 232 - 239; DOI: 10.1021/jm00028a005 |
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3-Substituted thieno[2,3-b][1,4]thiazine-6-sulfonamides. A novel class of topically active carbonic anhydrase inhibitors Cecilia A. Hunt, Pierre J. Mallorga, Stuart R. Michelson, Harvey Schwam, John M. Sondey, Robert L. Smith, Michael F. Sugrue, and Kenneth L. Shepard pp 240 - 247; DOI: 10.1021/jm00028a006 |
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Novel cAMP PDE III inhibitors: imidazo[4,5-b]pyridin-2(3H)-ones and thiazolo[4,5-b]pyridin-2(3H)-ones and their analogs Baldev Singh, Edward R. Bacon, Shaughnessy Robinson, Richard K. Fritz, George Y. Lesher, Virendra Kumar, John A. Dority, Michael Reuman, Gee Hong Kuo, and et al. pp 248 - 254; DOI: 10.1021/jm00028a007 |
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Enhanced selectivity of oxytocin antagonists containing sarcosine in position 7 Imre Pavo, Jirina Slaninova, Falk Fahrenholz, and Uwe Klein pp 255 - 259; DOI: 10.1021/jm00028a008 |
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Synthesis and structure-activity studies of N,N'-diarylguanidine derivatives. N-(1-naphthyl)-N'-(3-ethylphenyl)-N'-methylguanidine: a new, selective noncompetitive NMDA receptor antagonist N. L. Reddy, Lain-Yen Hu, R. E. Cotter, J. B. Fischer, W. J. Wong, R. N. McBurney, E. Weber, D. L. Holmes, S. T. Wong, and et al. pp 260 - 267; DOI: 10.1021/jm00028a009 |
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Synthesis and pharmacological evaluation of phenylacetamides as sodium-channel blockers Ioannis Roufos, Sheryl J. Hays, David J. Dooley, Roy D. Schwarz, Gregory W. Campbell, and Albert W. Probert pp 268 - 274; DOI: 10.1021/jm00028a010 |
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.alpha.-Spirocyclopentyl- and .alpha.-spirocyclopropyl-.gamma.-butyrolactones: conformationally constrained derivatives of anticonvulsant and convulsant .alpha.,.alpha.-disubstituted .gamma.-butyrolactones Eileen M. Peterson, Kun Xu, Katherine D. Holland, Ann C. McKeon, Steven M. Rothman, James A. Ferrendelli, and Douglas F. Covey pp 275 - 286; DOI: 10.1021/jm00028a011 |
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Antitumor agents. 144. New .gamma.-lactone ring-modified arylamino etoposide analogs as inhibitors of human DNA topoisomerase II Xiao Ming Zhou, Kenneth Jiann Hung Lee, Ji Cheng, Shihn Sheng Wu, Hong Xing Chen, Xin Guo, Yung Chi Cheng, and Kuo Hsiung Lee pp 287 - 292; DOI: 10.1021/jm00028a012 |
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Evaluation of a vitamin-cloaking strategy for oligopeptide therapeutics: biotinylated HIV-1 protease inhibitors I. Islam, K. Y. Ng, K. T. Chong, T. J. McQuade, J. O. Hui, K. F. Wilkinson, B. D. Rush, M. J. Ruwart, R. T. Borchardt, and J. F. Fisher pp 293 - 304; DOI: 10.1021/jm00028a013 |
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Adenosine deaminase inhibitors. Synthesis and biological evaluation of 4-amino-1-[2(S)-hydroxy-3(R)-nonyl]-1H-imidazo[4,5-c]pyridine [3-deaza-(+)-EHNA] and certain C1' derivatives Geraldine C. B. Harriman, Elie Abushanab, and Johanna D. Stoeckler pp 305 - 308; DOI: 10.1021/jm00028a014 |
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Tetrapeptide CCK agonists: structure-activity studies on modifications at the N-terminus Richard L. Elliott, Hana Kopecka, Michael J. Bennett, Youe Kong Shue, Richard Craig, Chun Wel Lin, Bruce R. Bianchi, Thomas R. Miller, David G. Witte, and et al. pp 309 - 313; DOI: 10.1021/jm00028a015 |
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A new approach to the design of .sigma.-2-selective ligands: synthesis and evaluation of N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(1-pyrrolidinyl)ethylamine-related polyamines at .sigma.-1 and .sigma.-2 receptor subtypes Brian R. de Costa, Xiao-shu He, Celia Dominguez, Janet Cutts, Wanda Williams, and Wayne D. Bowen pp 314 - 321; DOI: 10.1021/jm00028a016 |
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Synthesis and biological evaluation of 5-[[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]methylene]oxazoles, -thiazoles, and -imidazoles: novel dual 5-lipoxygenase and cyclooxygenase inhibitors with antiinflammatory activity Paul C. Unangst, David T. Connor, Wiaczeslaw A. Cetenko, Roderick J. Sorenson, Catherine R. Kostlan, Jagadish C. Sircar, Clifford D. Wright, Denis J. Schrier, and Richard D. Dyer pp 322 - 328; DOI: 10.1021/jm00028a017 |
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The Discovery of Sulfonamide Endothelin Antagonists and the Development of the Orally Active ETA Antagonist 5-(Dimethylamino)-N-(3,4-dimethyl-5- isoxazolyl)-1-naphthalenesulfonamide Philip D. Stein, John T. Hunt, David M. Floyd, Suzanne Moreland, Kenneth E. J. Dickinson, Caroline Mitchell, Eddie C.-K. Liu, Maria L. Webb, Natesan Murugesan, and et al. pp 329 - 331; DOI: 10.1021/jm00029a001 |
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A New Potent and Selective Histamine H3 Receptor Agonist, 4-(1H-imidazol-4-ylmethyl)piperidine Roeland C. Vollinga, Johannes P. de Koning, Frank P. Jansen, Rob Leurs, Wiro M. P. B. Menge, and Hendrik Timmerman pp 332 - 333; DOI: 10.1021/jm00029a002 |
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Enzyme-Activated Antagonists of the Strychnine-Insensitive Glycine/NMDA Receptor Francesco G. Salituro, Ronald C. Tomlinson, Bruce M. Baron, Michael G. Palfreyman, Ian A. McDonald, Werner Schmidt, Hui Qiu Wu, Paolo Guidetti, and Robert Schwarcz pp 334 - 336; DOI: 10.1021/jm00029a003 |
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Rational modification of human synovial fluid phospholipase A2 inhibitors M. Teresa Pisabarro, Angel R. Ortiz, Albert Palomer, Francesc Cabre, Luisa Garcia, Rebecca C. Wade, Federico Gago, David Mauleon, and Germano Carganico pp 337 - 341; DOI: 10.1021/jm00029a004 |
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Substituted O6-Benzylguanine Derivatives and Their Inactivation of Human O6-Alkylguanine-DNA Alkyltransferase Mi Young Chae, Mark G. McDougall, M. Eileen Dolan, Kristin Swenn, Anthony E. Pegg, and Robert C. Moschel pp 342 - 347; DOI: 10.1021/jm00029a005 |
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Design, synthesis, and in vitro activity of bis(succinimido)hexane peptide heterodimers with combined B1 and B2 antagonist activity John C. Cheronis, Eric T. Whalley, Lisa G. Allen, Sharon D. Loy, Megan W. Elder, Matthew J. Duggan, Kelly L. Gross, and James K. Blodgett pp 348 - 355; DOI: 10.1021/jm00029a006 |
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Structure, determination, pharmacological evaluation, and structure-activity studies of a new cyclic peptide substance P antagonist containing the new amino acid 3-prenyl-.beta.-hydroxytyrosine isolated from Aspergillus flavipes Colin J. Barrow, Muriel S. Doleman, Mark A. Bobko, and Raymond Cooper pp 356 - 363; DOI: 10.1021/jm00029a007 |
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Piperidinyltetralin .sigma. Ligands Paul J. Gilligan, Ahmed A. Kergaye, Bryan M. Lewis, and John F. McElroy pp 364 - 370; DOI: 10.1021/jm00029a008 |
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Relationships between structure and kinetics of cyclization of 2-aminoaryl amides: potential prodrugs of cyclization-activated aromatic mustards Graham J. Atwell, Bridget M. Sykes, Charmian J. O'Connor, and William A. Denny pp 371 - 380; DOI: 10.1021/jm00029a009 |
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Hypoxia-selective antitumor agents. 8. Bis(nitroimidazolyl)alkanecarboxamides: a new class of hypoxia-selective cytotoxins and hypoxic cell radiosensitizers Michael P. Hay, William R. Wilson, John W. Moselen, Brian D. Palmer, and William A. Denny pp 381 - 391; DOI: 10.1021/jm00029a010 |
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CNAD: a potent and specific inhibitor of alcohol dehydrogenase Barry M. Goldstein, Hong Li, Jeffrey P. Jones, J. Ellis Bell, Joanna Zeidler, Krzysztof W. Pankiewicz, and Kyoichi A. Watanabe pp 392 - 399; DOI: 10.1021/jm00029a011 |
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Dual-Action Cephalosporins Incorporating a 3'-Tertiary-Amine-Linked Quinolone Harry A. Albrecht, George Beskid, James G. Christenson, Kenneth H. Deitcher, Nafsika H. Georgopapadakou, Dennis D. Keith, Frederick M. Konzelmann, David L. Pruess, and Chung Chen Wei pp 400 - 407; DOI: 10.1021/jm00029a012 |
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Synthesis of high specific activity tritium-labeled [3H]-9-cis-retinoic acid and its application for identifying retinoids with unusual binding properties Marcus F. Boehm, Michael R. McClurg, Charles Pathirana, David Mangelsdorf, Steven K. White, Jonathan Hebert, David Winn, Mark E. Goldman, and Richard A. Heyman pp 408 - 414; DOI: 10.1021/jm00029a013 |
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Synthesis and Photodynamic Activities of Silicon 2,3-Naphthalocyanine Derivatives Nicole Brasseur, Tan-Loc Nguyen, Rejean Langlois, Rene Ouellet, Stephanie Marengo, Daniel Houde, and Johan E. van Lier pp 415 - 420; DOI: 10.1021/jm00029a014 |
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Selective Protection and Relative Importance of the Carboxylic Acid Groups of Zaragozic Acid A for Squalene Synthase Inhibition Tesfaye Biftu, John J. Acton, Gregory D. Berger, James D. Bergstrom, Claude Dufresne, Marc M. Kurtz, Robert W. Marquis, William H. Parsons, Deborah R. Rew, and Kenneth E. Wilson pp 421 - 424; DOI: 10.1021/jm00029a015 |
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Isosteric phosphonate analogs of ET-16-OMe. Synthesis and biological evaluation of the enantiomers of 2'-(Trimethylammonio)ethyl 4-(hexadecyloxy)-3-methoxybutanephosphonate and 2'-(trimethylammonio)ethyl 4-(hexadecylthio)-3-methoxybutanephosphonate Robert Bittman, Hoe Sup Byun, Brenda Mercier, and Hassan Salari pp 425 - 430; DOI: 10.1021/jm00029a016 |
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Solid-State and Solution Conformations of the Potent HIV Inhibitor, 4'-Azidothymidine Hans Maag, Janis T. Nelson, Jorge L. Rios Steiner, and Ernest J. Prisbe pp 431 - 438; DOI: 10.1021/jm00030a001 |
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Potent Gastrin-Releasing Peptide (GRP) Antagonists Derived from GRP(19-27) with a C-Terminal DPro.PSI.[CH2NH]Phe-NH2 and N-Terminal Aromatic Residues Johann J. Leban, Antonio Landavazo, John D. McDermed, Emanuel J. Diliberto, Marilyn Jansen, Beth Stockstill, and Frederick C. Kull pp 439 - 445; DOI: 10.1021/jm00030a002 |
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Antitumor Agents. 148. Synthesis and Biological Evaluation of Novel 4.beta.-Amino Derivatives of Etoposide with Better Pharmacological Profiles Yi Lin Zhang, Xin Guo, Yung Chi Cheng, and Kuo Hsiung Lee pp 446 - 452; DOI: 10.1021/jm00030a003 |
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Novel Series of TSAO-T Derivatives. Synthesis and Anti-HIV-1 Activity of 4-, 5-, and 6-Substituted Pyrimidine Analogs Ana San-Felix, Sonsoles Velazquez, Maria Jesus Perez-Perez, Jan Balzarini, Erik De Clercq, and Maria Jose Camarasa pp 453 - 460; DOI: 10.1021/jm00030a004 |
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Copper Complexation by 3-Hydroxypyridin-4-one Iron Chelators: Structural and Iron Competition Studies Ali El-Jammal, P. Lynne Howell, Mary A. Turner, Naiyin Li, and Douglas M. Templeton pp 461 - 466; DOI: 10.1021/jm00030a005 |
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6-(1H-Imidazol-1-yl)-7-nitro-2,3(1H,4H)-quinoxalinedione hydrochloride (YM90K) and related compounds: structure-activity relationships for the AMPA-type non-NMDA receptor J. Ohmori, S. Sakamoto, H. Kubota, M. Shimizu-Sasamata, M. Okada, S. Kawasaki, K. Hidaka, J. Togami, T. Furuya, and K. Murase pp 467 - 475; DOI: 10.1021/jm00030a006 |
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Inhibition of Cyclic Nucleotide Phosphodiesterase by Derivatives of 1,3-Bis(cyclopropylmethyl)xanthine Derek R. Buckle, Jonathan R. S. Arch, Brendan J. Connolly, Ashley E. Fenwick, Keith A. Foster, Kenneth J. Murray, Simon A. Readshaw, Mark Smallridge, and David G. Smith pp 476 - 485; DOI: 10.1021/jm00030a007 |
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Non-peptide Renin Inhibitors Containing 2-(((3-Phenylpropyl)phosphoryl)oxy)alkanoic Acid Moieties as P2-P3 Replacements Peter Raddatz, Klaus-Otto Minck, Friedrich Rippmann, and Claus-Jochen Schmitges pp 486 - 497; DOI: 10.1021/jm00030a008 |
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N-Phosphonomethyl Dipeptides and Their Phosphonate Prodrugs, a New Generation of Neutral Endopeptidase (NEP, EC 3.4.24.11) Inhibitors Stephane De Lombaert, Mark D. Erion, Jenny Tan, Louis Blanchard, Lena El-Chehabi, R. D. Ghai, Yumi Sakane, Carol Berry, and Angelo J. Trapani pp 498 - 511; DOI: 10.1021/jm00030a009 |
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Naphthalenic Lignan Lactones as Selective, Nonredox 5-Lipoxygenase Inhibitors. Synthesis and Biological Activity of (Methoxyalkyl)thiazole and Methoxytetrahydropyran Hybrids Yves Ducharme, Christine Brideau, Daniel Dube, Chi Chung Chan, Jean Pierre Falgueyret, John W. Gillard, Jocelyne Guay, John H. Hutchinson, Cyryl S. McFarlane, and et al. pp 512 - 518; DOI: 10.1021/jm00030a010 |
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Pyridobenzoxazepine and Pyridobenzothiazepine Derivatives as Potential Central Nervous System Agents: Synthesis and Neurochemical Study Jean Francois F. Liegeois, Francoise A. Rogister, Jacques Bruhwyler, Jacques Damas, Thuy Phuong Nguyen, Maria Olvido Inarejos, Eric M. G. Chleide, Michel G. A. Mercier, and Jacques E. Delarge pp 519 - 525; DOI: 10.1021/jm00030a011 |
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Inhibitors of Cholesterol Biosynthesis. 2. Hypocholesterolemic and Antioxidant Activities of Benzopyran and Tetrahydronaphthalene Analogs of the Tocotrienols Bradley C. Pearce, Rex A. Parker, Michael E. Deason, Douglas D. Dischino, Elizabeth Gillespie, Asaf A. Qureshi, J. J. Kim Wright, and Kevin Volk pp 526 - 541; DOI: 10.1021/jm00030a012 |
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Pyrido[2,3-d]pyrimidine Angiotensin II Antagonists John W. Ellingboe, Madelene Antane, Thomas T. Nguyen, Michael D. Collini, Schuyler Antane, Reinhold Bender, Dale Hartupee, Valerie White, John McCallum, and et al. pp 542 - 550; DOI: 10.1021/jm00030a013 |
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Antiviral Enantiomeric Preference for 5'-Noraristeromycin Suhaib M. Siddiqi, Xing Chen, Stewart W. Schneller, Satoru Ikeda, Robert Snoeck, Graciela Andrei, Jan Balzarini, and Erik De Clercq pp 551 - 554; DOI: 10.1021/jm00030a014 |
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Book Reviews pp 555 - 556; DOI: 10.1021/jm00030a600 |
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Discovery of new non-phospholipid inhibitors of the secretory phospholipases A2 Haydn G. Beaton, Colin Bennion, Stephen Connolly, Anthony R. Cook, Nigel P. Gensmantel, Catherine Hallam, Kim Hardy, Barbara Hitchin, Clive G. Jackson, and David H. Robinson pp 557 - 559; DOI: 10.1021/jm00031a001 |
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Inhibitors of Acyl-CoA:cholesterol O-Acyl Transferase (ACAT) as Hypocholesterolemic Agents.6.The First Water-Soluble ACAT Inhibitor with Lipid-Regulating Activity Drago R. Sliskovic, Brian R. Krause, Joseph A. Picard, Maureen Anderson, Richard F. Bousley, Katherine L. Hamelehle, Reynold Homan, Thomas N. Julian, Zara A. Rashidbaigi, and Richard L. Stanfield pp 560 - 562; DOI: 10.1021/jm00031a002 |
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P1 Aspartate-Based Peptide .alpha.-((2,6-Dichlorobenzoyl)oxy)methyl Ketones as Potent Time-Dependent Inhibitors of Interleukin-1.beta.-Converting Enzyme Roland E. Dolle, Denton Hoyer, C. V. C. Prasad, Stanley J. Schmidt, Carla T. Helaszek, Robert E. Miller, and Mark A. Ator pp 563 - 564; DOI: 10.1021/jm00031a003 |
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1-(((7,7-Dimethyl-2(S)-(2(S)-amino-4-(methylsulfonyl)butyramido)bicyclo[2.2.1]heptan-1(S)-yl)methyl)sulfonyl)-4-(2-methylphenyl)piperazine (L-368,899): An Orally Bioavailable, Non-Peptide Oxytocin Antagonist with Potential Utility for Managing Preterm Labor Peter D. Williams, Paul S. Anderson, Richard G. Ball, Mark G. Bock, LeighAnne Carroll, Shuet-Hing Lee Chiu, Bradley V. Clineschmidt, J. Chris Culberson, Jill M. Erb, and et al. pp 565 - 571; DOI: 10.1021/jm00031a004 |
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Synthesis and Antifungal Activity of 1,3,2-Benzodithiazole S-Oxides Larry L. Klein, Clinton M. Yeung, David E. Weissing, Paul A. Lartey, S. Ken Tanaka, Jacob J. Plattner, and Darcy J. Mulford pp 572 - 578; DOI: 10.1021/jm00031a005 |
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Synthesis of naltrexone-derived .delta.-opioid antagonists. Role of conformation of the .delta. address moiety P. S. Portoghese, M. Sultana, S. T. Moe, and A. E. Takemori pp 579 - 585; DOI: 10.1021/jm00031a006 |
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Synthesis and Antibacterial Activity of Thiazolopyrazine-Incorporated Tetracyclic Quinolone Antibacterials Yoshimasa Inoue, Hirosato Kondo, Masahiro Taguchi, Yoshikazu Jinbo, Fumio Sakamoto, and Goro Tsukamoto pp 586 - 592; DOI: 10.1021/jm00031a007 |
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Electron-Deficient DNA Intercalating Agents as Antitumor Drugs: Aza Analogs of the Experimental Clinical Agent N-[2-(Dimethylamino)ethyl]acridine-4-carboxamide Qingping Chen, Leslie W. Deady, Bruce C. Baguley, and William A. Denny pp 593 - 597; DOI: 10.1021/jm00031a008 |
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Tyrosine kinase inhibitors. 2. Synthesis of 2,2'-dithiobis(1H-indole-3-alkanamides) and investigation of their inhibitory activity against epidermal growth factor receptor and pp60v-src protein tyrosine kinases Andrew M. Thompson, David W. Fry, Alan J. Kraker, and William A. Denny pp 598 - 609; DOI: 10.1021/jm00031a009 |
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Synthesis and Structure-Activity Relationships of the Novel Homopropargylamine Antimycotics Peter Nussbaumer, Ingrid Leitner, and Anton Stuetz pp 610 - 615; DOI: 10.1021/jm00031a010 |
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Molecular Modeling Studies on Ligand Binding to Sialidase from Influenza Virus and the Mechanism of Catalysis Neil R. Taylor and Mark von Itzstein pp 616 - 624; DOI: 10.1021/jm00031a011 |
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New N.alpha.-Guanidinobenzoyl Derivatives of Hirudin-54-65 Containing Stabilized Carboxyl or Phosphoryl Groups on the Side Chain of Phenylalanine-63 Christophe Thurieau, Serge Simonet, Joseph Paladino, Jean-Francois Prost, Tony Verbeuren, and Jean-Luc Fauchere pp 625 - 629; DOI: 10.1021/jm00031a012 |
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Tetrapeptide CCK-A Agonists: Effect of Backbone N-Methylations on in vitro and in vivo CCK Activity Mark W. Holladay, Hana Kopecka, Thomas R. Miller, Lisa Bednarz, A. L. Nikkel, Bruce R. Bianchi, David G. Witte, Kazumi Shiosaki, Chun Wel Lin, and et al. pp 630 - 635; DOI: 10.1021/jm00031a013 |
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Structure-Activity Relationships of N6-Benzyladenosine-5'-uronamides as A3-Selective Adenosine Agonists Carola Gallo-Rodriguez, Xiao-duo Ji, Neli Melman, Barry D. Siegman, Lawrence H. Sanders, Jeraldine Orlina, Bilha Fischer, Quanlong Pu, Mark E. Olah, and et al. pp 636 - 646; DOI: 10.1021/jm00031a014 |
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Modulation of the Kynurenine Pathway in Search for New Neuroprotective Agents.Synthesis and Preliminary Evaluation of (m-Nitrobenzoyl)alanine, a Potent Inhibitor of Kynurenine-3-hydroxylase Roberto Pellicciari, Benedetto Natalini, Gabriele Costantino, Mahmoud R. Mahmoud, Luisa Mattoli, Bahman M. Sadeghpour, Flavio Moroni, Alberto Chiarugi, and Raffaella Carpenedo pp 647 - 655; DOI: 10.1021/jm00031a015 |
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The Solution Structure of a Monocyclic Analog of Endothelin [1,15 Aba]-ET-1, Determined by 1H NMR Spectroscopy Murray Coles, Sharon L. A. Munro, and David J. Craik pp 656 - 664; DOI: 10.1021/jm00031a016 |
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Haloperidol-Based Irreversible Inhibitors of the HIV-1 and HIV-2 Proteases James J. De Voss, Zhihua Sui, Dianne L. DeCamp, Rafael Salto, Lilia M. Babe, Charles S. Craik, and Paul R. Ortiz de Montellano pp 665 - 673; DOI: 10.1021/jm00031a017 |
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Matrix Metalloproteinase Inhibitors Containing a [(Carboxyalkyl)amino]zinc Ligand: Modification of the P1 and P2' Residues Frank K. Brown, Peter J. Brown, D. Mark Bickett, C. Lynn Chambers, H. Geoff Davies, David N. Deaton, David Drewry, Michael Foley, Andrew B. McElroy, and et al. pp 674 - 688; DOI: 10.1021/jm00031a018 |
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Novel [2-(4-Piperidinyl)ethyl](thio)ureas: synthesis and antiacetylcholinesterase activity Jean-Louis Vidaluc, Francis Calmel, Dennis Bigg, Elisabeth Carilla, Antoine Stenger, Philippe Chopin, and Mike Briley pp 689 - 695; DOI: 10.1021/jm00031a019 |
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An X-ray Crystallographic Study of the Nonsteroidal Contraceptive Agent Centchroman Suprabhat Ray, Amita Tandon, Indra Dwivedy, Scott R. Wilson, James P. O'Neil, and John A. Katzenellenbogen pp 696 - 700; DOI: 10.1021/jm00031a020 |
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In vitro and in vivo Activities of Reduced-Size Antagonists of Luteinizing Hormone-Releasing Hormone Fortuna Haviv, Timothy D. Fitzpatrick, Charles J. Nichols, Eugene N. Bush, Gilbert Diaz, Gary Bammert, A. T. Nguyen, Edwin S. Johnson, Judith Knittle, and Jonathan Greer pp 701 - 705; DOI: 10.1021/jm00031a021 |
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Isolation, Structural Determination, and Biological Activity of 6.alpha.-Hydroxytaxol, the Principal Human Metabolite of Taxol James W. Harris, Aspandiar Katki, Lawrence W. Anderson, Gwendolyn N. Chmurny, Joseph V. Paukstelis, and Jerry M. Collins pp 706 - 709; DOI: 10.1021/jm00031a022 |
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Synthesis of 2-Methyl-(Z)-4-(phenylimino)naphth[2,3-d]oxazol-9-one, a Monoimine Quinone with Selective Cytotoxicity toward Cancer Cells Violeta Benedetti-Doctorovich, Edward M. Burgess, John Lambropoulos, Daniel Lednicer, Donald Van Derveer, and Leon H. Zalkow pp 710 - 712; DOI: 10.1021/jm00031a023 |
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Book Reviews pp 713 - 716; DOI: 10.1021/jm00031a600 |
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3-Alkoxybenzo[b]thiophene-2-carboxamides as Inhibitors of Neutrophil-Endothelial Cell Adhesion Diane H. Boschelli, James B. Kramer, David T. Connor, Mark E. Lesch, Denis J. Schrier, Mark A. Ferin, and Clifford D. Wright pp 717 - 718; DOI: 10.1021/jm00032a001 |
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High-Affinity and Potent, Water-Soluble 5-Amino-1,4-benzodiazepine CCKB/Gastrin Receptor Antagonists Containing a Cationic Solubilizing Group Graham A. Showell, Sylvie Bourrain, Joseph G. Neduvelil, Stephen R. Fletcher, Raymond Baker, Alan P. Watt, Alan E. Fletcher, Stephen B. Freedman, John A. Kemp, and et al. pp 719 - 721; DOI: 10.1021/jm00032a002 |
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Second-Generation Benzodiazepine CCK-B Antagonists. Development of Subnanomolar Analogs with Selectivity and Water Solubility Mark G. Bock, Robert M. DiPardo, Eva C. Mellin, Randall C. Newton, Daniel F. Veber, Stephen B. Freedman, Alison J. Smith, Smita Patel, John A. Kemp, George R. Marshall, Alan E. Fletcher, Kerry L. Chapman, Paul S. Anderson, and Roger M. Freidinger pp 722 - 724; DOI: 10.1021/jm00032a003 |
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Pseudopeptide Inhibitors of Ras Farnesyl-Protein Transferase Samuel L. Graham, S. Jane deSolms, Elizabeth A. Giuliani, Nancy E. Kohl, Scott D. Mosser, Allen I. Oliff, David L. Pompliano, Elaine Rands, Michael J. Breslin, and et al. pp 725 - 732; DOI: 10.1021/jm00032a004 |
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Synthesis and antibacterial activity of new quinolones containing a 7-[3-(1-amino-1-methylethyl)-1-pyrrolidinyl] moiety. Gram-positive agents with excellent oral activity and low side-effect potential Susan E. Hagen, John M. Domagala, Stephen J. Gracheck, Josephine A. Sesnie, Michael A. Stier, and Mark J. Suto pp 733 - 738; DOI: 10.1021/jm00032a005 |
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Phosphonate Analogs of Carbocyclic Nucleotides Robert D. Elliott, Gregory A. Rener, James M. Riordan, John A. Secrist, L. Lee Bennett, William B. Parker, and John A. Montgomery pp 739 - 744; DOI: 10.1021/jm00032a006 |
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Synthesis of benzo-fused benzodiazepines employed as probes of the agonist pharmacophore of benzodiazepine receptors Weijiang Zhang, Konrad F. Koehler, Bradford Harris, Phil Skolnick, and James M. Cook pp 745 - 757; DOI: 10.1021/jm00032a007 |
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Antagonist, Partial Agonist, and Full Agonist Imidazo[1,5-a]quinoxaline Amides and Carbamates Acting through the GABAA/Benzodiazepine Receptor Ruth E. TenBrink, Wha B. Im, Vimala H. Sethy, Andrew H. Tang, and Don B. Carter pp 758 - 768; DOI: 10.1021/jm00032a008 |
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Conformationally Constrained Peptides and Semipeptides Derived from RGD as Potent Inhibitors of the Platelet Fibrinogen Receptor and Platelet Aggregation Fadia E. Ali, Donald B. Bennett, Raul R. Calvo, John D. Elliott, Shing-Mei Hwang, Thomas W. Ku, M. Amparo Lago, Andrew J. Nichols, Todd T. Romoff, and et al. pp 769 - 780; DOI: 10.1021/jm00032a009 |
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Comparative Molecular Field Analysis of the Antitumor Activity of 9H-Thiioxanthen-9-one Derivatives against Pancreatic Ductal Carcinoma 03 Jerome P. Horwitz, Irina Massova, Thomas E. Wiese, Brent H. Besler, and Thomas H. Corbett pp 781 - 786; DOI: 10.1021/jm00032a010 |
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Molecular Modeling Studies of Aldose Reductase Inhibitors Yong S. Lee, Robert Pearlstein, and Peter F. Kador pp 787 - 792; DOI: 10.1021/jm00032a011 |
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HIV-Inhibitory Natural Products. 11. Comparative Studies of Sulfated Sterols from Marine Invertebrates Tawnya C. McKee, John H. Cardellina II, Raffaele Riccio, Maria Valeria D'Auria, Maria Iorizzi, Luigi Minale, Robert A. Moran, Robert J. Gulakowski, James B. McMahon, and et al. pp 793 - 797; DOI: 10.1021/jm00032a012 |
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Synthesis and Biological Evaluation of 2',3'-Dideoxy-L-pyrimidine Nucleosides as Potential Antiviral Agents against Human Immunodeficiency Virus (HIV) and Hepatitis B Virus (HBV) Tai-Shun Lin, Mei-Zhen Luo, Mao-Chin Liu, S. Balakrishna Pai, Ginger E. Dutschman, and Yung-Chi Cheng pp 798 - 803; DOI: 10.1021/jm00032a013 |
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Inhibitors of Acyl-CoA:Cholesterol Acyltransferase. 1. Synthesis and Hypocholesterolemic Activity of Dibenz[b,e]oxepin-11-carboxanilides Toshiaki Kumazawa, Masashi Yanase, Hiroyuki Harakawa, Hiroyuki Obase, Shiro Shirakura, Eiko Ohishi, Shoji Oda, Kazuhiro Kubo, and Koji Yamada pp 804 - 810; DOI: 10.1021/jm00032a014 |
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[D-TRP32]Neuropeptide Y: A Competitive Antagonist of NPY in Rat Hypothalamus A. Balasubramaniam, S. Sheriff, M. E. Johnson, M. Prabhakaran, Y. Huang, J. E. Fischer, and W. T. Chance pp 811 - 815; DOI: 10.1021/jm00032a015 |
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Synthesis, Characterization, and Biological Activity of a New Potent Class of Anti-HIV Agents, the Peroxoniobium-Substituted Heteropolytungstates Gyu-Shik Kim, Deborah A. Judd, Craig L. Hill, and Raymond F. Schinazi pp 816 - 820; DOI: 10.1021/jm00032a016 |
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Enhanced Brain Delivery of an Anti-HIV Nucleoside 2'-F-ara-ddI by Xanthine Oxidase Mediated Biotransformation Kirupa Shanmuganathan, Tatiana Koudriakova, Satyanarayana Nampalli, Jinfa Du, James M. Gallo, Raymond F. Schinazi, and Chung K. Chu pp 821 - 827; DOI: 10.1021/jm00032a017 |
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6,9-Bis[(aminoalkyl)amino]benzo[g]isoquinoline-5,10-diones. A Novel Class of Chromophore-Modified Antitumor Anthracene-9,10-diones: Synthesis and Antitumor Evaluations A. Paul Krapcho, Mary E. Petry, Zelleka Getahun, John J. Landi Jr., John Stallman, Johanna F. Polsenberg, Cynthia E. Gallagher, Martin J. Maresch, Miles P. Hacker, and et al. pp 828 - 837; DOI: 10.1021/jm00032a018 |
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Benzo[f]quinazoline Inhibitors of Thymidylate Synthase: Methyleneamino-Linked Aroylglutamate Derivatives William Pendergast, Scott H. Dickerson, Inderjit K. Dev, Robert Ferone, David S. Duch, and Gary K. Smith pp 838 - 844; DOI: 10.1021/jm00032a019 |
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Structure-Activity Relationships in a Series of 5-[(2,5-Dihydroxybenzyl)amino]salicylate Inhibitors of EGF-Receptor-Associated Tyrosine Kinase: Importance of Additional Hydrophobic Aromatic Interactions Huixiong Chen, Janine Boiziau, Fabienne Parker, Patrick Mailliet, Alain Commercon, Bruno Tocque, Jean-Bernard Le Pecq, Bernard-Pierre Roques, and Christiane Garbay pp 845 - 859; DOI: 10.1021/jm00032a020 |
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Preferred Orientations in the Binding of 4'-Hydroxyacetanilide (Acetaminophen) to Cytochrome P450 1A1 and 2B1 Isoforms as Determined by 13C- and 15N-NMR Relaxation Studies Timothy G. Myers, Kenneth E. Thummel, Thomas F. Kalhorn, and Sidney D. Nelson pp 860 - 867; DOI: 10.1021/jm00032a021 |
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The Novel Ins(1,4,5)P3 Analog 3-Amino-3-deoxy-Ins(1,4,5)P3: A pH-Dependent Ins(1,4,5)P3 Receptor Partial Agonist in SH-SY5Y Neuroblastoma Cells Alan P. Kozikowski, Abdul H. Fauq, Robert A. Wilcox, R. A. John Challiss, and Stefan R. Nahorski pp 868 - 872; DOI: 10.1021/jm00032a022 |
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Specific Inhibitors of Ileal Bile Acid Transport Guenther Wess, Werner Kramer, Alfons Enhsen, Heiner Glombik, Karl-Heinz Baringhaus, Georg Boeger, Matthias Urmann, Klaus Bock, Horst Kleine, and et al. pp 873 - 875; DOI: 10.1021/jm00033a001 |
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A new orally active insulin-mimetic vanadyl complex: bis(pyrrolidine-N-carbodithioato)oxovanadium(IV) Hiromi Watanabe, Masami Nakai, Kyoko Komazawa, and Hiromu Sakurai pp 876 - 877; DOI: 10.1021/jm00033a002 |
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Resolution, Absolute Stereochemistry, and Pharmacology of the S-(+)- and R-(-)-Isomers of the Apparent Partial AMPA Receptor Agonist (R,S)-2-Amino-3-(3-hydroxy-5-phenylisoxazol-4-yl)propionic Acid [(R,S)-APPA] Bjarke Ebert, Sibylle Lenz, Lotte Brehm, Peter Bregnedal, Jan J. Hansen, Kristen Frederiksen, Klaus P. Bogeso, and Povl Krogsgaard-Larsen pp 878 - 884; DOI: 10.1021/jm00033a003 |
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Synthesis of L-Thiocitrulline, L-Homothiocitrulline, and S-Methyl-L-thiocitrulline: A New Class of Potent Nitric Oxide Synthase Inhibitors Krishnaswamy Narayanan and Owen W. Griffith pp 885 - 887; DOI: 10.1021/jm00033a004 |
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Enkephalin Analogs as Systemically Active Antinociceptive Agents: O- and N-Alkylated Derivatives of the Dipeptide Amide L-2,6-Dimethyltyrosyl-N-(3-phenylpropyl)-D-alaninamide Barnett S. Pitzele, Robert W. Hamilton, Kathleen D. Kudla, Sofya Tsymbalov, Awilda Stapelfeld, Michael A. Savage, Michael Clare, Donna L. Hammond, and Donald W. Hansen pp 888 - 896; DOI: 10.1021/jm00033a005 |
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A Novel 3-Substituted Benzazepinone Growth Hormone Secretagogue (L-692,429) William R. Schoen, Judith M. Pisano, Kristine Prendergast, Matthew J. Wyvratt, Michael H. Fisher, Kang Cheng, Wanda W.-S. Chan, Bridget Butler, Roy G. Smith, and Richard G. Ball pp 897 - 906; DOI: 10.1021/jm00033a006 |
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Synthesis of Selective Non-Ca2+ Mobilizing Inhibitors of D-myo-Inositol 1,4,5-Trisphosphate 5-Phosphatase Dethard Lampe, Changsheng Liu, and Barry V. L. Potter pp 907 - 912; DOI: 10.1021/jm00033a007 |
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Benzoxazolamines and Benzothiazolamines: Potent, Enantioselective Inhibitors of Leukotriene Biosynthesis with a Novel Mechanism of Action Edward S. Lazer, Clara K. Miao, Hin-Chor Wong, Ronald Sorcek, Denice M. Spero, Alex Gilman, Kollol Pal, Mark Behnke, Anne G. Graham, and et al. pp 913 - 923; DOI: 10.1021/jm00033a008 |
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Iron(III)-Chelating Resins. IX. Antibacterial Activity of a Water-Insoluble Iron(III)-Chelating Resin Minhua Feng, Leen van der Does, and Adriaan Bantjes pp 924 - 927; DOI: 10.1021/jm00033a009 |
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Homodimeric and Heterodimeric Bis(amino thiol) Oxometal Complexes with Rhenium(V) and Technetium(V). Control of Heterodimeric Complex Formation and an Approach to Metal Complexes that Mimic Steroid Hormones Dae Yoon Chi, James P. O'Neil, Carolyn J. Anderson, Michael J. Welch, and John A. Katzenellenbogen pp 928 - 937; DOI: 10.1021/jm00033a010 |
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Guaiacoxypropanolamine Derivatives of Capsaicin: A New Family of .beta.-Adrenoceptor Blockers with Intrinsic Cardiotonic Properties Ing-Jun Chen, Jwu-Lai Yeh, Shwu-Jen Liou, and Ai-Yu Shen pp 938 - 943; DOI: 10.1021/jm00033a011 |
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Novel 4-(Aryloxy)tetrahydropyridine Analogs of MPTP as Monoamine Oxidase A and B Substrates Amit S. Kalgutkar, Kay Castagnoli, Andrea Hall, and Neal Castagnoli pp 944 - 949; DOI: 10.1021/jm00033a012 |
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Development of a Receptor-Interaction Model for Serotonin 5-HT2 Receptor Antagonists. Predicting Selectivity with Respect to Dopamine D2 Receptors Kim Andersen, Tommy Liljefors, Klaus Gundertofte, Jens Perregaard, and Klaus P. Bogeso pp 950 - 962; DOI: 10.1021/jm00033a013 |
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The Use of the GRID Program in the 3-D QSAR Analysis of a Series of Calcium-Channel Agonists Andrew M. Davis, Nigel P. Gensmantel, Erik Johansson, and David P. Marriott pp 963 - 972; DOI: 10.1021/jm00033a014 |
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A Nonlinear Map of Substituent Constants for Selecting Test Series and Deriving Structure-Activity Relationships. I. Aromatic Series Daniel Domine, James Devillers, and Maurice Chastrette pp 973 - 980; DOI: 10.1021/jm00033a015 |
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A Nonlinear Map of Substituent Constants for Selecting Test Series and Deriving Structure-Activity Relationships. II. Aliphatic Series Daniel Domine, James Devillers, and Maurice Chastrette pp 981 - 987; DOI: 10.1021/jm00033a016 |
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Antiinflammatory 4,5-Diarylpyrroles: Synthesis and QSAR Wendell W. Wilkerson, William Galbraith, Kathleen Gans-Brangs, Mary Grubb, Walter E. Hewes, Bruce Jaffee, J. P. Kenney, Janet Kerr, and Nancy Wong pp 988 - 998; DOI: 10.1021/jm00033a017 |
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Discovery, Synthesis, and Bioactivity of Bis(heteroaryl)piperazines. 1. A Novel Class of Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors Donna L. Romero, Raymond A. Morge, Carolyn Biles, Norman Berrios-Pena, Paul D. May, John R. Palmer, Paul D. Johnson, Herman W. Smith, Mariano Busso, and et al. pp 999 - 1014; DOI: 10.1021/jm00033a018 |
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Dianilinophthalimides: Potent and Selective, ATP-Competitive Inhibitors of the EGF-Receptor Protein Tyrosine Kinase Uwe Trinks, Elisabeth Buchdunger, Pascal Furet, Wilhelm Kump, Helmut Mett, Thomas Meyer, Marcel Mueller, Urs Regenass, Greti Rihs, and et al. pp 1015 - 1027; DOI: 10.1021/jm00033a019 |
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6H-Pyrazolo[4,5,1-de]acridin-6-ones as a Novel Class of Antitumor Agents.Synthesis and Biological Activity Toru Sugaya, Yukiteru Mimura, Yasusi Shida, Yutaka Osawa, Ikuo Matsukuma, Shunichi Ikeda, Shiro Akinaga, Makoto Morimoto, Tadashi Ashizawa, and et al. pp 1028 - 1032; DOI: 10.1021/jm00033a020 |
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Non-peptide angiotensin II receptor antagonists. 2. Design, synthesis, and biological activity of N-substituted (phenylamino)phenylacetic acids and acyl sulfonamides. [Erratum to document cited in CA120(5):45190z] Daljit S. Dhanoa, Scott W. Bagley, Raymond S. L. Chang, Victor J. Lotti, Tsing Bau Chen, Salah D. Kivlighn, Gloria J. Zingaro, Peter K. S. Siegl, Arthur A. Patchett, and William J. Greenlee pp 1034 - 1034; DOI: 10.1021/jm00033a021 |
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Structure-based design of inhibitors of purine nucleoside phosphorylase. 3. 9-Arylmethyl derivatives of 9-deazaguanine substituted on the arylmethyl group. [Erratum to document cited in CA119(25):271601v] Mark D. Erion, Shri Niwas, Jerry D. Rose, Subramaniam Ananthan, Mark Allen, John A. Secrist, III, Y. Sudhakar Babu, Charles E. Bugg, Wayne C. Guida, and et al. pp 1034 - 1034; DOI: 10.1021/jm00033a022 |
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Book Reviews pp 1033 - 1033; DOI: 10.1021/jm00033a600 |
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Application of the Three-Dimensional Structures of Protein Target Molecules in Structure-Based Drug Design Jonathan Greer, John W. Erickson, John J. Baldwin, and Michael D. Varney pp 1035 - 1054; DOI: 10.1021/jm00034a001 |
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Novel Isoxazoles which Interact with Brain Cholinergic Channel Receptors Have Intrinsic Cognitive Enhancing and Anxiolytic Activities David S. Garvey, James T. Wasicak, Michael W. Decker, Jorge D. Brioni, Michael J. Buckley, James P. Sullivan, George M. Carrera, Mark W. Holladay, Stephen P. Arneric, and Michael Williams pp 1055 - 1059; DOI: 10.1021/jm00034a002 |
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A New Arylpiperazine Antipsychotic with High D2/D3/5-HT1A/.alpha.1A-Adrenergic Affinity and a Low Potential for Extrapyramidal Effects Allen B. Reitz, Debra J. Bennett, Paul S. Blum, Ellen E. Codd, Cynthia A. Maryanoff, Marta E. Ortegon, Michael J. Renzi, Malcolm K. Scott, Richard P. Shank, and Jeffry L. Vaught pp 1060 - 1062; DOI: 10.1021/jm00034a003 |
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Design and Synthesis of RNA-Specific Groove-Binding Cations: Implications for Antiviral Drug Design Adrian W. McConnaughie, Jaroslaw Spychala, Min Zhao, David Boykin, and W. David Wilson pp 1063 - 1069; DOI: 10.1021/jm00034a004 |
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New Dual Inhibitors of Neutral Endopeptidase and Angiotensin-Converting Enzyme: Rational Design, Bioavailability, and Pharmacological Responses in Experimental Hypertension Marie-Claude Fournie-Zaluski, Pascale Coric, Serge Turcaud, Nathalie Rousselet, Walter Gonzalez, Brigitte Barbe, Isabelle Pham, Nathalie Jullian, Jean-Baptiste Michel, and Bernard P. Roques pp 1070 - 1083; DOI: 10.1021/jm00034a005 |
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Effects of L-Cysteine on the Oxidation Chemistry of Dopamine: New Reaction Pathways of Potential Relevance to Idiopathic Parkinson's Disease Fa Zhang and Glenn Dryhurst pp 1084 - 1098; DOI: 10.1021/jm00034a006 |
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Three-Dimensional Structure-Activity Analysis of a Series of Porphyrin Derivatives with Anti-HIV-1 Activity Targeted to the V3 Loop of the gp120 Envelope Glycoprotein of the Human Immunodeficiency Virus Type 1 Asim Kumar Debnath, Shibo Jiang, Nathan Strick, Kang Lin, Paul Haberfield, and A. Robert Neurath pp 1099 - 1108; DOI: 10.1021/jm00034a007 |
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Structure-Based Design of Inhibitors of Purine Nucleoside Phosphorylase. 4. A Study of Phosphate Mimics Wayne C. Guida, Robert D. Elliott, H. Jeanette Thomas, John A. Secrist, Y. Sudhakar Babu, Charles E. Bugg, Mark D. Erion, Steven E. Ealick, and John A. Montgomery pp 1109 - 1114; DOI: 10.1021/jm00034a008 |
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Synthesis and Antiestrogenic Activity of Diaryl Thioether Derivatives Donald Poirier, Serge Auger, Yves Merand, Jacques Simard, and Fernand Labrie pp 1115 - 1125; DOI: 10.1021/jm00034a009 |
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Antitumor Agents. 150. 2',3',4',5',5,6,7-Substituted 2-Phenyl-4-quinolones and Related Compounds: Their Synthesis, Cytotoxicity, and Inhibition of Tubulin Polymerization Leping Li, Hui-Kang Wang, Sheng-Chu Kuo, Tian-Shung Wu, Dan Lednicer, Chii M. Lin, Ernest Hamel, and Kuo-Hsiung Lee pp 1126 - 1135; DOI: 10.1021/jm00034a010 |
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Cyclic .beta.-Casomorphin Analogs with Mixed .mu. Agonist/.delta. Antagonist Properties: Synthesis, Pharmacological Characterization, and Conformational Aspects Ralf Schmidt, Dirk Vogel, Carmen Mrestani-Klaus, Wolfgang Brandt, Klaus Neubert, Nga N. Chung, Carole Lemieux, and Peter W. Schiller pp 1136 - 1144; DOI: 10.1021/jm00034a011 |
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Calculation of Relative Differences in the Binding Free Energies of HIV1 Protease Inhibitors: A Thermodynamic Cycle Perturbation Approach M. Rami Reddy, Michael D. Varney, Vince Kalish, Vellarkad N. Viswanadhan, and Krzysztof Appelt pp 1145 - 1152; DOI: 10.1021/jm00034a012 |
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Thiopyrano[2,3,4-cd]indoles as 5-Lipoxygenase Inhibitors: Synthesis, Biological Profile, and Resolution of 2-[2-[1-(4-Chlorobenzyl)-4-methyl-6-[(5-phenylpyridin-2-yl)methoxy]-4,5-dihydro-1H-thiopyrano[2,3,4-cd]indol-2-yl]ethoxy]butanoic Acid J. H. Hutchinson, D. Riendeau, C. Brideau, C. Chan, J.-P. Falgueyret, J. Guay, T. R. Jones, C. Lepine, D. Macdonald, and et al. pp 1153 - 1164; DOI: 10.1021/jm00034a013 |
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Antineoplastic agents. 278. Isolation and structure of axinastatins 2 and 3 from a Western Caroline Island marine sponge George R. Pettit, Feng Gao, Ronald L. Cerny, Dennis L. Doubek, Larry P. Tackett, Jean M. Schmidt, and Jean-Charles Chapuis pp 1165 - 1168; DOI: 10.1021/jm00034a014 |
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Classical and Nonclassical Furo[2,3-d]pyrimidines as Novel Antifolates: Synthesis and Biological Activities Aleem Gangjee, Rajesh Devraj, John J. McGuire, Roy L. Kisliuk, Sherry F. Queener, and Louis R. Barrows pp 1169 - 1176; DOI: 10.1021/jm00034a015 |
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The Development of Cyclic Sulfolanes as Novel and High-Affinity P2 Ligands for HIV-1 Protease Inhibitors Arun K. Ghosh, Hee Yoon Lee, Wayne J. Thompson, Chris Culberson, M. Katharine Holloway, Sean P. McKee, Peter M. Munson, Tien T. Duong, Anthony M. Smith, and et al. pp 1177 - 1188; DOI: 10.1021/jm00034a016 |
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Antiplatelet Agents Based on Cyclooxygenase Inhibition without Ulcerogenesis. Evaluation and Synthesis of 4,5-Bis(4-methoxyphenyl)-2-substituted-thiazoles Akito Tanaka, Hiroyoshi Sakai, Yukio Motoyama, Takatoshi Ishikawa, and Hisashi Takasugi pp 1189 - 1199; DOI: 10.1021/jm00034a017 |
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Dibasic (Amidinoaryl)propanoic Acid Derivatives as Novel Blood Coagulation Factor Xa Inhibitors Takayasu Nagahara, Yukio Yokoyama, Kazue Inamura, Shin-ichi Katakura, Satoshi Komoriya, Hitoshi Yamaguchi, Tsuyoshi Hara, and Masahiro Iwamoto pp 1200 - 1207; DOI: 10.1021/jm00034a018 |
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In vitro Photoinduced Cytotoxicity and DNA Binding Properties of Psoralen and Coumarin Conjugates of Netropsin Analogs: DNA Sequence-Directed Alkylation and Cross-Link Formation Moses Lee, Mary C. Roldan, Margaret K. Haskell, Simon R. McAdam, and John A. Hartley pp 1208 - 1213; DOI: 10.1021/jm00034a019 |
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Structural Features Important for .sigma.1 Receptor Binding Richard A. Glennon, Seth Y. Ablordeppey, Abd M. Ismaiel, Mahmoud B. El-Ashmawy, James B. Fischer, and Kathleen Burke Howie pp 1214 - 1219; DOI: 10.1021/jm00034a020 |
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Secondary Amine Analogs of 3.beta.-(4'-Substituted phenyl)tropane-2.beta.-carboxylic Acid Esters and N-Norcocaine Exhibit Enhanced Affinity for Serotonin and Norepinephrine Transporters John W. Boja, Michael J. Kuhar, Theresa Kopajtic, Emily Yang, Philip Abraham, Anita H. Lewin, and F. Ivy Carroll pp 1220 - 1223; DOI: 10.1021/jm00034a021 |
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Synthesis and Evaluation of 7.alpha.-Iodo-5.alpha.-dihydrotestosterone as a Potential Radioligand for Androgen Receptor Robert M. Hoyte, Kethel Borderon, Karlene Bryson, Richard Allen, Richard B. Hochberg, and Theodore J. Brown pp 1224 - 1230; DOI: 10.1021/jm00034a022 |
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Book Reviews pp 1231 - 1232; DOI: 10.1021/jm00034a600 |
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Applications of Combinatorial Technologies to Drug Discovery. 1. Background and Peptide Combinatorial Libraries Mark A. Gallop, Ronald W. Barrett, William J. Dower, Stephen P. A. Fodor, and Eric M. Gordon pp 1233 - 1251; DOI: 10.1021/jm00035a001 |
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Potent, Selective, and Systemically-Available Inhibitors of Acyl-Coenzyme A:Cholesterol Acyl Transferase (ACAT) Peter A. McCarthy, Ernest S. Hamanaka, Carol A. Marzetta, Mark J. Bamberger, B. J. Gaynor, George Chang, Sarah E. Kelly, Philip B. Inskeep, James T. Mayne, and et al. pp 1252 - 1255; DOI: 10.1021/jm00035a002 |
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Mechanism-Based Design, Synthesis, and in vitro Antimalarial Testing of New 4-Methylated Trioxanes Structurally Related to Artemisinin: The Importance of a Carbon-Centered Radical for Antimalarial Activity Gary H. Posner, Chang Ho Oh, Dasong Wang, Lucia Gerena, Wilbur K. Milhous, Steven R. Meshnick, and Wanida Asawamahasadka pp 1256 - 1258; DOI: 10.1021/jm00035a003 |
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Design of Orally Active, Non-Peptidic Inhibitors of Human Leukocyte Elastase Frederick J. Brown, Donald W. Andisik, Peter R. Bernstein, Craig B. Bryant, Chris Ceccarelli, James R. Jr. Damewood, Philip D. Edwards, Roger A. Earley, Scott Feeney, and et al. pp 1259 - 1261; DOI: 10.1021/jm00035a004 |
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Synthesis of 2.beta.-Acyl-3.beta.-aryl-8-azabicyclo[3.2.1]octanes and Their Binding Affinities at Dopamine and Serotonin Transport Sites in Rat Striatum and Frontal Cortex Huw M. L. Davies, Elie Saikali, Nicholas J. S. Huby, Vernon J. Gilliatt, Julius J. Matasi, Tammy Sexton, and Steven R. Childers pp 1262 - 1268; DOI: 10.1021/jm00035a005 |
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Identification of L-Tryptophan Derivatives with Potent and Selective Antagonist Activity at the NK1 Receptor Angus M. MacLeod, Kevin J. Merchant, Frederick Brookfield, Fintan Kelleher, Graeme Stevenson, Andrew P. Owens, Christopher J. Swain, Margaret A. Cascieri, Sharon Sadowski, and et al. pp 1269 - 1274; DOI: 10.1021/jm00035a006 |
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Aromatase Inhibitors. Syntheses and Structure-Activity Studies of Novel Pyridyl-Substituted Indanones, Indans, and Tetralins Rolf W. Hartmann, Herbert Bayer, and Gertrud Gruen pp 1275 - 1281; DOI: 10.1021/jm00035a007 |
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Synthesis, Structure-Activity Relationships, and Pharmacological Evaluation of a Series of Fluorinated 3-Benzyl-5-Indolecarboxamides: Identification of 4-[[5-[((2R)-2-Methyl-4,4,4-trifluorobutyl)carbamoyl]-1-methylindol-3-yl]methyl]-3methoxy-N-[(2-methylphenyl)sulfonyl]benzamide, a Potent, Orally Active Antagonist of Leukotrienes D4 and E4 Robert T. Jacobs, Peter R. Bernstein, Laura A. Cronk, Edward P. Vacek, Lisa F. Newcomb, David Aharony, Carl K. Buckner, and Edward J. Kusner pp 1282 - 1297; DOI: 10.1021/jm00035a008 |
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Mechanism-Based Isocoumarin Inhibitors for Blood Coagulation Serine Proteases. Effect of the 7-Substituent in 7-Amino-4-chloro-3-(isothioureidoalkoxy)isocoumarins on Inhibitory and Anticoagulant Potency Chih-Min Kam, John E. Kerrigan, R. Richard Plaskon, Edward J. Duffy, Pete Lollar, F. L. Suddath, and James C. Powers pp 1298 - 1306; DOI: 10.1021/jm00035a009 |
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Synthesis and Antiviral Activities of 8-Alkynyl-, 8-Alkenyl-, and 8-Alkyl-2'-deoxyadenosine Analogs Gyula Sagi, Laszlo Otvos, Satoru Ikeda, Graciela Andrei, Robert Snoeck, and Erik De Clercq pp 1307 - 1311; DOI: 10.1021/jm00035a010 |
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6-Alkyl- and 6-Arylandrost-4-ene-3,17-diones as Aromatase Inhibitors. Synthesis and Structure-Activity Relationships Mitsuteru Numazawa and Mariko Oshibe pp 1312 - 1319; DOI: 10.1021/jm00035a011 |
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Synthesis of 2-Piperazinylbenzothiazole and 2-Piperazinylbenzoxazole Derivatives with 5-HT3 Antagonist and 5-HT4 Agonist Properties Antonio Monge, Maria del Carmen Pena, Juan Antonio Palop, Jose Maria Caldero, Juan Roca, Elisa Garcia, Gonzalo Romero, Joaquin del Rio, and Berta Lasheras pp 1320 - 1325; DOI: 10.1021/jm00035a012 |
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Protein Kinase C. Modeling of the Binding Site and Prediction of Binding Constants Shaomeng Wang, George W. A. Milne, Marc C. Nicklaus, Victor E. Marquez, Jeewoo Lee, and Peter M. Blumberg pp 1326 - 1338; DOI: 10.1021/jm00035a013 |
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Investigation of the Active Site of Aminopeptidase A Using a Series of New Thiol-Containing Inhibitors Eric N. Chauvel, Pascale Coric, Catherine Llorens-Cortes, Sherwin Wilk, Bernard P. Roques, and Marie-Claude Fournie-Zaluski pp 1339 - 1346; DOI: 10.1021/jm00035a014 |
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A Proposed Model of Bradykinin Bound to the Rat B2 Receptor and Its Utility for Drug Design Donald J. Kyle, Sarvajit Chakravarty, Jacqueline A. Sinsko, and Thomas M. Stormann pp 1347 - 1354; DOI: 10.1021/jm00035a015 |
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Molecular Requirements for the Inhibition of the Tetracycline Antiport Protein and the Effect of Potent Inhibitors on the Growth of Tetracycline-Resistant Bacteria Mark L. Nelson, Britt H. Park, and Stuart B. Levy pp 1355 - 1361; DOI: 10.1021/jm00035a016 |
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The Effect of Fluorine Substitution on the Metabolism and Antimalarial Activity of Amodiaquine Paul M. O'Neill, Anthony C. Harrison, Richard C. Storr, Shaun R. Hawley, Stephen A. Ward, and B. Kevin Park pp 1362 - 1370; DOI: 10.1021/jm00035a017 |
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An Enantiospecific Synthesis of the Human Cytomegalovirus Antiviral Agent [(R)-3-((2-Amino-1,6-dihydro-6-oxo-9H-purin-9-yl)methoxy)-4- hydroxybutyl]phosphonic Acid Stanley D. Chamberlain, Karen K. Biron, Ronna E. Dornsife, Devron R. Averett, Lilia Beauchamp, and George W. Koszalka pp 1371 - 1377; DOI: 10.1021/jm00035a018 |
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Synthesis and Anticholinergic Activity of the Four Stereoisomers of 4-(Dimethylamino)-2-phenyl-2-(2-pyridyl)pentanamide Hitoshi Oyasu, Masanobu Nagano, Atsushi Akahane, Masaaki Tomoi, Toshiji Tada, and Masaaki Matsuo pp 1378 - 1381; DOI: 10.1021/jm00035a019 |
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An Epimer of 5'-Noraristeromycin and Its Antiviral Properties Suhaib M. Siddiqi, Xing Chen, Stewart W. Schneller, Satoru Ikeda, Robert Snoeck, Graciela Andrei, Jan Balzarini, and Erik De Clercq pp 1382 - 1384; DOI: 10.1021/jm00035a020 |
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Applications of Combinatorial Technologies to Drug Discovery. 2. Combinatorial Organic Synthesis, Library Screening Strategies, and Future Directions Eric M. Gordon, Ronald W. Barrett, William J. Dower, Stephen P. A. Fodor, and Mark A. Gallop pp 1385 - 1401; DOI: 10.1021/jm00036a001 |
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3'-(Arylmethyl)- and 3'-(Aryloxy)-3-phenyl-4-hydroxyquinolin- 2(1H)-ones: Orally Active Antagonists of the Glycine Site on the NMDA Receptor Janusz J. Kulagowski, Raymond Baker, Neil R. Curtis, Ian M. Mawer, Angela M. Moseley, Mark P. Ridgill, Michael Rowley, Ian Stansfield, Paul D. Leeson, and et al. pp 1402 - 1405; DOI: 10.1021/jm00036a002 |
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Synthesis And Evaluation of 4-(2'-Methoxyphenyl)-1-[2'-[N-(2''-pyridinyl)- p-iodobenzamido]ethyl]piperazine (p-MPPI): A New Iodinated 5-HT1A Ligand Zhi-Ping Zhuang, Mei-Ping Kung, and Hank F. Kung pp 1406 - 1407; DOI: 10.1021/jm00036a003 |
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Structure-Activity Relationships of New Taxoids Derived from 14.beta.-Hydroxy-10-deacetylbaccatin III Iwao Ojima, Young Hoon Park, Chung-Ming Sun, Ivana Fenoglio, Giovanni Appendino, Paula Pera, and Ralph J. Bernacki pp 1408 - 1410; DOI: 10.1021/jm00036a004 |
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The Desferrithiocin Pharmacophore Raymond J. Bergeron, Charles Z. Liu, James S. McManis, Michael X. B. Xia, Samuel E. Algee, and Jan Wiegand pp 1411 - 1417; DOI: 10.1021/jm00036a005 |
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Conformational Analysis of the Prototype Nonclassical Cannabinoid CP-47,497, Using 2D NMR and Computer Molecular Modeling Xiang-Qun Xie, De-Ping Yang, Lawrence S. Melvin, and Alexandros Makriyannis pp 1418 - 1426; DOI: 10.1021/jm00036a006 |
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Novel Ligands Specific for Mitochondrial Benzodiazepine Receptors: 6-arylpyrrolo[2,1-d][1,5]benzothiazepine Derivatives. Synthesis, Structure-Activity Relationships, and Molecular Modeling Studies Isabella Fiorini, Vito Nacci, Silvia Maria Ciani, Antonio Garofalo, Giuseppe Campiani, Luisa Savini, Ettore Novellino, Gianni Greco, Paola Bernasconi, and Tiziana Mennini pp 1427 - 1438; DOI: 10.1021/jm00036a007 |
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Search for the Pharmacophore of Bispyridinium-Type Allosteric Modulators of Muscarinic Receptors Mario H. Botero Cid, Ulrike Holzgrabe, Evi Kostenis, Klaus Mohr, and Christian Traenkle pp 1439 - 1445; DOI: 10.1021/jm00036a008 |
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Characterization of Two Taxol Photoaffinity Analogs Bearing Azide and Benzophenone-Related Photoreactive Substituents in the A-Ring Side Chain Charles S. Swindell, Julia M. Heerding, Nancy E. Krauss, Susan Band Horwitz, Srinivasa Rao, and Israel Ringel pp 1446 - 1449; DOI: 10.1021/jm00036a009 |
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Conformationally Restricted Competitive Antagonists of Human/Rat Corticotropin-Releasing Factor Antonio Miranda, Steven C. Koerber, Jozsef Gulyas, Sabine L. Lahrichi, A. Grey Craig, Anne Corrigan, Arnold Hagler, Catherine Rivier, Wylie Vale, and Jean Rivier pp 1450 - 1459; DOI: 10.1021/jm00036a010 |
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Antitumor Agents. 152. In vitro Inhibitory Activity of Etoposide Derivative NPF Against Human Tumor Cell Lines and a Study of Its Conformation by X-ray Crystallography, Molecular Modeling, and NMR Spectroscopy Yi-Lin Zhang, Alexander Tropsha, Andrew T. McPhail, and Kuo-Hsiung Lee pp 1460 - 1464; DOI: 10.1021/jm00036a011 |
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Plant Antitumor Agents. 31.1 The Calycopterones, a New Class of Biflavonoids with Novel Cytotoxicity in a Diverse Panel of Human Tumor Cell Lines Monroe E. Wall, Mansukh C. Wani, Fekadu Fullas, John B. Oswald, Dan M. Brown, Thawatchai Santisuk, Vichai Reutrakul, Andrew T. McPhail, Norman R. Farnsworth, and et al. pp 1465 - 1470; DOI: 10.1021/jm00036a012 |
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Synthesis and Antitumor Activity of a Series of [2-Substituted-4,5-bis(aminomethyl)-1,3-Dioxolane]platinum(II) Complexes Dae-Kee Kim, Ganghyeok Kim, Jongsik Gam, Yong-Baik Cho, Hun-Taek Kim, Joo-Ho Tai, Key H. Kim, Weon-Seon Hong, and Jae-Gahb Park pp 1471 - 1485; DOI: 10.1021/jm00036a013 |
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Synthesis and in vitro Evaluation of 9-Anilino-3,6-diaminoacridines Active Against a Multidrug-Resistant Strain of the Malaria Parasite Plasmodium falciparum Swarna A. Gamage, Nisana Tepsiri, Prapon Wilairat, Stanley J. Wojcik, David P. Figgitt, Raymond K. Ralph, and William A. Denny pp 1486 - 1494; DOI: 10.1021/jm00036a014 |
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Structure-Activity Relationship of N17'-Substituted Norbinaltorphimine Congeners. Role of the N17' Basic Group in the Interaction with a Putative Address Subsite on the .kappa. Opioid Receptor P. S. Portoghese, C.-E. Lin, F. Farouz-Grant, and A. E. Takemori pp 1495 - 1500; DOI: 10.1021/jm00036a015 |
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Glutathione-S-transferase Activates Novel Alkylating Agents Matthew H. Lyttle, Apparao Satyam, Michael D. Hocker, Karin E. Bauer, Colby G. Caldwell, Hon C. Hui, Amy S. Morgan, Alemayehu Mergia, and Lawrence M. Kauvar pp 1501 - 1507; DOI: 10.1021/jm00036a016 |
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Retinobenzoic Acids. 6. Retinoid Antagonists with a Heterocyclic Ring Laurence Eyrolles, Hiroyuki Kagechika, Emiko Kawachi, Hiroshi Fukasawa, Tohru Iijima, Youko Matsushima, Yuichi Hashimoto, and Koichi Shudo pp 1508 - 1517; DOI: 10.1021/jm00036a017 |
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The [(Methyloxy)imino]methyl Moiety as a Bioisoster of Aryl. A Novel Class of Completely Aliphatic .beta.-Adrenergic Receptor Antagonists Bruno Macchia, Aldo Balsamo, M. C. Breschi, Grazia Chiellini, Marco Macchia, Adriano Martinelli, Claudia Martini, Claudia Nardini, Susanna Nencetti, and et al. pp 1518 - 1525; DOI: 10.1021/jm00036a018 |
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Synthesis and Structure-Activity Relationships of Deazaxanthines: Analogs of Potent A1- and A2-Adenosine Receptor Antagonists Bettina Grahner, Susanne Winiwarter, Wolfgang Lanzner, and Christa E. Mueller pp 1526 - 1534; DOI: 10.1021/jm00036a019 |
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Synthesis and Characterization of Radioiodinated N-(3-Iodopropen-1-yl)-2.beta.-carbomethoxy-3.beta.-(4-chlorophenyl)tropanes: Potential Dopamine Reuptake Site Imaging Agents Mark M. Goodman, Mei-Ping Kung, George W. Kabalka, Hank F. Kung, and Robert Switzer pp 1535 - 1542; DOI: 10.1021/jm00036a020 |
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Matrix metalloproteinase inhibitors containing a [(carboxyalkyl)amino] zinc ligand: Modification of the P1 and P2' residues. [Erratum to document cited in CA120:238898] Frank K. Brown, Peter J. Brown, D. Mark Bickett, C. Lynn Chambers, H. Geoff Davies, David N. Deaton, David Drewry, Michael Foley, Andrew B. McElroy, and et al. pp 1546 - 1546; DOI: 10.1021/jm00036a021 |
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Book Reviews pp 1543 - 1545; DOI: 10.1021/jm00036a600 |
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2-(3,4-Dichlorophenyl)-N-methyl-N-[(1S)-1-(3-isothiocyanatophenyl)-2-(1- pyrrolidinyl)ethyl]acetamide: An Opioid Receptor Affinity Label That Produces Selective and Long-Lasting .kappa. Antagonism in Mice An-Chih Chang, Akira E. Takemori, and Philip S. Portoghese pp 1547 - 1549; DOI: 10.1021/jm00037a001 |
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3-[4-(1,2-Diphenylbut-1-enyl)phenyl]acrylic Acid: A Non-Steroidal Estrogen with Functional Selectivity for Bone over Uterus in Rats Timothy M. Willson, Brad R. Henke, Tanya M. Momtahen, Paul S. Charifson, Kenneth W. Batchelor, Dennis B. Lubahn, Linda B. Moore, Beverly B. Oliver, Howard R. Sauls, and et al. pp 1550 - 1552; DOI: 10.1021/jm00037a002 |
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1,3-Diarylindan-2-carboxylic Acids, Potent and Selective Non-Peptide Endothelin Receptor Antagonists John D. Elliott, M. Amparo Lago, Russell D. Cousins, Aiming Gao, Jack D. Leber, Karl F. Erhard, Ponnal Nambi, Nabil A. Elshourbagy, Chandrika Kumar, and et al. pp 1553 - 1557; DOI: 10.1021/jm00037a003 |
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N-.omega.-Fluoroalkyl Analogs of (1R)-2.beta.-Carbomethoxy-3.beta.-(4-iodophenyl)tropane (.beta.-CIT): Radiotracers for Positron Emission Tomography and Single Photon Emission Computed Tomography Imaging of Dopamine Transporters John L. Neumeyer, Alexander Campbell, Shaoyin Wang, Yigong Gao, Richard A. Milius, Nora S. Kula, Ross J. Baldessarini, Yolanda Zea-Ponce, Ronald M. Baldwin, and Robert B. Innis pp 1558 - 1561; DOI: 10.1021/jm00037a004 |
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Novel Asp32-Replacement Tetrapeptide Analogs as Potent and Selective CCK-A Agonists Richard L. Elliott, Hana Kopecka, Michael D. Tufano, Youe-Kong Shue, Andre J. Gauri, Chun-Wel Lin, Bruce R. Bianchi, Thomas R. Miller, David G. Witte, and et al. pp 1562 - 1568; DOI: 10.1021/jm00037a005 |
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CCK-A-Selective Tetrapeptides Containing Lys(N.epsilon.)-Amide Residues: Favorable in vivo and in vitro Effects of N-Methylation at the Aspartyl Residue Michael J. Bennett, A. L. Nikkel, Bruce R. Bianchi, Thomas R. Miller, Lisa Bednarz, David G. Witte, Michael Stashko, Song Shung Wang, Paul A. Gore, and et al. pp 1569 - 1571; DOI: 10.1021/jm00037a006 |
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[L-Ala3]DPDPE: A New Enkephalin Analog with a Unique Opioid Receptor Activity Profile. Further Evidence of .delta.-Opioid Receptor Multiplicity Ronald C. Haaseth, Peter J. Horan, Edward J. Bilsky, Peg Davis, Teresa Zalewska, Jirina Slaninova, Henry I. Yamamura, Steven J. Weber, Thomas P. Davis, and et al. pp 1572 - 1577; DOI: 10.1021/jm00037a007 |
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14.alpha.,14'.beta.-[Dithiobis[(2-oxo-2,1-ethanediyl)imino]]bis(7,8-dihydromorphinone) and 14.alpha.,14'.beta.-[Dithiobis[(2-oxo-2,1-ethanediyl)imino]]bis-7,8-dihydro-N-(cyclopropyl- methyl)normorphinone: Chemistry and Opioid Binding Properties Sydney Archer, Ahmad Seyed-Mozaffari, Qi Jiang, and Jean M. Bidlack pp 1578 - 1585; DOI: 10.1021/jm00037a008 |
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Design and Synthesis of Side-Chain Conformationally Restricted Phenylalanines and Their Use for Structure-Activity Studies on Tachykinin NK-1 Receptor Hubert Josien, Solange Lavielle, Alie Brunissen, Monique Saffroy, Yvette Torrens, Jean-Claude Beaujouan, Jacques Glowinski, and Gerard Chassaing pp 1586 - 1601; DOI: 10.1021/jm00037a009 |
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DNA Sequence-Specific Reading by Echinomycin: Role of Hydrogen Bonding and Stacking Interactions Jose Gallego, F. J. Luque, Modesto Orozco, Carolina Burgos, Julio Alvarez-Builla, M. Melia Rodrigo, and Federico Gago pp 1602 - 1609; DOI: 10.1021/jm00037a010 |
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Nitrobenzyl Phosphorodiamidates as Potential Hypoxia-Selective Alkylating Agents R. Timothy Mulcahy, Jerry J. Gipp, James P. Schmidt, Carolyn Joswig, and Richard F. Borch pp 1610 - 1615; DOI: 10.1021/jm00037a011 |
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Synthesis and Antitumor Activities of Novel 6-5 Fused Ring Heterocycle Antifolates: N-[4-[.omega.-(2-Amino-4-substituted-6,7-dihydrocyclopenta[d]pyrimidin-5-yl)alkyl]benzoyl]-L-glutamic Acids Yoshihiko Kotake, Atsumi Iijima, Kentaro Yoshimatsu, Naoko Tamai, Yoichi Ozawa, Nozomu Koyanagi, Kyosuke Kitoh, and Hiroaki Nomura pp 1616 - 1624; DOI: 10.1021/jm00037a012 |
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A Comparison of the Cytotoxic and Physical Properties of Aziridinyl Quinone Derivatives Based on the Pyrrolo[1,2-a]benzimidazole and Pyrrolo[1,2-a]indole Ring Systems Romesh C. Boruah and Edward B. Skibo pp 1625 - 1631; DOI: 10.1021/jm00037a013 |
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Non-Peptide Angiotensin II Receptor Antagonists: Synthesis and Biological Activity of a Series of Novel 4,5-Dihydro-4-oxo-3H-imidazo[4,5-c]pyridine Derivatives Werner W. K. R. Mederski, Dieter Dorsch, Heinz-Hermann Bokel, Norbert Beier, Ingeborg Lues, and Pierre Schelling pp 1632 - 1645; DOI: 10.1021/jm00037a014 |
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Synthesis and Carbonic Anhydrase Inhibitory Activity of 4-Substituted 2-Thiophenesulfonamides Judy M. Holmes, Gary C. M. Lee, Mercy Wijono, Robert Weinkam, Larry A. Wheeler, and Michael E. Garst pp 1646 - 1651; DOI: 10.1021/jm00037a015 |
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Inhibitors of Acyl-CoA:Cholesterol Acyltransferase (ACAT). 7. Development of a Series of Substituted N-Phenyl-N'-[(1-phenylcyclopentyl)methyl]ureas with Enhanced Hypocholesterolemic Activity Bharat K. Trivedi, Terri Stoeber Purchase, Ann Holmes, Corinne E. Augelli-Szafran, Arnold D. Essenburg, Katherine L. Hamelehle, Richard L. Stanfield, Richard F. Bousley, and Brian R. Krause pp 1652 - 1659; DOI: 10.1021/jm00037a016 |
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Antipsoriatic Anthrones with Modulated Redox Properties. 2. Novel Derivatives of Chrysarobin and Isochrysarobin-Antiproliferative Activity and 5-Lipoxygenase Inhibition Klaus Mueller, Peter Leukel, Klaus Ziereis, and Ingo Gawlik pp 1660 - 1669; DOI: 10.1021/jm00037a017 |
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Molecular Structures and Conformational Studies of Triarylcyclopropyl and Related Nonsteroidal Anti-Estrogens M. Bilayet Hossain, Dick van der Helm, Francis J. Schmitz, Eva O. Pordesimo, Robert A. Magarian, Karen L. Meyer, Lynette B. Overacre, and Billy W. Day pp 1670 - 1683; DOI: 10.1021/jm00037a018 |
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C-Glycosyl Bond Conformation in Oxazofurin: Crystallographic and Computational Studies of the Oxazole Analog of Tiazofurin Barry M. Goldstein, Hong Li, Wendy H. Hallows, David A. Langs, Palmarisa Franchetti, Loredana Cappellacci, and Mario Grifantini pp 1684 - 1688; DOI: 10.1021/jm00037a019 |
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Structural Studies on Bioactive Compounds. 23. Synthesis of Polyhydroxylated 2-Phenylbenzothiazoles and a Comparison of their Cytotoxicities and Pharmacological Properties with Genistein and Quercetin Malcolm F. G. Stevens, Carol J. McCall, Peter Lelievald, Peter Alexander, Audrey Richter, and Donna E. Davies pp 1689 - 1695; DOI: 10.1021/jm00037a020 |
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Selective Type IV Phosphodiesterase Inhibitors as Antiasthmatic Agents. The Syntheses and Biological Activities of 3-(Cyclopentyloxy)-4-methoxybenzamides and Analogs Michael J. Ashton, David C. Cook, Garry Fenton, Jan-Anders Karlsson, Malcolm N. Palfreyman, David Raeburn, Andrew J. Ratcliffe, John E. Souness, Suga Thurairatnam, and Nigel Vicker pp 1696 - 1703; DOI: 10.1021/jm00037a021 |
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Presynaptic Cholinergic Modulators as Potent Cognition Enhancers and Analgesic Drugs. 1. Tropic and 2-Phenylpropionic Acid Esters Fulvio Gualtieri, Gabriele Conti, Silvia Dei, Maria Paola Giovannoni, Francesca Nannucci, Maria Novella Romanelli, Serena Scapecchi, Elisabetta Teodori, Luisa Fanfani, Carla Ghelardini, Alberto Giotti, and Alessandro Bartolini pp 1704 - 1711; DOI: 10.1021/jm00037a022 |
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Presynaptic Cholinergic Modulators as Potent Cognition Enhancers and Analgesic Drugs. 2. 2-Phenoxy-, 2-(Phenylthio)-, and 2-(Phenylamino)alkanoic Acid Esters Fulvio Gualtieri, Claudia Bottalico, Anna Calandrella, Silvia Dei, Maria Paola Giovannoni, Stefania Mealli, Maria Novella Romanelli, Serena Scapecchi, Elisabetta Teodori, and et al. pp 1712 - 1719; DOI: 10.1021/jm00037a023 |
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2-Alkynyl Derivatives of Adenosine-5'-N-ethyluronamide: Selective A2 Adenosine Receptor Agonists with Potent Inhibitory Activity on Platelet Aggregation Gloria Cristalli, Rosaria Volpini, Sauro Vittori, Emidio Camaioni, Angela Monopoli, Annamaria Conti, Silvio Dionisotti, Cristina Zocchi, and Ennio Ongini pp 1720 - 1726; DOI: 10.1021/jm00037a024 |
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Molecular Similarity, Quantitative Chirality, and QSAR for Chiral Drugs Alon Seri-Levy, Susan West, and W. Graham Richards pp 1727 - 1732; DOI: 10.1021/jm00037a025 |
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2-Azetidinones as Inhibitors of Cholesterol Absorption Duane A. Burnett, Mary Ann Caplen, Harry R. Davis, Robert E. Burrier, and John W. Clader pp 1733 - 1736; DOI: 10.1021/jm00038a001 |
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Synthesis and Characterization of [125I]-N-(N-Benzylpiperidin-4-yl)-4-iodobenzamide, a New .sigma. Receptor Radiopharmaceutical: High-Affinity Binding to MCF-7 Breast Tumor Cells Christy S. John, Bertold J. Vilner, and Wayne D. Bowen pp 1737 - 1739; DOI: 10.1021/jm00038a002 |
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Anti-HIV Michellamines from Ancistrocladus korupensis Michael R. Boyd, Yali F. Hallock, John H. Cardellina II, Kirk P. Manfredi, John W. Blunt, James B. McMahon, Robert W. Buckheit Jr., Gerhard Bringmann, Manuela Schaeffer, and et al. pp 1740 - 1745; DOI: 10.1021/jm00038a003 |
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Newly discovered stereochemical requirements in the side-chain conformation of .delta. opioid agonists for recognizing opioid .delta. receptors Xinhua Qian, Katalin E. Koever, Mark D. Shenderovich, Bih-Show Lou, Aleksandra Misicka, Teresa Zalewska, Robert Horvath, Peg Davis, E. J. Bilsky, and et al. pp 1746 - 1757; DOI: 10.1021/jm00038a004 |
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Amino Diol HIV Protease Inhibitors. 1. Design, Synthesis, and Preliminary SAR Joel C. Barrish, Eric Gordon, Masud Alam, Pin-Fang Lin, Gregory S. Bisacchi, Ping Chen, Peter T. W. Cheng, Alan W. Fritz, Jill A. Greytok, and et al. pp 1758 - 1768; DOI: 10.1021/jm00038a005 |
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Pharmacophores from Binding Data Arthur M. Doweyko pp 1769 - 1778; DOI: 10.1021/jm00038a006 |
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3,4-Dihydro-3-amino-2H-1-benzopyran Derivatives as 5-HT1A Receptor Ligands and Potential Anxiolytic Agents. 1. Synthesis and Structure-Activity Relationship Studies Tchao Podona, Beatrice Guardiola-Lemaitre, Daniel-Henri Caignard, Gerard Adam, Bruno Pfeiffer, Pierre Renard, and Gerald Guillaumet pp 1779 - 1793; DOI: 10.1021/jm00038a007 |
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Synthesis and Antitumor Activity of Novel Mitomycin Derivatives Containing Functional Groups at the C-6-Methyl Position Hitoshi Arai, Yutaka Kanda, Tadashi Ashizawa, Makoto Morimoto, Katsushige Gomi, Motomichi Kono, and Masaji Kasai pp 1794 - 1804; DOI: 10.1021/jm00038a008 |
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Synthesis and Antitumor Activity of Novel 6-Alkyl-6-demethylmitomycins Hitoshi Arai, Yutaka Kanda, Tadashi Ashizawa, Makoto Morimoto, Katsushige Gomi, Motomichi Kono, and Masaji Kasai pp 1805 - 1809; DOI: 10.1021/jm00038a009 |
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Inhibitors of Acyl-CoA:Cholesterol O-Acyl Transferase (ACAT) as Hypocholesterolemic Agents. 8. Incorporation of Amide or Amine Functionalities into a Series of Disubstituted Ureas and Carbamates. Effects on ACAT Inhibition in vitro and Efficacy in vivo Patrick M. O'Brien, Drago R. Sliskovic, C. John Blankley, Bruce. D Roth, Michael W. Wilson, Katherine L. Hamelehle, Brian R. Krause, and Richard L. Stanfield pp 1810 - 1822; DOI: 10.1021/jm00038a010 |
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Dual Angiotensin Converting Enzyme/Thromboxane Synthase Inhibitors Gary M. Ksander, Mark Erion, Andrew M. Yuan, Clive G. Diefenbacher, Lena El-Chehabi, Don Cote, and Nigel Levens pp 1823 - 1832; DOI: 10.1021/jm00038a011 |
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In vivo Inhibition of Cathepsin B by Peptidyl (Acyloxy)methyl Ketones Bonnie M. Wagner, Roger A. Smith, Peter J. Coles, Leslie J. Copp, Michael J. Ernest, and Allen Krantz pp 1833 - 1840; DOI: 10.1021/jm00038a012 |
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A New Series of Photoactivatable and Iodinatable Linear Vasopressin Antagonists Eric Carnazzi, Andre Aumelas, Claude Barberis, Gilles Guillon, and Rene Seyer pp 1841 - 1849; DOI: 10.1021/jm00038a013 |
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Synthetic Macromolecular Inhibitors of Human Leukocyte Elastase. 1. Synthesis of Peptidyl Carbamates Bound to Water-Soluble Polymers: Poly-.alpha.,.beta.-[N-(2-hydroxyethyl)-D,L-aspartamide] and Poly-.alpha.-[N5-(2-hydroxyethyl)-L-glutamine] Frantisek Rypacek, William R. Banks, Dagmar Noskova, and George A. Digenis pp 1850 - 1856; DOI: 10.1021/jm00038a014 |
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Synthesis, Oral Bioavailability Determination, and in vitro Evaluation of Prodrugs of the Antiviral Agent 9-[2-(Phosphonomethoxy)ethyl]adenine (PMEA) John E. Jr. Starrett, David R. Tortolani, John Russell, Michael J. M. Hitchcock, Valerie Whiterock, John C. Martin, and Muzammil M. Mansuri pp 1857 - 1864; DOI: 10.1021/jm00038a015 |
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New Thiol Inhibitors of Neutral Endopeptidase EC 3.4.24.11: Synthesis and Enzyme Active-Site Recognition Isabel Gomez-Monterrey, Ann Beaumont, Patrick Nemecek, Bernard P. Roques, and Marie-Claude Fournie-Zaluski pp 1865 - 1873; DOI: 10.1021/jm00038a016 |
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Synthesis and Biological Activities of a New Set of Irreversibly Acting 2-(4'-Isothiocyanatobenzyl)imidazoline Analogs in Rat Thoracic Aorta Meri Slavica, Longping Lei, Popat N. Patil, Alex Kerezy, Dennis R. Feller, and Duane D. Miller pp 1874 - 1881; DOI: 10.1021/jm00038a017 |
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N-Benzylnaltrindoles as Long-Acting .delta.-Opioid Receptor Antagonists V. L. Korlipara, A. E. Takemori, and P. S. Portoghese pp 1882 - 1885; DOI: 10.1021/jm00038a018 |
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Synthesis and .delta.-Opioid Receptor Antagonist Activity of a Naltrindole Analog with a Regioisomeric Indole Moiety P. S. Portoghese, S. Ohkawa, S. T. Moe, and A. E. Takemori pp 1886 - 1888; DOI: 10.1021/jm00038a019 |
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(R)-Methanandamide: A Chiral Novel Anandamide Possessing Higher Potency and Metabolic Stability Vasiliki Abadji, Sonyuan Lin, Gihan Taha, Graeme Griffin, Lesley A. Stevenson, Roger G. Pertwee, and Alexandros Makriyannis pp 1889 - 1893; DOI: 10.1021/jm00038a020 |
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(6,7-Diaryldihydropyrrolizin-5-yl)acetic Acids, a Novel Class of Potent Dual Inhibitors of Both Cyclooxygenase and 5-Lipoxygenase Stefan A. Laufer, Jan Augustin, Gerd Dannhardt, and Werner Kiefer pp 1894 - 1897; DOI: 10.1021/jm00038a021 |
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Additions and Corrections - Three-Dimensional Structure-Activity Analysis of a Series of Porphyrin Derivatives with Anti-HIV-1 Activity Targeted to the V3 Loop of the gp120 Envelope Glycoprotein of the Human Immunodeficiency Virus Type 1. Asim Kumar Debnath, Shibo Jiang, Nathan Strick, Kang Lin, Paul Haberfield, and A. Robert Neurath pp 1898 - 1898; DOI: 10.1021/jm00038a600 |
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Approaches toward Selective Inhibition of Nitric Oxide Synthase Michael A. Marletta pp 1899 - 1907; DOI: 10.1021/jm00039a001 |
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Derivatives of a Novel Cyclopeptolide. 1. Synthesis, Antifungal Activity, and Structure-Activity Relationships Gerhard Emmer, Maximilian A. Grassberger, Josef G. Meingassner, Gerhard Schulz, and Michael Schaude pp 1908 - 1917; DOI: 10.1021/jm00039a002 |
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Derivatives of a Novel Cyclopeptolide. 2. Synthesis, Activity against Multidrug Resistance in CHO and KB Cells in vitro, and Structure-Activity Relationships Gerhard Emmer, Maximilian A. Grassberger, Gerhard Schulz, Danielle Boesch, Claire Gaveriaux, and Francis Loor pp 1918 - 1928; DOI: 10.1021/jm00039a003 |
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Influence of Amine Substituents on 5-HT2A versus 5-HT2C Binding of Phenylalkyl- and Indolylalkylamines Richard A. Glennon, Malgorzata Dukat, Mohamed El-Bermawy, Ho Law, Joseph De Los Angeles, Milt Teitler, Allison King, and Katharine Herrick-Davis pp 1929 - 1935; DOI: 10.1021/jm00039a004 |
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Organometallic Anticancer Agents: The Effect of the Central Metal and Halide Ligands on the Interaction of Metallocene Dihalides Cp2MX2 with Nucleic Acid Constituents Joanne H. Murray and Margaret M. Harding pp 1936 - 1941; DOI: 10.1021/jm00039a005 |
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The Discovery of Capsazepine, the First Competitive Antagonist of the Sensory Neuron Excitants Capsaicin and Resiniferatoxin Christopher S. J. Walpole, Stuart Bevan, Guenter Bovermann, Johann J. Boelsterli, Robin Breckenridge, John W. Davies, Glyn A. Hughes, Iain James, Lukas Oberer, and et al. pp 1942 - 1954; DOI: 10.1021/jm00039a006 |
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Design, Synthesis, and Study of 9-Substituted Ellipticine and 2-Methylellipticinium Analogs as Potential CNS-Selective Antitumor Agents Wayne K. Anderson, Ariamala Gopalsamy, and Peech S. Reddy pp 1955 - 1963; DOI: 10.1021/jm00039a007 |
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Novel (4-Phenylpiperidinyl)- and (4-Phenylpiperazinyl)alkyl-Spaced Esters of 1-Phenylcyclopentanecarboxylic Acids as Potent .sigma.-Selective Compounds Robert L. Hudkins, Richard B. Mailman, and Diane L. DeHaven-Hudkins pp 1964 - 1970; DOI: 10.1021/jm00039a008 |
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Asimin, Asiminacin, and Asiminecin: Novel Highly Cytotoxic Asimicin Isomers from Asimina triloba Geng-Xian Zhao, Laura R. Miesbauer, David L. Smith, and Jerry L. McLaughlin pp 1971 - 1976; DOI: 10.1021/jm00039a009 |
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Synthesis and Topical Antiinflammatory and Antiallergic Activities of Antioxidant o-Aminophenol Derivatives Naoki Sugiyama, Fumihiko Akahoshi, Shigeki Kuwahara, Masahiko Kajii, Yoshiko Sakaue, Haruko Yakumaru, Masanori Sugiura, and Chikara Fukaya pp 1977 - 1982; DOI: 10.1021/jm00039a010 |
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Novel Potassium-Channel Openers: Preparation and Pharmacological Evaluation of Racemic and Optically Active N-(6-Amino-3-pyridyl)-N'-bicycloalkyl-N''-cyanoguanidine Derivatives Masahiro Eda, Tadahiro Takemoto, S. Ono, Takehiro Okada, Keigo Kosaka, Maki Gohda, Sumio Matzno, Norifumi Nakamura, and Chikara Fukaya pp 1983 - 1990; DOI: 10.1021/jm00039a011 |
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Synthesis and Characterization of Selective Fluorescent Ligands for the neurokinin NK2 Receptor Charles G. Bradshaw, Karin Ceszkowski, Gerardo Turcatti, Isabel J. M. Beresford, and Andre Chollet pp 1991 - 1995; DOI: 10.1021/jm00039a012 |
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Syntheses and Anticholinesterase Activity of Tetrahydrobenzazepine Carbamates Yuhpyng L. Chen, Dane Liston, Jann Nielsen, Douglas Chapin, Audrey Dunaiskis, Kirk Hedberg, Jeffery Ives, Jonathan Jr. Johnson, and Shawn Jones pp 1996 - 2000; DOI: 10.1021/jm00039a013 |
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The Discovery of an Unusually Selective and Novel Cocaine Analog: Difluoropine. Synthesis and Inhibition of Binding at Cocaine Recognition Sites Peter C. Meltzer, Anna. Y. Liang, and Bertha. K. Madras pp 2001 - 2010; DOI: 10.1021/jm00039a014 |
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3-(2-(3-Pyridinyl)thiazolidin-4-oyl)indoles, a Novel Series of Platelet Activating Factor Antagonists George S. Sheppard, Daisy Pireh, George M. Carrera Jr., Mark G. Bures, H. Robin Heyman, Douglas H. Steinman, Steven K. Davidsen, James G. Phillips, Denise E. Guinn, Paul D. May, Richard D. Conway, David A. Rhein, William C. Calhoun, Daniel H. Albert, Terrance J. Magoc, George W. Carter, and JamesB. Summers pp 2011 - 2032; DOI: 10.1021/jm00039a015 |
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Tyrosine Kinase Inhibitors. 3. Structure-Activity Relationships for Inhibition of Protein Tyrosine Kinases by Nuclear-Substituted Derivatives of 2,2'-Dithiobis(1-methyl-N-phenyl-1H-indole-3-carboxamide) Gordon W. Rewcastle, Brian D. Palmer, Ellen M. Dobrusin, David W. Fry, Alan J. Kraker, and William A. Denny pp 2033 - 2042; DOI: 10.1021/jm00039a016 |
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Novel Spirosuccinimide Aldose Reductase Inhibitors Derived from Isoquinoline-1,3-diones: 2-[(4-Bromo-2-fluorophenyl)methyl]-6-fluorospiro[isoquinoline-4(11H),3'-pyrrolidine]-1,2',3,5'(2H)-tetrone and Congeners. 1 Michael S. Malamas, Thomas C. Hohman, and Jane Millen pp 2043 - 2058; DOI: 10.1021/jm00039a017 |
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N-Substituted Spirosuccinimide, Spiropyridazine, Spiroazetidine, and Acetic Acid Aldose Reductase Inhibitors Derived from Isoquinoline-1,3-diones. 2 Michael S. Malamas and Thomas C. Hohman pp 2059 - 2070; DOI: 10.1021/jm00039a018 |
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New Potent Prolyl Endopeptidase Inhibitors: Synthesis and Structure-Activity Relationships of Indan and Tetralin Derivatives and Their Analogs Yoshiaki Tanaka, Seiichi Niwa, Hiroyasu Nishioka, Takeshi Yamanaka, Motoki Torizuka, Koji Yoshinaga, Naomi Kobayashi, Yugo Ikeda, and Heihachiro Arai pp 2071 - 2078; DOI: 10.1021/jm00039a019 |
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Novel Acyl-CoA:Cholesterol Acyltransferase Inhibitors. Synthesis and Biological Activity of 3-Quinolylurea Derivatives Hiroyuki Tawada, Myles Harcourt, Noriaki Kawamura, Masahiro Kajino, Eiichiro Ishikawa, Yasuo Sugiyama, Hitoshi Ikeda, and Kanji Meguro pp 2079 - 2084; DOI: 10.1021/jm00039a020 |
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Selective Inhibitors of Monoamine Oxidase. 2. Arylamide SAR Morton Harfenist, Charles T. Joyner, Patrick D. Mize, and Helen L. White pp 2085 - 2089; DOI: 10.1021/jm00039a021 |
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Studies on Neurokinin Antagonists. 4. Synthesis and Structure-Activity Relationships of Novel Dipeptide Substance P Antagonists: N2-[(4R)-4-Hydroxy-1-[(1-methyl-1H-indol-3-yl)carbonyl]-L-prolyl]-N-methyl-N-(phenylmethyl)-3-(2-naphthyl)-L-alaninamide and Its Related Compounds Daijiro Hagiwara, Hiroshi Miyake, Norihiro Igari, Masako Karino, Yasue Maeda, Takashi Fujii, and Masaaki Matsuo pp 2090 - 2099; DOI: 10.1021/jm00039a022 |
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Identification of Two Hydrophobic Patches in the Active-Site Cavity of Human Carbonic Anhydrase II by Solution-Phase and Solid-State Studies and Their Use in the Development of Tight-Binding Inhibitors Ahamindra Jain, George M. Whitesides, Richard S. Alexander, and David W. Christianson pp 2100 - 2105; DOI: 10.1021/jm00039a023 |
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Cyclic GMP Phosphodiesterase Inhibitors. 2. Requirement of 6-Substitution of Quinazoline Derivatives for Potent and Selective Inhibitory Activity Yasutaka Takase, Takao Saeki, Nobuhisa Watanabe, Hideyuki Adachi, Shigeru Souda, and Isao Saito pp 2106 - 2111; DOI: 10.1021/jm00039a024 |
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Thienyl and Thiazolyl Acyclic Analogs of 5-Deazatetrahydrofolic Acid Stephen J. Hodson, Eric C. Bigham, David S. Duch, Gary K. Smith, and Robert Ferone pp 2112 - 2115; DOI: 10.1021/jm00039a025 |
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Studies on analogs of classical antifolates bearing the naphthoyl group in place of benzoyl in the side chain. [Erratum to document cited in CA120:192237] James R. Piper, Cheryl A. Johnson, Joseph A. Maddry, Neeta D. Malik, John J. McGuire, Glenys M. Otter, and Francis M. Sirotnak pp 2120 - 2120; DOI: 10.1021/jm00039a026 |
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Book Review pp 2116 - 2119; DOI: 10.1021/jm00039a600 |
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Retro-Binding Tripeptide Thrombin Active-Site Inhibitors: Discovery, Synthesis, and Molecular Modeling Edwin J. Iwanowicz, Wan F. Lau, James Lin, Daniel G. M. Roberts, and Steven M. Seiler pp 2122 - 2124; DOI: 10.1021/jm00040a001 |
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Probes for Narcotic Receptor Mediated Phenomena. 19. Synthesis of (+)-4-[(.alpha.R)-.alpha.-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]-N,N-diethylbenzamide (SNC 80): A Highly Selective, Nonpeptide .delta. Opioid Receptor Agonist Silvia N. Calderon, Richard B. Rothman, Frank Porreca, Judith L. Flippen-Anderson, Robert W. McNutt, Heng Xu, Larren E. Smith, Edward J. Bilsky, Peg Davis, and Kenner C. Rice pp 2125 - 2128; DOI: 10.1021/jm00040a002 |
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A New Series of PDGF Receptor Tyrosine Kinase Inhibitors: 3-Substituted Quinoline Derivatives Martin P. Maguire, Kimberly R. Sheets, Karen McVety, Alfred P. Spada, and Asher Zilberstein pp 2129 - 2137; DOI: 10.1021/jm00040a003 |
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4-[(Alkylamino)methyl]furo[3,2-c]pyridines: A New Series of Selective .kappa.-Receptor Agonists Alan Naylor, Duncan B. Judd, David I. C. Scopes, Ann G. Hayes, and Philip J. Birch pp 2138 - 2144; DOI: 10.1021/jm00040a004 |
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Comparison of the Conformation of Active and Nonactive Backbone Cyclic Analogs of Substance P as a Tool To Elucidate Features of the Bioactive Conformation: NMR and Molecular Dynamics in DMSO and Water Simona Golic Grdadolnik, Dale F. Mierke, Gerardo Byk, Irena Zeltser, Chaim Gilon, and Horst Kessler pp 2145 - 2152; DOI: 10.1021/jm00040a005 |
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Synthesis and Anticonvulsant Properties of New Benzylpyridazine Derivatives Stephane Moreau, Pascal Coudert, Catherine Rubat, Daniel Gardette, Danielle Vallee-Goyet, Jacques Couquelet, Pierre Bastide, and Pierre Tronche pp 2153 - 2160; DOI: 10.1021/jm00040a006 |
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S-(N-Aryl-N-hydroxycarbamoyl)glutathione Derivatives Are Tight-Binding Inhibitors of Glyoxalase I and Slow Substrates for Glyoxalase II Nunna S. R. K. Murthy, Tina Bakeris, Malcolm J. Kavarana, Diana S. Hamilton, Yin Lan, and Donald J. Creighton pp 2161 - 2166; DOI: 10.1021/jm00040a007 |
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Synthesis and Biological Activity of N.omega.-Hemiphthaloyl-.alpha.,.omega.-diaminoalkanoic Acid Analogs of Aminopterin and 3',5-Dichloroaminopterin Andre Rosowsky, Henry Bader, Joel E. Wright, Khandan Keyomarsi, and Larry H. Matherly pp 2167 - 2174; DOI: 10.1021/jm00040a008 |
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Hypoxia-Selective Antitumor Agents. 9. Structure-Activity Relationships for Hypoxia-Selective Cytotoxicity among Analogs of 5-[N,N-Bis(2-chloroethyl)amino]-2,4-dinitrobenzamide Brian D. Palmer, William R. Wilson, Graham J. Atwell, Diane Schultz, Xing Z. Xu, and William A. Denny pp 2175 - 2184; DOI: 10.1021/jm00040a009 |
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Anticancer Specificity of Some Ellipticinium Salts against Human Brain Tumors in vitro Edward M. Acton, Ven L. Narayanan, Prabhakar A. Risbood, Robert H. Shoemaker, David T. Vistica, and Michael R. Boyd pp 2185 - 2189; DOI: 10.1021/jm00040a010 |
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Design and Synthesis of Ellipticinium Salts and 1,2-Dihydroellipticines with High Selectivities against Human CNS Cancers in vitro Jurjus Jurayj, Rudiger D. Haugwitz, Ravi K. Varma, Kenneth D. Paull, John F. Barrett, and Mark Cushman pp 2190 - 2197; DOI: 10.1021/jm00040a011 |
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Synthesis of Androst-5-en-7-ones and Androsta-3,5-dien-7-ones and Their Related 7-Deoxy Analogs as Conformational and Catalytic Probes for the Active Site of Aromatase Mitsuteru Numazawa, Ayako Mutsumi, Mii Tachibana, and Kumiko Hoshi pp 2198 - 2205; DOI: 10.1021/jm00040a012 |
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Three-dimensional quantitative structure-activity relationship of human immunodeficiency virus (I) protease inhibitors. 2. Predictive power using limited exploration of alternate binding modes Tudor I. Oprea, Chris L. Waller, and Garland R. Marshall pp 2206 - 2215; DOI: 10.1021/jm00040a013 |
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Inhibition of Human Immunodeficiency Virus Type 1 Replication by Phosphonoformate- and Phosphonoacetate-2',3'-Dideoxy-3'-thiacytidine Conjugates Anne-Sophie Charvet, Michel Camplo, Philippe Faury, Jean-Christophe Graciet, Nicolas Mourier, Jean-Claude Chermann, and Jean-Louis Kraus pp 2216 - 2223; DOI: 10.1021/jm00040a014 |
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Identification of Tricyclic Analogs Related to Ellagic Acid as Potent/Selective Tyrosine Protein Kinase Inhibitors Robert L. Dow, Thomas T. Chou, Bruce M. Bechle, Colin Goddard, and Eric R. Larson pp 2224 - 2231; DOI: 10.1021/jm00040a015 |
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Phospholipase C Inhibitors: A New Class of Agents Frank W. Perrella, Shih-Fong Chen, Davette L. Behrens, Robert F. III Kaltenbach, and Steven P. Seitz pp 2232 - 2237; DOI: 10.1021/jm00040a016 |
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Novel, Potent Luteinizing Hormone-Releasing Hormone Antagonists with Improved Solubility in Water Anna Janecka, Tomasz Janecki, Si-mei Shan, Cyril Bowers, and Karl Folkers pp 2238 - 2241; DOI: 10.1021/jm00040a017 |
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Nonpeptide Peptidomimetic Antagonists of the Neuropeptide Y Receptor: Benextramine Analogs with Selectivity for the Peripheral Y2 Receptor Chandra Chaurasia, Gregory Misse, Richard Tessel, and Michael B. Doughty pp 2242 - 2248; DOI: 10.1021/jm00040a018 |
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Synthesis of Substituted 3-Carbamoylecgonine Methyl Ester Analogs: Irreversible and Photoaffinity Ligands for the Cocaine Receptor/Dopamine Transporter Richard H. Kline, Amy J. Eshleman, Mohyee E. Eldefrawi, and Jeremy Wright pp 2249 - 2252; DOI: 10.1021/jm00040a019 |
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Editorial - "Mean Graphs" of NCI Screening Data pp 2121 - 2121; DOI: 10.1021/jm00040a600 |
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Evolution of a Novel Series of [(N,N-Dimethylamino)propyl]- and Piperazinylbenzanilides as the First Selective 5-HT1D Antagonists John W. Clitherow, David I. C. Scopes, Malcolm Skingle, Christopher C. Jordan, Wasyl Feniuk, Ian B. Campbell, Malcolm C. Carter, Eric W. Collington, Helen E. Connor, and et al. pp 2253 - 2257; DOI: 10.1021/jm00041a001 |
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Novel 3.alpha.-(Diphenylmethoxy)tropane Analogs: Potent Dopamine Uptake Inhibitors without Cocaine-like Behavioral Profiles Amy Hauck Newman, Andrew C. Allen, Sari Izenwasser, and Jonathan L. Katz pp 2258 - 2261; DOI: 10.1021/jm00041a002 |
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Discovery of a Potent, Peripherally Selective trans-3,4-Dimethyl-4-(3-hydroxyphenyl)piperidine Opioid Antagonist for the Treatment of Gastrointestinal Motility Disorders Dennis M. Zimmerman, Jaswant S. Gidda, Buddy E. Cantrell, Darryle D. Schoepp, Bryan G. Johnson, and J. David Leander pp 2262 - 2265; DOI: 10.1021/jm00041a003 |
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Computer Modeling Analysis for Enediyne Chromophore-Apoprotein Complex of Macromolecular Antitumor Antibiotic C-1027 Yasushi Okuno, Masami Otsuka, and Yukio Sugiura pp 2266 - 2273; DOI: 10.1021/jm00041a004 |
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Crystal-Structure-Based Design and Synthesis of Novel C-Terminal Inhibitors of HIV Protease Michael D. Varney, Krzysztof Appelt, Vince Kalish, M. Rami Reddy, John Tatlock, Cindy L. Palmer, William H. Romines, Bor-Wen Wu, and Linda Musick pp 2274 - 2284; DOI: 10.1021/jm00041a005 |
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Novel 1-Phenylcycloalkanecarboxylic Acid Derivatives Are Potent and Selective .sigma.1 Ligands Silvia N. Calderon, Sari Izenwasser, Brett Heller, J. Silvio Gutkind, Mariena V. Mattson, Tsung-Ping Su, and Amy Hauck Newman pp 2285 - 2291; DOI: 10.1021/jm00041a006 |
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Central Cholinergic Agents. 6. Synthesis and Evaluation of 3-[1-(Phenylmethyl)-4-piperidinyl]-1-(2,3,4,5-tetrahydro-1H-1-benzazepin-8-yl)- 1-propanones and Their Analogs as Central Selective Acetylcholinesterase Inhibitors Yuji Ishihara, Keisuke Hirai, Masaomi Miyamoto, and Giichi Goto pp 2292 - 2299; DOI: 10.1021/jm00041a007 |
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Modeling the anticarcinogenic action of retinoids by making use of the OASIS method. 3. Inhibition of the induction of ornithine decarboxylase by arotinoids Danail Bonchev, William A. Seitz, Clifton F. Mountain, and Alexandru T. Balaban pp 2300 - 2307; DOI: 10.1021/jm00041a008 |
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Benzisoxazole- and Benzisothiazole-3-carboxamides as Potential Atypical Antipsychotic Agents Nicholas J. Hrib, John G. Jurcak, Kendra L. Burgher, Paul G. Conway, Harold B. Hartman, Lisa L. Kerman, Joachim E. Roehr, and Ann T. Woods pp 2308 - 2314; DOI: 10.1021/jm00041a009 |
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Compass: Predicting Biological Activities from Molecular Surface Properties. Performance Comparisons on a Steroid Benchmark Ajay N. Jain, Kimberle Koile, and David Chapman pp 2315 - 2327; DOI: 10.1021/jm00041a010 |
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A Structure-Activity Relationship Study of Benzylic Modifications of 4-[1-(1-Naphthyl)ethyl]-1H-imidazoles on .alpha.1- and .alpha.2-Adrenergic Receptors Seoung-Soo Hong, Karl J. Romstedt, Dennis R. Feller, Fu-Lian Hsu, Thomas L. Cupps, Robert A. Lyon, and Duane D. Miller pp 2328 - 2333; DOI: 10.1021/jm00041a011 |
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Design, Synthesis and Evaluation of Substituted Triarylnipecotic Acid Derivatives as GABA Uptake Inhibitors: Identification of a Ligand with Moderate Affinity and Selectivity for the Cloned Human GABA Transporter GAT-3 T. G. Murali Dhar, Laurence A. Borden, Sriram Tyagarajan, Kelli E. Smith, Theresa A. Branchek, Richard L. Weinshank, and Charles Gluchowski pp 2334 - 2342; DOI: 10.1021/jm00041a012 |
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Design and Synthesis of Seco-oxysterol Analogs as Potential Inhibitors of 3-Hydroxy-3-methylglutaryl-Coenzyme A (HMG-CoA) Reductase Gene Transcription Scott D. Larsen, Charles H. Spilman, Yoshi Yagi, Dac M. Dinh, Karen L. Hart, and Gerard F. Hess pp 2343 - 2351; DOI: 10.1021/jm00041a013 |
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6-Azasteroids: Structure-Activity Relationships for Inhibition of Type 1 and 2 Human 5.alpha.-Reductase and Human Adrenal 3.beta.-Hydroxy-.DELTA.5-steroid Dehydrogenase/3-Keto-.DELTA.5-steroid Isomerase Stephen V. Frye, Curt D. Haffner, Patrick R. Maloney, Robert A. Mook Jr., George F. Dorsey, Roger N. Hiner, Cindy M. Cribbs, Thomas N. Wheeler, John A. Ray, and et al. pp 2352 - 2360; DOI: 10.1021/jm00041a014 |
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Novel Prodrugs of Alkylating Agents Derived from 2-Fluoro- and 3-Fluorobenzoic Acids for Antibody-Directed Enzyme Prodrug Therapy Caroline J. Springer, Ion Niculescu-Duvaz, and R. Barbara Pedley pp 2361 - 2370; DOI: 10.1021/jm00041a015 |
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Synthesis and SAR Studies of Novel Triazolopyrimidine Derivatives as Potent, Orally Active Angiotensin II Receptor Antagonists Eric Nicolai, Gerard Cure, Joel Goyard, Maud Kirchner, Jean-Marie Teulon, Annie Versigny, Michele Cazes, Francois Caussade, Angela Virone-Oddos, and Alix Cloarec pp 2371 - 2386; DOI: 10.1021/jm00041a016 |
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14-Epi Stereoisomers of 25-Hydroxy- and 1.alpha.,25-Dihydroxyvitamin D3: Synthesis, Isomerization to Previtamins, and Biological Studies David F. Maynard, William G. Trankle, Anthony W. Norman, and William H. Okamura pp 2387 - 2393; DOI: 10.1021/jm00041a017 |
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Inhibitors of Acyl-CoA:Cholesterol O-Acyltransferase. 11. Structure-Activity Relationships of Several Series of Compounds Derived from N-(Chlorocarbonyl) Isocyanate Joseph A. Picard, Richard F. Bousley, Helen T. Lee, Katherine L. Hamelehle, Brian R. Krause, Laura L. Minton, Drago R. Sliskovic, and Richard L. Stanfield pp 2394 - 2400; DOI: 10.1021/jm00041a018 |
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Geiparvarin Analogs. 4.1. Synthesis and Cytostatic Activity of Geiparvarin Analogs Bearing a Carbamate Moiety or a Furocoumarin Fragment on the Alkenyl Side Chain S. Manfredini, P. G. Baraldi, R. Bazzanini, M. Guarneri, D. Simoni, J. Balzarini, and E. De Clercq pp 2401 - 2405; DOI: 10.1021/jm00041a019 |
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A new photoaffinity analog of cGMP: Potent inhibitor of cyclic nucleotide phosphodiesterase James W. Clack and Peter J. Stein pp 2406 - 2410; DOI: 10.1021/jm00041a020 |
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Leukotriene B4 (LTB4) Receptor Antagonists: A Series of (Hydroxyphenyl)pyrazoles Richard W. Harper, William T. Jackson, Larry L. Froelich, Robert J. Boyd, Timothy E. Aldridge, and David K. Herron pp 2411 - 2420; DOI: 10.1021/jm00041a021 |
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Oxadiazoles as Ester Bioisosteric Replacements in Compounds Related to Disoxaril. Antirhinovirus Activity Guy D. Diana, Deborah L. Volkots, Theodore J. Nitz, Thomas R. Bailey, Melody A. Long, Niranjan Vescio, Suzanne Aldous, Daniel C. Pevear, and Frank J. Dutko pp 2421 - 2436; DOI: 10.1021/jm00041a022 |
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Synthesis of a Series of 4-(Arylethynyl)-6-chloro-4-cyclopropyl-3,4-dihydroquinazolin-2(1H)-ones as Novel Non-nucleoside HIV-1 Reverse Transcriptase Inhibitors Thomas J. Tucker, Terry A. Lyle, Catherine M. Wiscount, Susan F. Britcher, Steven D. Young, William M. Sanders, William C. Lumma, Mark E. Goldman, Julie A. O'Brien, and et al. pp 2437 - 2444; DOI: 10.1021/jm00041a023 |
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Synthesis and Evaluation of 9-Hydroxy-5-methyl- (and 5,6-dimethyl)-6H-pyrido[4,3-b]carbazole-1-N-[(dialkylamino)alkyl]carboxamides, a New Promising Series of Antitumor Olivacine Derivatives Richard Jaszfold-Howorko, Corinne Landras, Alain Pierre, Ghanem Atassi, Nicolas Guilbaud, Laurence Kraus-Berthier, Stephane Leonce, Yves Rolland, Jean-Francois Prost, and Emile Bisagni pp 2445 - 2452; DOI: 10.1021/jm00041a024 |
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Dopaminergic Benzo[a]phenanthridines: Resolution and Pharmacological Evaluation of the Enantiomers of Dihydrexidine, the Full Efficacy D1 Dopamine Receptor Agonist Timm A. Knoerzer, David E. Nichols, William K. Brewster, Val J. Watts, David Mottola, and Richard B. Mailman pp 2453 - 2460; DOI: 10.1021/jm00041a025 |
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Mercaptoacyl aminoacid inhibitors of atriopeptidase. 1. Structure-activity relationship studies of methionine and S-alkylcysteine derivatives Bernard R. Neustadt, Elizabeth M. Smith, Terry L. Nechuta, Alan A. Bronnenkant, Martin F. Haslanger, Robert W. Watkins, Caroline J. Foster, and Edmund J. Sybertz pp 2461 - 2476; DOI: 10.1021/jm00041a026 |
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Structure-Based Design of Inhibitors of Purine Nucleoside Phosphorylase. 5. 9-Deazahypoxanthines Shri Niwas, Pooran Chand, Ved P. Pathak, and John A. Montgomery pp 2477 - 2480; DOI: 10.1021/jm00041a027 |
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Synthesis and Tissue Biodistribution of [.omega.-11C]Palmitic Acid. A Novel Pet Imaging Agent for Cardiac Fatty acid Metabolism Brad O. Buckman, Henry F. VanBrocklin, Carmen S. Dence, Steven R. Bergmann, Michael J. Welch, and John A. Katzenellenbogen pp 2481 - 2485; DOI: 10.1021/jm00041a028 |
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Synthesis and antibacterial activity of thiazolopyrazine-incorporated tetracyclic quinolone antibacterials. [Erratum to document cited in CA121:9355] Yoshimasa Inoue, Hirosato Kondo, Masahiro Taguichi, Yoshikazu Jinbo, Fumio Sakamoto, and Goro Tsukamoto pp 2488 - 2488; DOI: 10.1021/jm00041a029 |
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Book Reviews pp 2486 - 2487; DOI: 10.1021/jm00041a600 |
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GABAA Receptor Agonists, Partial Agonists, and Antagonists. Design and Therapeutic Prospects Povl Krogsgaard-Larsen, Bente Froelund, Flemming S. Joergensen, and Arne Schousboe pp 2489 - 2505; DOI: 10.1021/jm00042a001 |
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Structure-Based Design of HIV-1 Protease Inhibitors: Replacement of Two Amides and a 10.pi.-Aromatic System by a Fused Bis-tetrahydrofuran Arun K. Ghosh, Wayne J. Thompson, Paula M. D. Fitzgerald, J. Chris Culberson, Melinda G. Axel, Sean P. McKee, Joel R. Huff, and Paul S. Anderson pp 2506 - 2508; DOI: 10.1021/jm00042a002 |
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5-[(3-Nitropyrid-2-yl)amino]indoles: Novel Serotonin Agonists with Selectivity for the 5-HT1D Receptor. Variation of the C3 Substituent on the Indole Template Leads to Increased 5-HT1D Receptor Selectivity John E. Macor, David H. Blank, Carol B. Fox, Lorraine A. Lebel, Michael E. Newman, Ronald J. Post, Kevin Ryan, Anne W. Schmidt, David W. Schulz, and B. Kenneth Koe pp 2509 - 2512; DOI: 10.1021/jm00042a003 |
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Synthesis of Naphthalenesulfonic Acid Small Molecules as Selective Inhibitors of the DNA Polymerase and Ribonuclease H Activities of HIV-1 Reverse Transcriptase Prem Mohan, Shoshana Loya, Orna Avidan, Sandeep Verma, Gurnam S. Dhindsa, Man Fai Wong, Peggy P. Huang, Makoto Yashiro, Masanori Baba, and Amnon Hizi pp 2513 - 2519; DOI: 10.1021/jm00042a004 |
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HIV-1 Reverse Transcriptase Inhibitor Design Using Artificial Neural Networks Igor V. Tetko, Vsevolod Yu. Tanchuk, Neliya P. Chentsova, Svetlana V. Antonenko, Gennady I. Poda, Valery P. Kukhar, and Alexander I. Luik pp 2520 - 2526; DOI: 10.1021/jm00042a005 |
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Genetically Evolved Receptor Models: A Computational Approach to Construction of Receptor Models D. Eric Walters and R. Michael Hinds pp 2527 - 2536; DOI: 10.1021/jm00042a006 |
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Non-Peptide Fibrinogen Receptor Antagonists. 2. Optimization of a Tyrosine Template as a Mimic for Arg-Gly-Asp Melissa S. Egbertson, Charles T.-C. Chang, Mark E. Duggan, Robert J. Gould, Wasyl Halczenko, George D. Hartman, William L. Laswell, Joseph J. Lynch Jr., Robert J. Lynch, and et al. pp 2537 - 2551; DOI: 10.1021/jm00042a007 |
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Cyclic Benzamides as Mixed Dopamine D2/Serotonin 5-HT2 Receptor Antagonists: Potential Atypical Antipsychotic Agents Mark H. Norman, Greg C. Rigdon, Frank Navas, and Barrett R. Cooper pp 2552 - 2563; DOI: 10.1021/jm00042a008 |
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Synthesis and Atypical Antipsychotic Profile of Some 2-(2-Piperidinoethyl)benzocycloalkanones as Analogs of Butyrophenone Jose A. Fontenla, Javier Osuna, Elizabeth Rosa, Ma Elena Castro, Tomas G-Ferreiro, Isabel Loza-Garcia, Jose M. Calleja, Ferran Sanz, Jesus Rodriguez, and et al. pp 2564 - 2573; DOI: 10.1021/jm00042a009 |
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Spirovesamicols: Conformationally Restricted Analogs of 2-(4-Phenylpiperidino)cyclohexanol (Vesamicol, AH5183) as Potential Modulators of Presynaptic Cholinergic Function S. M. N. Efange, A. B. Khare, C. Foulon, S. K. Akella, and S. M. Parsons pp 2574 - 2582; DOI: 10.1021/jm00042a010 |
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Synthesis and Biological Properties of5-o-Carboranyl-1-(2-deoxy-2-fluoro-.beta.-D-arabinofuranosyl)uracil Geraldine Fulcrand-El Kattan, Naganna M. Goudgaon, Nurcan Ilksoy, Jay-Tung Huang, Kyoichi A. Watanabe, Jean-Pierre Sommadossi, and Raymond F. Schinazi pp 2583 - 2588; DOI: 10.1021/jm00042a011 |
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Comparative Molecular Field Analysis Using GRID Force-Field and GOLPE Variable Selection Methods in a Study of Inhibitors of Glycogen Phosphorylase b Gabriele Cruciani and Kimberly A. Watson pp 2589 - 2601; DOI: 10.1021/jm00042a012 |
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Synthesis and Structure-Activity Relationships of New Antitumor Taxoids. Effects of Cyclohexyl Substitution at the C-3' and/or C-2 of Taxotere (Docetaxel) Iwao Ojima, Olivier Duclos, Martine Zucco, Marie-Christine Bissery, C. Combeau, P. Vrignaud, J. F. Riou, and Francois Lavelle pp 2602 - 2608; DOI: 10.1021/jm00042a013 |
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Maleimidoethyl 3-(Tri-n-butylstannyl)hippurate: A Useful Radioiodination Reagent for Protein Radiopharmaceuticals To Enhance Target Selective Radioactivity Localization Yasushi Arano, Kouji Wakisaka, Yoshiro Ohmomo, Takashi Uezono, Takahiro Mukai, Hiroshi Motonari, Hiromitsu Shiono, Harumi Sakahara, Junji Konishi, and et al. pp 2609 - 2618; DOI: 10.1021/jm00042a014 |
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Synthesis and Pharmacological Properties of 11-Hydroxy-3-(1',1'-dimethylheptyl)hexahydrocannabinol: A High Affinity Cannabinoid Agonist Guo Yan, Dali Yin, Atmaram D. Khanolkar, David R. Compton, Billy R. Martin, and Alexandros Makriyannis pp 2619 - 2622; DOI: 10.1021/jm00042a015 |
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2,6-Disubstituted Aryl Carboxylic Acids, Leaving Groups "Par Excellence" for Benzisothiazolone Inhibitors of Human Leukocyte Elastase Chakrapani Subramanyam, Malcolm R. Bell, Philip Carabateas, John J. Court, John A. Jr. Dority, Edward Ferguson, Robert Gordon, Dennis J. Hlasta, Virendra Kumar, and et al. pp 2623 - 2626; DOI: 10.1021/jm00043a001 |
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5,7-Dimethoxy-3-(4-Pyridinyl)Quinoline Is a Potent and Selective Inhibitor of Human Vascular .beta.-Type Platelet-Derived Growth Factor Receptor Tyrosine Kinase Roland E. Dolle, Joseph A. Dunn, Mark Bobko, Baldev Singh, Joan E. Kuster, Eugene Baizman, Alex L. Harris, David G. Sawutz, Deborah Miller, and et al. pp 2627 - 2629; DOI: 10.1021/jm00043a002 |
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Synthesis, Structural Characterization, and Antitumor Properties of a Novel Class of Large-Ring Platinum(II) Chelate Complexes Incorporating the cis-1,4-Diaminocyclohexane Ligand in a Unique Locked Boat Conformation James D. Hoeschele, H. D. Hollis Showalter, Alan J. Kraker, William L. Elliott, Billy J. Roberts, and Jeff W. Kampf pp 2630 - 2636; DOI: 10.1021/jm00043a003 |
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A Basis for New Approaches to the Chemotherapy of AIDS: Novel Genes in HIV-1 Potentially Encode Selenoproteins Expressed by Ribosomal Frameshifting and Termination Suppression E. W. Taylor, C. S. Ramanathan, R. K. Jalluri, and R. G. Nadimpalli pp 2637 - 2654; DOI: 10.1021/jm00043a004 |
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Synthesis and Biological Evaluation of C-3'-Modified Analogs of 9(R)-Dihydrotaxol Leping Li, Sheela A. Thomas, Larry L. Klein, Clinton M. Yeung, Clarence J. Maring, David J. Grampovnik, Paul A. Lartey, and Jacob J. Plattner pp 2655 - 2663; DOI: 10.1021/jm00043a005 |
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A Novel Nonpeptide HIV-1 Protease Inhibitor: Elucidation of the Binding Mode and Its Application in the Design of Related Analogs Elizabeth A. Lunney, Susan E. Hagen, John M. Domagala, Christine Humblet, Janet Kosinski, Bradley D. Tait, Joseph S. Warmus, Michael Wilson, Donna Ferguson, and et al. pp 2664 - 2677; DOI: 10.1021/jm00043a006 |
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Discovery of Nanomolar Ligands for 7-Transmembrane G-Protein-Coupled Receptors from a Diverse N-(Substituted)glycine Peptoid Library Ronald N. Zuckermann, Eric J. Martin, David C. Spellmeyer, Gregory B. Stauber, Kevin R. Shoemaker, Janice M. Kerr, Gianine M. Figliozzi, Dane A. Goff, Michael A. Siani, and et al. pp 2678 - 2685; DOI: 10.1021/jm00043a007 |
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Binding of 5H-Dibenzo[b,e][1,4]diazepine and Chiral 5H-Dibenzo[a,d]cycloheptene Analogs of Clozapine to Dopamine and Serotonin Receptors Shawn T. Phillips, Tomas de Paulis, Bruce M. Baron, Barry W. Siegel, Philip Seeman, Hubert H. M. Van Tol, Hong-chang Guan, and Howard E. Smith pp 2686 - 2696; DOI: 10.1021/jm00043a008 |
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[(3-Pyridylalkyl)piperidylidene]benzocycloheptapyridine Derivatives as Dual Antagonists of PAF and Histamine Elena Carceller, Manuel Merlos, Marta Giral, Dolors Balsa, Carmen Almansa, Javier Bartroli, Julian Garcia-Rafanell, and Javier Forn pp 2697 - 2703; DOI: 10.1021/jm00043a009 |
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Substituted 1,3-Dipropylxanthines as Irreversible Antagonists of A1 Adenosine Receptors Peter J. Scammells, Stephen P. Baker, Luiz Belardinelli, and Ray A. Olsson pp 2704 - 2712; DOI: 10.1021/jm00043a010 |
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Cyclic Peptides with a Phosphinic Bond as Potent Inhibitors of a Zinc Bacterial Collagenase Athanasios Yiotakis, Alain Lecoq, Stamatia Vassiliou, Isabelle Raynal, Philippe Cuniasse, and Vincent Dive pp 2713 - 2720; DOI: 10.1021/jm00043a011 |
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Novel Benzisoxazole Derivatives as Potent and Selective Inhibitors of Acetylcholinesterase Anabella Villalobos, James F. Blake, C. Kelly Biggers, Todd W. Butler, Douglas S. Chapin, Yuhpyng L. Chen, Jeffrey L. Ives, Shawn B. Jones, Dane R. Liston, and et al. pp 2721 - 2734; DOI: 10.1021/jm00043a012 |
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substituted (S)-Phenylpiperidines and Rigid Congeners as Preferential Dopamine Autoreceptor Antagonists: Synthesis and Structure-Activity Relationships Clas Sonesson, Chiu-Hong Lin, Lars Hansson, Nicholas Waters, Kjell Svensson, Arvid Carlsson, Martin W. Smith, and Haakan Wikstroem pp 2735 - 2753; DOI: 10.1021/jm00043a013 |
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Structure-Activity Relationship Studies of Central Nervous System Agents. 13.4-[3-(Benzotriazol-1-yl)propyl]-1-(2-methoxyphenyl)piperazine, a New Putative 5-HT1A Receptor Antagonist, and Its Analogs Jerzy L. Mokrosz, Maria H. Paluchowska, Ewa Chojnacka-Wojcik, Malgorzata Filip, Sijka Charakchieva-Minol, Anna Deren-Wesolek, and Maria J. Mokrosz pp 2754 - 2760; DOI: 10.1021/jm00043a014 |
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Structure-Affinity Relationship Studies on 5-HT1A receptor Ligands. 2. Heterobicyclic Phenylpiperazines with N4-Aralkyl Substituents Bart J. van Steen, Ineke van Wijngaarden, Martin Th. M. Tulp, and Willem Soudijn pp 2761 - 2773; DOI: 10.1021/jm00043a015 |
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Design, Synthesis, and Neurochemical Evaluation of 2-Amino-5-(alkoxycarbonyl)-3,4,5,6-tetrahydropyridines and 2-Amino-5-(alkoxycarbonyl)-1,4,5,6-tetrahydropyrimidines as M1 Muscarinic Receptor Agonists Philip G. Dunbar, Graham J. Durant, Taikyun Rho, Babatunde Ojo, James J. III Huzl, Douglas A. Smith, Afif A. El-Assadi, Sbeih Sbeih, Dan O. Ngur, and et al. pp 2774 - 2782; DOI: 10.1021/jm00043a016 |
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Identification of a Receptor-Binding Region in the Core Segment of the Human Anaphylatoxin C5a Isidoros Vlattas, Iou Iou Sytwu, James Dellureficio, James Stanton, Albert F. Braunwalder, Nicholas Galakatos, Richard Kramer, Bruce Seligmann, Matthew A. Sills, and James Wasvary pp 2783 - 2790; DOI: 10.1021/jm00043a017 |
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Synthesis and Antibacterial Activity of Thiazolopyrazine-Incorporated Tetracyclic Quinolone Antibacterial Agents. 2 Yoshikazu Jinbo, Hirosato Kondo, Masahiro Taguchi, Yoshimasa Inoue, Fumio Sakamoto, and Goro Tsukamoto pp 2791 - 2796; DOI: 10.1021/jm00043a018 |
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Photodynamic Antitumor Agents: .beta.-Methoxyethyl Groups Give Access to Functionalized Porphycenes and Enhance Cellular Uptake and Activity Clemens Richert, Jurina M. Wessels, Martin Mueller, Michael Kisters, Thomas Benninghaus, and Alwin E. Goetz pp 2797 - 2807; DOI: 10.1021/jm00043a019 |
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Triazolinone Biphenylsulfonamide Derivatives as Orally Active Angiotensin II Antagonists with Potent AT1 Receptor Affinity and Enhanced AT2 Affinity Wallace T. Ashton, Linda L. Chang, Kelly L. Flanagan, Steven M. Hutchins, Elizabeth M. Naylor, Prasun K. Chakravarty, Arthur A. Patchett, William J. Greenlee, Tsing-Bau Chen, and et al. pp 2808 - 2824; DOI: 10.1021/jm00043a020 |
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Book Reviews pp 2825 - 2826; DOI: 10.1021/jm00043a600 |
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5-(Nonyloxy)tryptamine: A Novel High-Affinity 5-HT1D.beta. Serotonin Receptor Agonist Richard A. Glennon, Seoung-Soo Hong, Malgorzata Dukat, Milt Teitler, and Kathy Davis pp 2828 - 2830; DOI: 10.1021/jm00044a001 |
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Aza-Tricyclic Substance P Antagonists John A. Lowe, Susan E. Drozda, Stafford McLean, D. K. Bryce, Rosemary T. Crawford, R. Michael Snider, Kelly P. Longo, Atsushi Nagahisa, and Megumi Tsuchiya pp 2831 - 2840; DOI: 10.1021/jm00044a002 |
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Structure-Activity Study of 5-Substituted 1-Carbobenzoxy-2-iminohydantoins as Potential Anticonvulsant Agents Zhong-Yue Sun, Chul-Hoon Kwon, and John N. D. Wurpel pp 2841 - 2845; DOI: 10.1021/jm00044a003 |
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Structure-Activity Relationships of 1,2,4-Triazolo[1,5-a]quinoxalines and Their 1-Deaza Analogs Imidazo[1,2-a]quinoxalines at the Benzodiazepine Receptor Daniela Catarzi, Lucia Cecchi, Vittoria Colotta, Fabrizio Melani, Guido Filacchioni, Claudia Martini, Laura Giusti, and Antonio Lucacchini pp 2846 - 2850; DOI: 10.1021/jm00044a004 |
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On the interaction of the aromatic part of dopaminergic agonists with the receptor Darko Kocjan pp 2851 - 2855; DOI: 10.1021/jm00044a005 |
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Isothiocyanate-Substituted .kappa.-Selective Opioid Receptor Ligands Derived from N-Methyl-N-[(1S)-1-phenyl-2-(1-pyrrolidinyl)ethyl]phenylacetamide S. Ananda Weerawarna, Ronda D. Davis, and Wendel L. Nelson pp 2856 - 2864; DOI: 10.1021/jm00044a006 |
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Synthesis, Ligand Binding, and QSAR (CoMFA and Classical) Study of 3.beta.-(3'-Substituted phenyl)-, 3.beta.-(4'-Substituted phenyl)-, and 3.beta.-(3',4'-Disubstituted phenyl)tropane-2.beta.-carboxylic Acid Methyl Esters F. Ivy Carroll, S. Wayne Mascarella, Michael A. Kuzemko, Yigong Gao, Philip Abraham, Anita H. Lewin, John W. Boja, and Michael J. Kuhar pp 2865 - 2873; DOI: 10.1021/jm00044a007 |
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Homology Modeling of the Dopamine D2 Receptor and Its Testing by Docking of Agonists and Tricyclic Antagonists Martha M. Teeter, Mark Froimowitz, Boguslaw Stec, and Curtiss J. DuRand pp 2874 - 2888; DOI: 10.1021/jm00044a008 |
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An Investigation of Desferrithiocin Metabolism Raymond J. Bergeron, Markus Wollenweber, and Jan Wiegand pp 2889 - 2895; DOI: 10.1021/jm00044a009 |
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Synthesis and Antiviral Activity Evaluation of Some Aminoadamantane Derivatives Nicolas Kolocouris, George B. Foscolos, Antonios Kolocouris, Panayotis Marakos, Nicole Pouli, George Fytas, Satoru Ikeda, and Erik De Clercq pp 2896 - 2902; DOI: 10.1021/jm00044a010 |
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Benzoselenazolinone Derivatives Designed To Be Glutathione Peroxidase Mimetics Feature Inhibition of Cyclooxygenase/5-Lipoxygenase Pathways and Anti-inflammatory Activity Vincent Galet, Jean-Luc Bernier, Jean-Piere Henichart, Daniel Lesieur, Claire Abadie, Luc Rochette, Albert Lindenbaum, Jacqueline Chalas, Jean-Francois Renaud de la Faverie, and et al. pp 2903 - 2911; DOI: 10.1021/jm00044a011 |
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Studies on the Mechanism of Decomposition and Structural Factors Affecting the Aqueous Stability of 1,2-Bis(sulfonyl)-1-alkylhydrazines Philip G. Penketh, Krishnamurthy Shyam, and Alan C. Sartorelli pp 2912 - 2917; DOI: 10.1021/jm00044a012 |
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Stereospecific Synthesis of Peptidyl .alpha.-Keto Amides as Inhibitors of Calpain Scott L. Harbeson, Susan M. Abelleira, Alan Akiyama, Robert Barrett, Renee M. Carroll, Julie Ann Straub, Jaroslaw N. Tkacz, Chichih Wu, and Gary F. Musso pp 2918 - 2929; DOI: 10.1021/jm00044a013 |
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Synthesis and Structure-Activity Relationships of Novel Retinoid X Receptor-Selective Retinoids Marcus F. Boehm, Lin Zhang, Beth Ann Badea, Steven K. White, Dale E. Mais, Elaine Berger, Carla M. Suto, Mark E. Goldman, and Richard A. Heyman pp 2930 - 2941; DOI: 10.1021/jm00044a014 |
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Benzimidazole Ribonucleosides: Design, Synthesis, and Antiviral Activity of Certain 2-(Alkylthio)- and 2-(Benzylthio)-5,6-dichloro-1-(.beta.-D-ribofuranosyl)benzimidazoles Rodrigo V. Devivar, Etsuko Kawashima, Ganapathi R. Revankar, Julie M. Breitenbach, Edward D. Kreske, John C. Drach, and Leroy B. Townsend pp 2942 - 2949; DOI: 10.1021/jm00044a015 |
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Differential Inhibition of Aminopeptidase A and Aminopeptidase N by New .beta.-Amino Thiols Eric N. Chauvel, Catherine Llorens-Cortes, Pascale Coric, Sherwin Wilk, Bernard P. Roques, and Marie-Claude Fournie-Zaluski pp 2950 - 2957; DOI: 10.1021/jm00044a016 |
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Novel Synthesis of Cyclic Amide-Linked Analogs of Angiotensins II and III John M. Matsoukas, John Hondrelis, George Agelis, Kleomenis Barlos, Dimitrios Gatos, Renee Ganter, Diana Moore, and Graham J. Moore pp 2958 - 2969; DOI: 10.1021/jm00044a017 |
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8-Azaxanthine Derivatives as Antagonists of Adenosine Receptors Palmarisa Franchetti, Lea Messini, Loredana Cappellacci, Mario Grifantini, Antonio Lucacchini, Claudia Martini, and Generoso Senatore pp 2970 - 2975; DOI: 10.1021/jm00044a018 |
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Synthesis of a Photoaffinity Taxol Analog and Its Use in Labeling Tubulin Debjani Dasgupta, Haeil Park, Geraldine C. B. Harriman, Gunda I. Georg, and Richard H. Himes pp 2976 - 2980; DOI: 10.1021/jm00044a019 |
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Structure-Activity Studies of Antitumor Taxanes: Synthesis of Novel C-13 Side Chain Homologated Taxol and Taxotere Analogs Lalith R. Jayasinghe, Apurba Datta, Syed M. Ali, Jan Zygmunt, David G. Vander Velde, and Gunda I. Georg pp 2981 - 2984; DOI: 10.1021/jm00044a020 |
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Editorial - The Perspective Series Mike Williams pp 2827 - 2827; DOI: 10.1021/jm00044a600 |
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Combinatorial Technologies Involving Reiterative Division/Coupling/Recombination: Statistical Considerations Kevin Burgess, Andy I. Liaw, and Naisyin Wang pp 2985 - 2987; DOI: 10.1021/jm00045a001 |
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Reductive Hydrolysis of the 59,60-Amide Bond of Teicoplanin Antibiotics: A Key Step from Natural to Synthetic Glycopeptides Adriano Malabarba and Romeo Ciabatti pp 2988 - 2990; DOI: 10.1021/jm00045a002 |
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Nonpeptide Renin Inhibitors with Good Intraduodenal Bioavailability and Efficacy in Dog Steven A. Boyd, Anthony K. L. Fung, William R. Baker, Robert A. Mantei, Herman H. Stein, Jerome Cohen, Jennifer L. Barlow, Vered Klinghofer, Jerry L. Wessale, and et al. pp 2991 - 3007; DOI: 10.1021/jm00045a003 |
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Synthesis, Resolution, and SAR of (.+-.)-2-Amino-N-methyl-.alpha.-(3-methyl-2-thienyl)benzeneethanamine and Related Analogs as Noncompetitive NMDA Antagonists with Neuroprotective Properties Lawrence L. Martin, George E. Lee, Thomas B. K. Lee, Douglas K. Rush, Carole A. Wilmot, Erich Paulus, Ulrich Elben, John J. Grome, Elena Porsche-Wiebking, and et al. pp 3008 - 3015; DOI: 10.1021/jm00045a004 |
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Synthesis and Quantitative Structure-Activity Relationships of Anticonvulsant 2,3,6-Triaminopyridines Joachim K. Seydel, Klaus-J. Schaper, Eugene A. Coats, Hans P. Cordes, Peter Emig, Juergen Engel, Bernhard Kutscher, and Emmanuel E. Polymeropoulos pp 3016 - 3022; DOI: 10.1021/jm00045a005 |
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Synthesis and Biological Activity of 3-[2-(Dimethylamino)ethyl]-5-[(1,1-dioxo-5-methyl-1,2,5-thiadiazolidin-2-yl)methyl]-1H-indole and Analogs: Agonists for the 5-HT1D Receptor Jose L. Castro, Raymond Baker, Alexander R. Guiblin, Sarah C. Hobbs, Matthew R. Jenkins, Michael G. N. Russell, Margaret S. Beer, Josephine A. Stanton, Kate Scholey, and et al. pp 3023 - 3032; DOI: 10.1021/jm00045a006 |
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Antitumor Agents. VII. Synthesis and Antitumor Activity of Novel Hexacyclic Camptothecin Analogs Masamichi Sugimori, Akio Ejima, Satoru Ohsuki, Kouichi Uoto, Ikuo Mitsui, Kensuke Matsumoto, Yasuyoshi Kawato, Megumi Yasuoka, Keiki Sato, and et al. pp 3033 - 3039; DOI: 10.1021/jm00045a007 |
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Design, Synthesis, and Biological Evaluation of Cosalane, a Novel Anti-HIV Agent Which Inhibits Multiple Features of Virus Reproduction Mark Cushman, W. Marek Golebiewski, James B. McMahon, Robert W. Buckheit, David J. Clanton, Owen Weislow, Rudiger D. Haugwitz, John P. Bader, Lisa Graham, and William G. Rice pp 3040 - 3050; DOI: 10.1021/jm00045a008 |
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Cancer Chemopreventive 3-Substituted-4-oxoretinoic Acids Y. Fulmer Shealy, Carla A. Hosmer, James M. Riordan, John W. Wille, Tina S. Rogers, and Donald L. Hill pp 3051 - 3056; DOI: 10.1021/jm00045a009 |
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Synthesis of New Acyclic Pyrimidine Nucleoside Analogs as Potential Antiviral Drugs Kurt Eger, Eberhard M. Kluender, and Mathias Schmidt pp 3057 - 3061; DOI: 10.1021/jm00045a010 |
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Novel Dual Inhibitors of 5-Lipoxygenase and Thromboxane A2 Synthetase: Synthesis and Structure-Activity Relationships of 3-Pyridylmethyl-Substituted 2-Amino-6-hydroxybenzothiazole Derivatives Shigeki Hibi, Yasushi Okamoto, Katsuya Tagami, Hirotoshi Numata, Naoki Kobayashi, Masanobu Shinoda, Tetsuya Kawahara, Manabu Murakami, Kiyoshi Oketani, and et al. pp 3062 - 3070; DOI: 10.1021/jm00045a011 |
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Heteroaryl-Fused 2-Phenylisothiazolone Inhibitors of Cartilage Breakdown Stephen W. Wright, Joseph J. Petraitis, Matthew M. Abelman, Douglas G. Batt, Lori L. Bostrom, Ronald L. Corbett, Carl P. Decicco, Susan V. Di Meo, Bruce Freimark, and et al. pp 3071 - 3078; DOI: 10.1021/jm00045a012 |
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Inhibitors of HIV-1 Proteinase Containing 2-Heterosubstituted 4-Amino-3-hydroxy-5-phenylpentanoic Acid: Synthesis, Enzyme Inhibition, and Antiviral Activity Dieter Scholz, Andreas Billich, Brigitte Charpiot, Peter Ettmayer, Philipp Lehr, Brigitte Rosenwirth, Erwin Schreiner, and Hubert Gstach pp 3079 - 3089; DOI: 10.1021/jm00045a013 |
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Non-peptidic Inhibitors of Human Leukocyte Elastase. 1. The Design and Synthesis of Pyridone-Containing Inhibitors Peter Warner, Rosalyn C. Green, Bruce Gomes, and Anne M. Strimpler pp 3090 - 3099; DOI: 10.1021/jm00045a014 |
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Rational Design, Synthesis, and Crystallographic Analysis of a Hydroxyethylene-Based HIV-1 Protease Inhibitor Containing a Heterocyclic P1'-P2' Amide Bond Isostere Scott K. Thompson, Krishna H. M. Murthy, Baoguang Zhao, Evon Winborne, David W. Green, Seth M. Fisher, Renee L. DesJarlais, Thaddeus A. Jr. Tomaszek, Thomas D. Meek, and et al. pp 3100 - 3107; DOI: 10.1021/jm00045a015 |
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Bromobenzofuran-Based Non-peptide Antagonists of Angiotensin II: GR138950, a Potent Antihypertensive Agent with High Oral Bioavailability Duncan B. Judd, Michael D. Dowle, David Middlemiss, David I. C. Scopes, Barry C. Ross, Torquil I. Jack, Martin Pass, Elvira Tranquillini, Julie E. Hobson, and et al. pp 3108 - 3120; DOI: 10.1021/jm00045a016 |
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Synthesis and Opioid Activity of 7-Oxygenated 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolinols Chen-Yu Cheng, Ling-Wei Hsin, Ming-Cheng Tsai, William K. Schmidt, Christine Smith, and S. William Tam pp 3121 - 3127; DOI: 10.1021/jm00045a017 |
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Molecular Modeling Studies of Some Choline Acetyltransferase Inhibitors M. Kontoyianni, G. B. McGaughey, E. L. Stewart, C. J. Cavallito, and J. P. Bowen pp 3128 - 3131; DOI: 10.1021/jm00045a018 |
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Comparison of a DSB-120 DNA Interstrand Cross-Linked Adduct with the Corresponding Bis-tomaymycin Adduct: An Example of a Successful Template-Directed Approach to Drug Design Based upon the Monoalkylating Compound Tomaymycin John A. Mountzouris, Jeh-Jeng Wang, David Thurston, and Laurence H. Hurley pp 3132 - 3140; DOI: 10.1021/jm00045a019 |
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Docking Analysis of a Series of Benzylamino Acetylcholinesterase Inhibitors with a Phthalimide, Benzoyl, or Indanone Moiety Yoshio Yamamoto, Yuji Ishihara, and Irwin D. Kuntz pp 3141 - 3153; DOI: 10.1021/jm00045a020 |
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Sugar-Linked Dithiocarbamates as Modulators of Metabolic and Genotoxic Properties of N-Nitroso Compounds Byung-Hoon Lee, Barbara Bertram, Peter Schmezer, Norbert Frank, and Manfred Wiessler pp 3154 - 3162; DOI: 10.1021/jm00045a021 |
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A Marked Change of Receptor Affinity of the 2-Methyl-5-(3-hydroxyphenyl)morphans upon Attachment of an (E)-8-Benzylidene Moiety: Synthesis and Evaluation of a New Class of .sigma. Receptor Ligands Craig M. Bertha, Mariena V. Mattson, Judith L. Flippen-Anderson, Richard B. Rothman, Heng Xu, Xian-Yuan Cha, Karen Becketts, and Kenner C. Rice pp 3163 - 3170; DOI: 10.1021/jm00045a022 |
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Decapeptide Agonists of Human C5a: The Relationship between Conformation and Spasmogenic and Platelet Aggregatory Activities Sam D. Sanderson, Leonid Kirnarsky, Simon A. Sherman, Julia A. Ember, Angela M. Finch, and Stephen M. Taylor pp 3171 - 3180; DOI: 10.1021/jm00045a023 |
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Analogs of the Marine Immunosuppressant Microcolin A: Preparation and Biological Activity Frank E. Koehn, Oliver J. McConnell, Ross E. Longley, Susan H. Sennett, and John K. Reed pp 3181 - 3186; DOI: 10.1021/jm00045a024 |
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Tricyclic Analogs of Acyclovir and Ganciclovir. Influence of Substituents in the Heterocyclic Moiety on the Antiviral Activity Bozenna Golankiewicz, Tomasz Ostrowski, Graciela Andrei, Robert Snoeck, and Erik De Clercq pp 3187 - 3190; DOI: 10.1021/jm00045a025 |
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Inhibition of Topoisomerase I by Anthracycline Antibiotics: Evidence for General Inhibition of Topoisomerase I by DNA-Binding Agents Robert T. Crow and Donald M. Crothers pp 3191 - 3194; DOI: 10.1021/jm00045a026 |
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Comparative molecular field analysis of the antitumor activity of 9H-thioxanthen-9-one derivatives against pancreatic ductal carcinoma 03. [Erratum to document cited in CA120:315145] Jerome P. Horowitz, Irina Massova, Thomas E. Wiese, Brent H. Besler, and Thomas H. Corbett pp 3196 - 3196; DOI: 10.1021/jm00045a027 |
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Book Reviews pp 3195 - 3195; DOI: 10.1021/jm00045a600 |
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(+)-1-(3S,4R)-[3-(4-Phenylbenzyl)-4- hydroxychroman-7-yl]cyclopentane Carboxylic Acid, a Highly Potent, Selective Leukotriene B4 Antagonist with Oral Activity in the Murine Collagen-Induced Arthritis Model Kevin Koch, Lawrence S. Melvin Jr., Lawrence A. Reiter, Michael S. Biggers, Henry J. Showell, Richard J. Griffiths, E. Roy Pettipher, John B. Cheng, Anthony J. Milici, and et al. pp 3197 - 3199; DOI: 10.1021/jm00046a001 |
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Structure-Based Design of HIV Protease Inhibitors: 4-Hydroxycoumarins and 4-Hydroxy-2-pyrones as Non-peptidic Inhibitors Suvit Thaisrivongs, Paul K. Tomich, Keith D. Watenpaugh, Kong-Teck Chong, W. Jeffrey Howe, Chih-Ping Yang, Joseph W. Strohbach, Steve R. Turner, James P. McGrath, and et al. pp 3200 - 3204; DOI: 10.1021/jm00046a002 |
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"Glycylcyclines". 3. 9-Aminodoxycyclinecarboxamides Timothy C. Barden, Brian L. Buckwalter, Raymond T. Testa, Peter J. Petersen, and Ving J. Lee pp 3205 - 3211; DOI: 10.1021/jm00046a003 |
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Tridentate ligands containing the SNS donor atom set as a novel backbone for the development of technetium brain-imaging agents Spiros G. Mastrostamatis, Minas S. Papadopoulos, Ioannis C. Pirmettis, Evagelia Paschali, Alexandra D. Varvarigou, Chariklia I. Stassinopoulou, Cathrine P. Raptopoulou, Aris Terzis, and Efstratios Chiotellis pp 3212 - 3218; DOI: 10.1021/jm00046a004 |
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Synthesis, Binding Properties, and 18F Labeling of Fluorocarazolol, a High-Affinity .beta.-Adrenergic Receptor Antagonist Lei Zheng, Marc S. Berridge, and Paul Ernsberger pp 3219 - 3230; DOI: 10.1021/jm00046a005 |
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Synthesis and Structure-Activity Relationships of Novel Naphthalenic and Bioisosteric Related Amidic Derivatives as Melatonin Receptor Ligands Patrick Depreux, Daniel Lesieur, Hamid Ait Mansour, Peter Morgan, H. Edward Howell, Pierre Renard, Daniel-Henri Caignard, Bruno Pfeiffer, Philippe Delagrange, and et al. pp 3231 - 3239; DOI: 10.1021/jm00046a006 |
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Synthesis and Biological Activity of Bile Acid-Derived HMG-CoA Reductase Inhibitors. The Role of 21-Methyl in Recognition of HMG-CoA Reductase and the Ileal Bile Acid Transport System Guenther Wess, Werner Kramer, Xiao Bing Han, Klaus Bock, Alfons Enhsen, Heiner Glombik, Karl-Heinz Baringhaus, Georg Boeger, Matthias Urmann, and et al. pp 3240 - 3246; DOI: 10.1021/jm00046a007 |
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3-Amino-5,5-dimethylhexanoic Acid. Synthesis, Resolution, and Effects on Carnitine Acyltransferases Ahsraf Saeed, Jeanie B. McMillin, Paul E. Wolkowicz, and Wayne J. Brouillette pp 3247 - 3251; DOI: 10.1021/jm00046a008 |
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Synthesis and Structure-Activity Studies on Acidic Amino Acids and Related Diacids as NMDA Receptor Ligands Tommy N. Johansen, Karla Frydenvang, Bjarke Ebert, Povl Krogsgaard-Larsen, and Ulf Madsen pp 3252 - 3262; DOI: 10.1021/jm00046a009 |
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6,7,8,9-Tetrahydro-N,N-di-n-propyl-3H-benzindol-8-amines. Derivatives as Potent and Orally Active Serotonin 5-HT1A Receptor Agonists Peter Stjernloef, Thomas Elebring, Jonas Nilsson, Bengt Andersson, Soeren Lagerkvist, Kjell Svensson, Agneta Ekman, Arvid Carlsson, and Haakan Wikstroem pp 3263 - 3273; DOI: 10.1021/jm00046a010 |
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The Squalestatins: Novel Inhibitors of Squalene Synthase. Enzyme Inhibitory Activities and in vivo Evaluation of C1-Modified Analogs Panayiotis A. Procopiou, Esme J. Bailey, Mark J. Bamford, Andy P. Craven, Brian W. Dymock, John G. Houston, Julie L. Hutson, Barrie E. Kirk, Alun D. McCarthy, and et al. pp 3274 - 3281; DOI: 10.1021/jm00046a011 |
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Technetium-99m N,N'-Bis(2-mercapto-2-methylpropyl)-2-aminobenzylamine: Technetium-99m Complexes of a Novel Bis(aminoethanethiol) Ligand Lynn C. Francesconi, Yun Y. Yang, Mei-Ping Kung, Xiao X. Zhang, Jeffrey J. Billings, Yu-Zhi Guo, and Hank F. Kung pp 3282 - 3288; DOI: 10.1021/jm00046a012 |
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Bicyclic Hydantoins with a Bridgehead Nitrogen. Comparison of Anticonvulsant Activities with Binding to the Neuronal Voltage-Dependent Sodium Channel Wayne J. Brouillette, Vladimir P. Jestkov, Milton L. Brown, M. Shamim Akhtar, Timothy M. DeLorey, and George B. Brown pp 3289 - 3293; DOI: 10.1021/jm00046a013 |
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The Synthesis and Thymidylate Synthase Inhibitory Activity of L-.gamma.-L-Linked Dipeptide and L-.gamma.-Amide Analogs of 2-Desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583) Graham M. F. Bisset, Vassilios Bavetsias, Timothy J. Thornton, Krzysztof Pawelczak, A. Hilary Calvert, Leslie R. Hughes, and Ann L. Jackman pp 3294 - 3302; DOI: 10.1021/jm00046a014 |
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Nonpeptidic Inhibitors of Human Leukocyte Elastase. 2. Design, Synthesis, and in vitro Activity of a Series of 3-Amino-6-aryl-2-oxopyridyl Trifluoromethyl Ketones James R. Damewood Jr., Philip D. Edwards, Scott Feeney, Bruce C. Gomes, Gary B. Steelman, Paul A. Tuthill, Joseph C. Williams, Peter Warner, Sheila A. Woolson, and et al. pp 3303 - 3312; DOI: 10.1021/jm00046a015 |
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Nonpeptidic Inhibitors of Human Leukocyte Elastase. 3. Design, Synthesis, X-ray Crystallographic Analysis, and Structure-Activity Relationships for a Series of Orally Active 3-Amino-6-phenyl-2-pyridinyl Trifluoromethyl Ketones Peter R. Bernstein, Don Andisik, Prudence K. Bradley, Craig B. Bryant, Christopher Ceccarelli, James R. Damewood Jr., Roger Earley, Philip D. Edwards, Scott Feeney, and et al. pp 3313 - 3326; DOI: 10.1021/jm00046a016 |
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(E)-3-[[[[6-(2-Carboxyethenyl)-5-[[8-(4-methoxyphenyl)octyl]oxy]-2-pyridinyl]methyl]thio]methyl]benzoic Acid and Related Compounds: High Affinity Leukotriene B4 Receptor Antagonists Robert A. Daines, Pamela A. Chambers, Drake S. Eggleston, James J. Foley, Don E. Griswold, R. Curtis Haltiwanger, Dalia R. Jakas, William D. Kingsbury, Lenox D. Martin, and et al. pp 3327 - 3336; DOI: 10.1021/jm00046a017 |
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The Effect of the Aromatic Rings of Taxol on Biological Activity and Solution Conformation: Synthesis and Evaluation of Saturated Taxol and Taxotere Analogs Thomas C. Boge, Richard H. Himes, David G. Vander Velde, and Gunda I. Georg pp 3337 - 3343; DOI: 10.1021/jm00046a018 |
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(Fluorocyclopropyl)quinolones. 2. Synthesis and Stereochemical Structure-Activity Relationships of Chiral 7-(7-Amino-5-azaspiro[2.4]heptan-5-yl)-1-(2-fluorocyclopropyl)quinolone Antibacterial Agents Youichi Kimura, Shohgo Atarashi, Katsuhiro Kawakami, Kenichi Sato, and Isao Hayakawa pp 3344 - 3352; DOI: 10.1021/jm00046a019 |
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Synthesis and Biochemical Evaluation of a Series of Aminoflavones as Potential Inhibitors of Protein-Tyrosine Kinases p56lck, EGFr, and p60v-src Mark Cushman, Helen Zhu, Robert L. Geahlen, and Alan J. Kraker pp 3353 - 3362; DOI: 10.1021/jm00046a020 |
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Design, Synthesis, and Biological Activity of Methoctramine-Related Tetraamines Bearing a 11-Acetyl-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one Moiety: Structural Requirements for Optimum Occupancy of Muscarinic Receptor Subtypes As Revealed by Symmetrical and Unsymmetrical Polyamines Anna Minarini, Maria L. Bolognesi, Roberta Budriesi, Marco Canossa, Alberto Chiarini, Santi Spampinato, and Carlo Melchiorre pp 3363 - 3372; DOI: 10.1021/jm00046a021 |
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Structure-Activity Relationships of 1,3-Dialkylxanthine Derivatives at Rat A3 Adenosine Receptors Hea Ok Kim, Xiao-duo Ji, Neli Melman, Mark E. Olah, Gary L. Stiles, and Kenneth A. Jacobson pp 3373 - 3382; DOI: 10.1021/jm00046a022 |
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Synthetic Laminin-like Peptides and Pseudopeptides as Potential Antimetastatic Agents Ming Zhao, Hynda K. Kleinman, and Michael Mokotoff pp 3383 - 3388; DOI: 10.1021/jm00046a023 |
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Conformationally Locked Nucleoside Analogs. Synthesis of Dideoxycarbocyclic Nucleoside Analogs Structurally Related to Neplanocin C Juan B. Rodriguez, Victor E. Marquez, Marc C. Nicklaus, Hiroaki Mitsuya, and Joseph J. Barchi pp 3389 - 3399; DOI: 10.1021/jm00046a024 |
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Antitumor Agents 155. Synthesis and Biological Evaluation of 3',6,7-Substituted 2-Phenyl-4-quinolones as Antimicrotubule Agents Leping Li, Hui-Kang Wang, Sheng-Chu Kuo, Tian-Shung Wu, Anthony Mauger, Chii M. Lin, Ernest Hamel, and Kuo-Hsiung Lee pp 3400 - 3407; DOI: 10.1021/jm00046a025 |
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Antipodal .alpha.-N-(Methyl through Decyl)-N-normetazocines (5,9.alpha.-Dimethyl-2'-hydroxy-6,7-benzomorphans): In vitro and In vivo Properties Everette L. May, Mario D. Aceto, Edward R. Bowman, Christine Bentley, Billy R. Martin, Louis S. Harris, Fedor Medzihradsky, Mariena V. Mattson, and Arthur E. Jacobson pp 3408 - 3418; DOI: 10.1021/jm00046a026 |
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Polyacrylamides Bearing Pendant .alpha.-Sialoside Groups Strongly Inhibit Agglutination of Erythrocytes by Influenza A Virus: Multivalency and Steric Stabilization of Particulate Biological Systems Watson J. Lees, Andrew Spaltenstein, Jill E. Kingery-Wood, and George M. Whitesides pp 3419 - 3433; DOI: 10.1021/jm00046a027 |
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Synthesis and Pharmacological Evaluation of Isoindolo[1,2-b]quinazolinone and Isoindolo[2,1-a]benzimidazole Derivatives Related to the Antitumor Agent Batracylin Sanath K. Meegalla, Gregory J. Stevens, Charlene A. McQueen, Allan Y. Chen, Chiang Yu, Leroy F. Liu, Louis R. Barrows, and Edmond J. LaVoie pp 3434 - 3439; DOI: 10.1021/jm00046a028 |
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Structure-Activity Relationship Studies of N-Sulfonyl Analogs of Cocaine: Role of Ionic Interaction in Cocaine Binding Alan P. Kozikowski, M. K. Eddine Saiah, John S. Bergmann, and Kenneth M. Johnson pp 3440 - 3442; DOI: 10.1021/jm00046a029 |
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L-735,524: The Design of a Potent and Orally Bioavailable HIV Protease Inhibitor Bruce D. Dorsey, Rhonda B. Levin, Stacy L. McDaniel, Joseph P. Vacca, James P. Guare, Paul L. Darke, Joan A. Zugay, Emilio A. Emini, William A. Schleif, and et al. pp 3443 - 3451; DOI: 10.1021/jm00047a001 |
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Self-Immolative Prodrugs: Candidates for Antibody-Directed Enzyme Prodrug Therapy in Conjunction with a Nitroreductase Enzyme Anthony B. Mauger, Philip J. Burke, Hanif H. Somani, Frank Friedlos, and Richard J. Knox pp 3452 - 3458; DOI: 10.1021/jm00047a002 |
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Structure-Activity Relationships of Sialyl Lewis x-Containing Oligosaccharides. 1. Effect of Modifications of the Fucose Moiety John Y. Ramphal, Zhong-Li Zheng, Carl Perez, Leslie E. Walker, Shawn A. DeFrees, and Federico C. A. Gaeta pp 3459 - 3463; DOI: 10.1021/jm00047a003 |
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Antiproliferative Properties of Polyamine Analogs: A Structure-Activity Study Raymond J. Bergeron, James S. McManis, Charles Z. Liu, Yang Feng, William R. Weimar, Gabriel R. Luchetta, Qianhong Wu, Jackqueline Ortiz-Ocasio, J. R. Timothy Vinson, and et al. pp 3464 - 3476; DOI: 10.1021/jm00047a004 |
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Structure-Activity Study of Neuropeptide FF: Contribution of N-Terminal Regions to Affinity and Activity Sophie Gicquel, Honore Mazarguil, Corinne Desprat, Michele Allard, Jean-Philippe Devillers, Guy Simonnet, and Jean-Marie Zajac pp 3477 - 3481; DOI: 10.1021/jm00047a005 |
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Selective .kappa.-Opioid Agonists: Synthesis and Structure-Activity Relationships of Piperidines Incorporating an Oxo-Containing Acyl Group Giuseppe Giardina, Geoffrey D. Clarke, Giulio Dondio, Giuseppe Petrone, Massimo Sbacchi, and Vittorio Vecchietti pp 3482 - 3491; DOI: 10.1021/jm00047a006 |
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Synthesis and Structure-Activity Relationships of Peptidyl .alpha.-Keto Heterocycles as Novel Inhibitors of Prolyl Endopeptidase Seiji Tsutsumi, Tsuneo Okonogi, Seiji Shibahara, Shokichi Ohuchi, Emiko Hatsushiba, Arthur A. Patchett, and Burton G. Christensen pp 3492 - 3502; DOI: 10.1021/jm00047a007 |
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Synthesis and Structure-Activity Relationship of Methyl-Substituted Indolo[2,3-b]quinolines: Novel Cytotoxic, DNA Topoisomerase II Inhibitors Wanda Peczynska-Czoch, Francois Pognan, Lukasz Kaczmarek, and Janusz Boratynski pp 3503 - 3510; DOI: 10.1021/jm00047a008 |
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Acyl CoA:Cholesterol Acyltransferase (ACAT) Inhibitors: Synthesis and Structure-Activity Relationship Studies of a New Series of Trisubstituted Imidazoles C. Anne Higley, Richard G. Wilde, Thomas P. Maduskuie, Alexander L. Johnson, Pennio Pennev, Jeffrey T. Billheimer, Candy S. Robinson, Peter J. Gillies, and Ruth R. Wexler pp 3511 - 3522; DOI: 10.1021/jm00047a009 |
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The Discovery and Structure-Activity Relationships of 1,2,3,6-Tetrahydro-4-phenyl-1-[(arylcyclohexenyl)alkyl]pyridines. Dopamine Autoreceptor Agonists and Potential Antipsychotic Agents Jon L. Wright, Bradley W. Caprathe, Dennis M. Downing, Shelly A. Glase, Thomas G. Heffner, Juan C. Jaen, Stephen J. Johnson, Suzanne R. Kesten, Robert G. MacKenzie, and et al. pp 3523 - 3533; DOI: 10.1021/jm00047a010 |
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Synthesis and Evaluation of the Anti-HIV Activity of Aza and Deaza Analogs of IsoddA and Their Phosphates as Prodrugs Palmarisa Franchetti, Loredana Cappellacci, Mario Grifantini, Lea Messini, Ghassan Abu Sheikha, Anna Giulia Loi, Enzo Tramontano, Antonella De Montis, Maria Grazia Spiga, and Paolo La Colla pp 3534 - 3541; DOI: 10.1021/jm00047a011 |
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Synthesis and Evaluation of Nicotine Analogs as Neuronal Nicotinic Acetylcholine Receptor Ligands Nan-Horng Lin, George M. Carrera, and David J. Anderson pp 3542 - 3553; DOI: 10.1021/jm00047a012 |
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Synthesis and Antiviral (HIV-1, HBV) Activities of 5-Halo-6-methoxy(or azido)-5,6-dihydro-3'-fluoro-3'-deoxythymidine Diastereomers. Potential Prodrugs to 3'-Fluoro-3'-deoxythymidine Rakesh Kumar, Lili Wang, Leonard I. Wiebe, and Edward E. Knaus pp 3554 - 3560; DOI: 10.1021/jm00047a013 |
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Small-Molecule Immunostimulants. Synthesis and Activity of 7,8-Disubstituted Guanosines and Structurally Related Compounds Allen B. Reitz, Michael G. Goodman, Barbara L. Pope, Dennis C. Argentieri, Stanley C. Bell, Levelle E. Burr, Erika Chourmouzis, Jon Come, Jacquelyn H. Goodman, and et al. pp 3561 - 3578; DOI: 10.1021/jm00047a014 |
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Nucleic Acid-Related Compounds. 84. Synthesis of 6'-(E and Z)-Halohomovinyl Derivatives of Adenosine, Inactivation of S-Adenosyl-L-homocysteine Hydrolase, and Correlation of Anticancer and Antiviral Potencies with Enzyme Inhibition Stanislaw F. Wnuk, Chong-Sheng Yuan, Ronald T. Borchardt, Jan Balzarini, Erik De Clercq, and Morris J. Robins pp 3579 - 3587; DOI: 10.1021/jm00047a015 |
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Agents Combining Thromboxane Receptor Antagonism with Thromboxane Synthase Inhibition: [[[2-(1H-Imidazol-1-yl)ethylidene]amino]oxy]alkanoic Acids Paolo Cozzi, Antonio Giordani, Maria Menichincheri, Antonio Pillan, Vittorio Pinciroli, Arsenia Rossi, Roberto Tonani, Daniele Volpi, Monica Tamburin, and et al. pp 3588 - 3604; DOI: 10.1021/jm00047a016 |
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Selective Inhibition of Trypanosomal Glyceraldehyde-3-phosphate Dehydrogenase by Protein Structure-Based Design: Toward New Drugs for the Treatment of Sleeping Sickness Christophe L. M. J. Verlinde, Mia Callens, Serge Van Calenbergh, Arthur Van Aerschot, Piet Herdewijn, Veronique Hannaert, Paul A. M. Michels, Fred R. Opperdoes, and Wim G. J. Hol pp 3605 - 3613; DOI: 10.1021/jm00047a017 |
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2-Substitution of N6-Benzyladenosine-5'-uronamides Enhances Selectivity for A3 Adenosine Receptors Hea O. Kim, Xiao-duo Ji, Suhaib M. Siddiqi, Mark E. Olah, Gary L. Stiles, and Kenneth A. Jacobson pp 3614 - 3621; DOI: 10.1021/jm00047a018 |
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Neuropeptide Y N-Terminal Deletion Fragments: Correlation between Solution Structure and Receptor Binding Activity at Y1 Receptors in Rat Brain Cortex Longqin Hu, Preeti Balse, and Michael B. Doughty pp 3622 - 3629; DOI: 10.1021/jm00047a019 |
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Influence of Lipophilicity on the Biological Activity of Cyclic Pseudopeptide NK-2 Receptor Antagonists Laura Quartara, Gaetano Fabbri, Renzo Ricci, Riccardo Patacchini, Vittorio Pestellini, Carlo Alberto Maggi, Vincenzo Pavone, Antonio Giachetti, and Federico Arcamone pp 3630 - 3638; DOI: 10.1021/jm00047a020 |
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Three-Dimensional Molecular Shape Analysis-Quantitative Structure-Activity Relationship of a Series of Cholecystokinin-A Receptor Antagonists John S. Tokarski and Anton J. Hopfinger pp 3639 - 3654; DOI: 10.1021/jm00047a021 |
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(4-[18F]Fluoro-3-iodobenzyl)guanidine, a Potential MIBG Analog for Positron Emission Tomography Ganesan Vaidyanathan, Donna J. Affleck, and Michael R. Zalutsky pp 3655 - 3662; DOI: 10.1021/jm00047a022 |
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Synthesis and 5-Lipoxygenase Inhibitory Activities of Some Novel 2-Substituted 5-Benzofuran Hydroxamic Acids Kwasi A. Ohemeng, Mary A. Appollina, Van N. Nguyen, Charles F. Schwender, Monica Singer, Michele Steber, Justin Ansell, Dennis Argentieri, and William Hageman pp 3663 - 3667; DOI: 10.1021/jm00047a023 |
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Synthesis of N-Acetylglucosamine-Modified ara-C and Its Effect on Ovarian Cancer Cells Hiroshi Fujimoto, Tsutomu Takayanagi, and Katsumi Ajisaka pp 3668 - 3670; DOI: 10.1021/jm00047a024 |
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A New Class of Non-peptidic Cholecystokinin-B/Gastrin Receptor Antagonists Based on Dibenzobicyclo[2.2.2]octane S. Barret Kalindjian, Michael J. Bodkin, Ildiko M. Buck, David J. Dunstone, Caroline M. R. Low, Iain M. McDonald, Michael J. Pether, and Katherine I. M. Steel pp 3671 - 3673; DOI: 10.1021/jm00048a001 |
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Improved Binding Affinity for Cyclophilin A by a Cyclosporin Derivative Singly Modified at Its Effector Domain Christos Papageorgiou, Andrea Florineth, and Vincent Mikol pp 3674 - 3676; DOI: 10.1021/jm00048a002 |
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Design, Synthesis, X-ray Analysis, and Dopamine Receptor-Modulating Activity of Mimics of the "C5" Hydrogen-Bonded Conformation in the Peptidomimetic 2-Oxo-3(R)-[(2(S)-pyrrolidinylcarbonyl)amino]-1-pyrrolidineacetamide Paul W. Baures, William H. Ojala, William B. Gleason, Ram K. Mishra, and Rodney L. Johnson pp 3677 - 3683; DOI: 10.1021/jm00048a003 |
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Design, Synthesis, and Conformational Analysis of a Novel Macrocyclic HIV-Protease Inhibitor Brent L. Podlogar, Robert A. Farr, Dirk Friedrich, Celine Tarnus, Edward W. Huber, Robert J. Cregge, and Daniel Schirlin pp 3684 - 3692; DOI: 10.1021/jm00048a004 |
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Synthesis and Diuretic Activity of Alkyl- and Arylguanidine Analogs of N,N'-Dicyclohexyl-4-morpholinecarboxamidine in Rats and Dogs Sam C. Perricone, Stephen J. Humphrey, Louis L. Skaletzky, Boyd E. Graham, Ralph A. Zandt, and Gerald R. Zins pp 3693 - 3700; DOI: 10.1021/jm00048a005 |
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Nitrogen-in-the-Ring Pyranoses and Furanoses: Structural Basis of Inhibition of Mammalian Glycosidases Naoki Asano, Kengo Oseki, Haruhisa Kizu, and Katsuhiko Matsui pp 3701 - 3706; DOI: 10.1021/jm00048a006 |
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Synthesis and Structure-Activity Relationships of a Series of Penicillin-Derived HIV Proteinase Inhibitors: Heterocyclic Ring Systems Containing P1' and P2' Substituents John Kitchin, Richard C. Bethell, Nicholas Cammack, Simon Dolan, Derek N. Evans, Stuart Holman, Duncan S. Holmes, Peter McMeekin, Chi L. Mo, and et al. pp 3707 - 3716; DOI: 10.1021/jm00048a007 |
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Synthesis and Structure-Activity Relationships in a Series of Antiinflammatory Corticosteroid Analogs, Halomethyl Androstane-17.beta.-carbothioates and -17.beta.-carboselenoates Gordon H. Phillipps, Esme J. Bailey, Brian M. Bain, Raymond A. Borella, Jacky B. Buckton, John C. Clark, Alice E. Doherty, Alan F. English, Harold Fazakerley, and et al. pp 3717 - 3729; DOI: 10.1021/jm00048a008 |
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Synthesis and Biological Activity of 2-Hydroxy and 2-Alkoxy Analogs of 1.alpha.,25-Dihydroxy-19-norvitamin D3 Rafal R. Sicinski, Kato L. Perlman, and Hector F. DeLuca pp 3730 - 3738; DOI: 10.1021/jm00048a009 |
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Novel Acyclic Nucleotides and Nucleoside 5'-Triphosphates Imitating 2',3'-Dideoxy-2',3'-didehydro nucleotides: Synthesis and Biological Properties Elena A. Shirokova, Natalia B. Tarussova, Alexander V. Shipitsin, Dmitry G. Semizarov, and Alexander A. Krayevsky pp 3739 - 3748; DOI: 10.1021/jm00048a010 |
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Generally Applicable, Convenient Solid-Phase Synthesis and Receptor Affinities of Octreotide Analogs W. Barry Edwards, Cynthia G. Fields, Carolyn J. Anderson, Tammy S. Pajeau, Michael J. Welch, and Gregg B. Fields pp 3749 - 3757; DOI: 10.1021/jm00048a011 |
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Analysis of linear and nonlinear QSAR data using neural networks David T. Manallack, Dianne D. Ellis, and David J. Livingstone pp 3758 - 3767; DOI: 10.1021/jm00048a012 |
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A generalized formalism of three-dimensional quantitative structure-property relationship analysis for flexible molecules using tensor representation A. J. Hopfinger, Benjamin J. Burke, and William J. Dunn pp 3768 - 3774; DOI: 10.1021/jm00048a013 |
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Construction of a molecular shape analysis: three-dimensional quantitative structure-activity relationship for an analog series of pyridobenzodiazepinone inhibitors of muscarinic 2 and 3 receptors Benjamin J. Burke, William J. III Dunn, and William J. Dunn pp 3775 - 3788; DOI: 10.1021/jm00048a014 |
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5-Phenyl-3-ureidobenzazepin-2-ones as Cholecystokinin-B Receptor Antagonists John A. Lowe, David L. Hageman, Susan E. Drozda, Stafford McLean, Dianne K. Bryce, Rosemary T. Crawford, Stevin Zorn, Jean Morrone, and Jon Bordner pp 3789 - 3811; DOI: 10.1021/jm00048a015 |
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Peptide-Linked 1,3-Dialkyl-3-acyltriazenes: Gastrin Receptor Directed Antineoplastic Alkylating Agents Brigitte F. Schmidt, Lidia Hernandez, Carol Rouzer, Grzegorz Czerwinski, Gwendolyn Chmurny, and Christopher J. Michejda pp 3812 - 3818; DOI: 10.1021/jm00048a016 |
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Inhibition of Topoisomerase II Catalytic Activity by Pyridoacridine Alkaloids from a Cystodytes sp. Ascidian: A Mechanism for the Apparent Intercalator-Induced Inhibition of Topoisomerase II Leonard A. McDonald, Glenn S. Eldredge, Louis R. Barrows, and Chris M. Ireland pp 3819 - 3827; DOI: 10.1021/jm00048a017 |
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Synthesis and Antimicrobial Activity of Novel [(3-Aminopyrimidiniumyl)thio]methyl Cephalosporins Yong-Zu Kim, Jong-Chan Lim, Jae-Hong Yeo, Chan-Sik Bang, Won-Sup Kim, Sam-Sik Kim, Yong-Min Woo, Duck-Ho Yang, Hunseung Oh, and Keepyung Nahm pp 3828 - 3833; DOI: 10.1021/jm00048a018 |
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Cyclopropamitosenes, Novel Bioreductive Anticancer Agents. Synthesis, Electrochemistry, and Biological Activity of 7-Substituted Cyclopropamitosenes and Related Indolequinones Ann S. Cotterill, Christopher J. Moody, Roger J. Mortimer, Claire L. Norton, Noeleen O'Sullivan, Miriam A. Stephens, Nelson R. Stradiotto, Elizabeth Swann, and Ian J. Stratford pp 3834 - 3843; DOI: 10.1021/jm00048a019 |
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Adenosine Deaminase Inhibitors. Synthesis and Biological Evaluation of Putative Metabolites of (+)-erythro-9-(2S-Hydroxy-3R-nonyl)adenine Chandra Vargeese, Mallela S. P. Sarma, Palle V. P. Pragnacharyulu, Elie Abushanab, Shih-Ying Li, and Johanna D. Stoeckler pp 3844 - 3849; DOI: 10.1021/jm00048a020 |
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The Synthesis of Nucleoside 5'-O-(1,1-Dithiotriphosphates) Andrzej Okruszek, Magdalena Olesiak, and Jan Balzarini pp 3850 - 3854; DOI: 10.1021/jm00048a021 |
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Binding of Fluorescent and Spin-Labeled C-Terminal Hirudin Analogs to Thrombin Sornampillai Sankarapandi, Judith K. Woodford, John L. Krstenansky, and Lawrence J. Berliner pp 3855 - 3858; DOI: 10.1021/jm00048a022 |
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Book Reviews pp 3859 - 3862; DOI: 10.1021/jm00048a600 |
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Aspartyl .alpha.-((1-Phenyl-3-(trifluoromethyl)- pyrazol-5-yl)oxy)methyl Ketones as Interleukin-1.beta. Converting Enzyme Inhibitors. Significance of the P1 and P3 Amido Nitrogens for Enzyme-Peptide Inhibitor Binding Roland E. Dolle, Jasbir Singh, James Rinker, Denton Hoyer, C. V. C. Prasad, Todd L. Graybill, Joseph M. Salvino, Carla T. Helaszek, Robert E. Miller, and Mark A. Ator pp 3863 - 3866; DOI: 10.1021/jm00049a001 |
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(-)-11-Hydroxy-7'-isothiocyanato-1',1'- dimethylheptyl-.DELTA.8-THC: A Novel, High-Affinity Irreversible Probe for the Cannabinoid Receptor in the Brain Yan Guo, Vasiliki Abadji, Kelley L. Morse, Donna J. Fournier, Xiuyan Li, and Alexandros Makriyannis pp 3867 - 3870; DOI: 10.1021/jm00049a002 |
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4,7.beta.-Dimethyl-4-azacholestan-3-one (MK-386) and Related 4-Azasteroids as Selective Inhibitors of Human Type 1 5.alpha.-Reductase Raman K. Bakshi, Gool F. Patel, Gary H. Rasmusson, Walter F. Baginsky, George Cimis, Kenneth Ellsworth, Benedict Chang, Herb Bull, Richard L. Tolman, and Georgianna S. Harris pp 3871 - 3874; DOI: 10.1021/jm00049a003 |
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Synthesis, Cocaine Receptor Affinity, and Dopamine Uptake Inhibition of Several New 2.beta.-Substituted 3.beta.-Phenyltropanes Shreekrishna V. Kelkar, Sari Izenwasser, Jonathan L. Katz, Cheryl L. Klein, Naijue Zhu, and Mark L. Trudell pp 3875 - 3877; DOI: 10.1021/jm00049a004 |
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Selective Cyclooxygenase Inhibitors: Novel 1,2-Diarylcyclopentenes Are Potent and Orally Active COX-2 Inhibitors David B. Reitz, James J. Li, Monica B. Norton, Emily J. Reinhard, Joe T. Collins, Gary D. Anderson, Susan A. Gregory, Carol M. Koboldt, William E. Perkins, and et al. pp 3878 - 3881; DOI: 10.1021/jm00049a005 |
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Orally Active Non-Peptide Fibrinogen Receptor (GpIIb/IIIa) Antagonists: Identification of 4-[4-[4-(Aminoimino methyl)phenyl]-1-piperazinyl]-1- piperidineacetic Acid as a Long-Acting, Broad-Spectrum Antithrombotic Agent Colin D. Eldred, Brian Evans, Sean Hindley, Brian D. Judkins, Henry A. Kelly, John Kitchin, Philip Lumley, Barry Porter, Barry C. Ross, and et al. pp 3882 - 3885; DOI: 10.1021/jm00049a006 |
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L-N6-(1-Iminoethyl)lysine: A Selective Inhibitor of Inducible Nitric Oxide Synthase William M. Moore, R. Keith Webber, Gina M. Jerome, Foe S. Tjoeng, Thomas P. Misko, and Mark G. Currie pp 3886 - 3888; DOI: 10.1021/jm00049a007 |
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Design and Synthesis of Potent and Highly Selective Thrombin Inhibitors Kurt Hilpert, Jean Ackermann, David W. Banner, Alain Gast, Klaus Gubernator, Paul Hadvary, Ludvik Labler, Klaus Mueller, Gerard Schmid, and et al. pp 3889 - 3901; DOI: 10.1021/jm00049a008 |
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Synthesis and Antitumor Evaluation of Bis[(pivaloyloxy)methyl] 2'-Deoxy-5-fluorouridine 5'-Monophosphate (FdUMP): A Strategy To Introduce Nucleotides into Cells David Farquhar, Saeed Khan, Devendra N. Srivastva, and Priscilla P. Saunders pp 3902 - 3909; DOI: 10.1021/jm00049a009 |
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Design, Synthesis, and Biological Properties of highly Potent Cyclic Dynorphin A Analogs. Analogs Cyclized between Positions 5 and 11 Jean-Philippe Meyer, Nathan Collins, Feng-Di Lung, Peg Davis, Teresa Zalewska, Frank Porreca, Henry I. Yamamura, and Victor J. Hruby pp 3910 - 3917; DOI: 10.1021/jm00049a010 |
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Unambiguous Total Synthesis of the Enantiomers of myo-Inositol 1,3,4-Trisphosphate: 1L-myo-Inositol 1,3,4-Trisphosphate Mobilizes Intracellular Ca2+ in Limulus Photoreceptors Andrew M. Riley, Richard Payne, and Barry V. L. Potter pp 3918 - 3927; DOI: 10.1021/jm00049a011 |
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Nonpeptide Angiotensin II Receptor Antagonists. Synthesis, in vitro Activity, and Molecular Modeling Studies of N-[(Heterobiaryl)methyl]imidazoles Aldo Salimbeni, Renato Canevotti, Fabio Paleari, Fabrizio Bonaccorsi, Anna R. Renzetti, Laura Belvisi, Gianpaolo Bravi, and Carlo Scolastico pp 3928 - 3938; DOI: 10.1021/jm00049a012 |
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Synthesis of Oxadiazolidinedione Derivatives as Quisqualic Acid Analogs and Their Evaluation at a Quisqualate-Sensitized Site in the Rat Hippocampus Shankar Venkatraman, Robert J. Roon, Marvin K. Schulte, James F. Koerner, and Rodney L. Johnson pp 3939 - 3946; DOI: 10.1021/jm00049a013 |
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Anti-AIDS Agents. 15. Synthesis and Anti-HIV Activity of Dihydroseselins and Related Analogs Li Huang, Yoshiki Kashiwada, L. Mark Cosentino, Sharon Fan, Chin-Ho Chen, Andrew T. McPhail, Toshihiro Fujioka, Kunihide Mihashi, and Kuo-Hsiung Lee pp 3947 - 3955; DOI: 10.1021/jm00049a014 |
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Tricyclic Quinoxalinediones: 5,6-Dihydro-1H-pyrrolo[1,2,3-de]quinoxaline-2,3-diones and 6,7-Dihydro-1H,5H-pyrido[1,2,3-de]quinoxaline-2,3-diones as Potent Antagonists for the Glycine Binding Site of the NMDA Receptor Ryu Nagata, Norihiko Tanno, Toru Kodo, Nobuyuki Ae, Hiroshi Yamaguchi, Tamiki Nishimura, Fujio Antoku, Tohru Tatsuno, Terufumi Kato, and et al. pp 3956 - 3968; DOI: 10.1021/jm00049a015 |
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Dipeptide Phosphonates as Inhibitors of Dipeptidyl Peptidase IV Bogdan Boduszek, Jozef Oleksyszyn, Chih-Min Kam, Joe Selzler, Robert E. Smith, and James C. Powers pp 3969 - 3976; DOI: 10.1021/jm00049a016 |
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[[.omega.-(Heterocyclylamino)alkoxy]benzyl]-2,4-thiazolidinediones as potent antihyperglycemic agents Barrie C. C. Cantello, Michael A. Cawthorne, Graham P. Cottam, Peter T. Duff, David Haigh, Richard M. Hindley, Carolyn A. Lister, Stephen A. Smith, and Peter L. Thurlby pp 3977 - 3985; DOI: 10.1021/jm00049a017 |
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Chemical and Biological Evaluation of Hydrolysis Products of Cyclophosphamide Veronique Gilard, Robert Martino, Marie-C. Malet-Martino, Bernhard Kutscher, Arndt Mueller, Ulf Niemeyer, Joerg Pohl, and Emmanuel E. Polymeropoulos pp 3986 - 3993; DOI: 10.1021/jm00049a018 |
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PRO_LIGAND: An Approach to de Novo Molecular Design. 2. Design of Novel Molecules from Molecular Field Analysis (MFA) Models and Pharmacophores Bohdan Waszkowycz, David E. Clark, David Frenkel, Jin Li, Christopher W. Murray, Barry Robson, and David R. Westhead pp 3994 - 4002; DOI: 10.1021/jm00049a019 |
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Cephem Sulfones as Inactivators of Human Leukocyte Elastase. 5. 7.alpha.-Methoxy- and 7.alpha.-Chloro-1,1-dioxocephem 4-Ketones Marco Alpegiani, Pierluigi Bissolino, Riccardo Corigli, Stefano Del Nero, Ettore Perrone, Vincenzo Rizzo, Nereo Sacchi, Giuseppe Cassinelli, Giovanni Franceschi, and Antonio Baici pp 4003 - 4019; DOI: 10.1021/jm00049a020 |
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Selective Ligands for Rat A3 Adenosine Receptors: Structure-Activity Relationships of 1,3-Dialkylxanthine 7-Riboside Derivatives Hea Ok Kim, Xiao-duo Ji, Neli Melman, Mark E. Olah, Gary L. Stiles, and Kenneth A. Jacobson pp 4020 - 4030; DOI: 10.1021/jm00049a021 |
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Structure-Activity Relationships of C1 and C6 Side Chains of Zaragozic Acid A Derivatives Mitree M. Ponpipom, Narindar N. Girotra, Robert L. Bugianesi, Cathleen D. Roberts, Gregory D. Berger, Robert M. Burk, Robert W. Marquis, William H. Parsons, Kenneth F. Bartizal, and et al. pp 4031 - 4051; DOI: 10.1021/jm00049a022 |
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Book Reviews pp 4152 - 4152; DOI: 10.1021/jm00049a600 |
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The Glycine Site on the NMDA Receptor: Structure-Activity Relationships and Therapeutic Potential Paul D. Leeson and Leslie L. Iversen pp 4053 - 4067; DOI: 10.1021/jm00050a001 |
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A Highly Potent, Orally Active Imidazo[4,5-b]pyridine Biphenyl Acylsulfonamide (MK-996; L-159,282): A New AT1-Selective Angiotensin II Receptor Antagonist Prasun K. Chakravarty, Elizabeth M. Naylor, Anna Chen, Raymond S. L. Chang, Tsing-Bau Chen, Kristy A. Faust, Victor J. Lotti, Salah D. Kivlighn, Robert A. Gable, and et al. pp 4068 - 4072; DOI: 10.1021/jm00050a002 |
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GC Sequence Specific Recognition by an N-Formamido, C-Terminus-Modified and Imidazole-Containing Analog of Netropsin Moses Lee, Christopher S. Preti, Emily Vinson, Michael D. Wyatt, and John A. Hartley pp 4073 - 4075; DOI: 10.1021/jm00050a003 |
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Multisubstrate Inhibition of 4-Hydroxybenzoate 3-Monooxygenase Francesco G. Salituro, David A. Demeter, Herschel J. R. Weintraub, Bruce J. Lippert, Robert J. Resvick, and Ian A. McDonald pp 4076 - 4078; DOI: 10.1021/jm00050a004 |
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Novel Antiproliferative Agents Derived from Lavendustin A Peter Nussbaumer, Anthony P. Winiski, Salvatore Cammisuli, Peter Hiestand, Gisbert Weckbecker, and Anton Stuetz pp 4079 - 4084; DOI: 10.1021/jm00050a005 |
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Bioisosteres of Arecoline: 1,2,3,6-Tetrahydro-5-pyridyl-Substituted and 3-Piperidyl-Substituted Derivatives of Tetrazoles and 1,2,3-Triazoles. Synthesis and Muscarinic Activity Ejner K. Moltzen, Henrik Pedersen, Klaus P. Boegesoe, Eddi Meier, Kristen Frederiksen, Connie Sanchez, and Hanne Loeve Lemboel pp 4085 - 4099; DOI: 10.1021/jm00050a006 |
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A Comparative Molecular Field Analysis Model for 6-Arylpyrrolo[2,1-d][1,5]benzothiazepines Binding Selectively to the Mitochondrial Benzodiazepine Receptor Giovanni Greco, Ettore Novellino, Isabella Fiorini, Vito Nacci, Giuseppe Campiani, Silvia M. Ciani, Antonio Garofalo, Paola Bernasconi, and Tiziana Mennini pp 4100 - 4108; DOI: 10.1021/jm00050a007 |
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Conformational Analysis, Pharmacophore Identification, and Comparative Molecular Field Analysis of Ligands for the Neuromodulatory .sigma.3 Receptor Andrew M. Myers, Paul S. Charifson, Constance E. Owens, Nora S. Kula, Andrew T. McPhail, Ross J. Baldessarini, Raymond G. Booth, and Steven D. Wyrick pp 4109 - 4117; DOI: 10.1021/jm00050a008 |
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Substrate Specificity in Short-Chain Phospholipid Analogs at the Active Site of Human Synovial Phospholipase A2 T. N. Wheeler, Steven G. Blanchard, Frank Fang, Yolanda Gray-Nunez, Cole O. Harris, Millard H. Lambert, Mukund M. Mehrotra, Derek J. Parks, R. C. Andrew, and et al. pp 4118 - 4129; DOI: 10.1021/jm00050a009 |
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Molecular Similarity Indices in a Comparative Analysis (CoMSIA) of Drug Molecules to Correlate and Predict Their Biological Activity Gerhard Klebe, Ute Abraham, and Thomas Mietzner pp 4130 - 4146; DOI: 10.1021/jm00050a010 |
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Syntheses of Racemic and Nearly Optically Pure Ether Lipids and Evaluation of in vitro Antineoplastic Activities Richard I. Duclos, Hwa Hwoy Chia, Osama H. Abdelmageed, Henry Esber, Donna J. Fournier, and Alexandros Makriyannis pp 4147 - 4154; DOI: 10.1021/jm00050a011 |
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The Synthesis and in vitro Evaluation of a 99mTechnetium-Nitroimidazole Complex Based on a Bis(amine-phenol) Ligand: Comparison to BMS-181321 K. Ramalingam, N. Raju, P. Nanjappan, K. E. Linder, J. Pirro, W. Zeng, W. Rumsey, D. P. Nowotnik, and A. D. Nunn pp 4155 - 4163; DOI: 10.1021/jm00050a012 |
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Quantitative Structure-Activity Relationships/Comparative Molecular Field Analysis (QSAR/CoMFA) for Receptor-Binding Properties of Halogenated Estradiol Derivatives Tsvetan G. Gantchev, Hasrat Ali, and Johan E. van Lier pp 4164 - 4176; DOI: 10.1021/jm00050a013 |
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An Evaluation of the Antirhinoviral Activity of Acylfuran Replacements for 3-Methylisoxazoles. Are 2-Acetylfurans Bioisosteres for 3-Methylisoxazoles? Thomas R. Bailey, Guy D. Diana, John P. Mallamo, Niranjan Vescio, Tandy L. Draper, Philip M. Carabateas, Melody A. Long, Vincent L. Giranda, Frank J. Dutko, and Daniel C. Pevear pp 4177 - 4184; DOI: 10.1021/jm00050a014 |
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1,2,3-Triazole-[2,5-Bis-O-(tert-butyldimethylsilyl)-.beta.-D-ribofuranosyl]-3'-spiro-5''-(4''-amino-1'',2''-oxathiole 2'',2''-dioxide) (TSAO) Analogs: Synthesis and Anti-HIV-1 Activity Rosa Alvarez, Sonsoles Velazquez, Ana San-Felix, Stefano Aquaro, Erik De Clercq, Carlo-Federico Perno, Anna Karlsson, Jan Balzarini, and Maria Jose Camarasa pp 4185 - 4194; DOI: 10.1021/jm00050a015 |
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7-Azetidinylquinolones as Antibacterial Agents. 2. Synthesis and Biological Activity of 7-(2,3-Disubstituted-1-azetidinyl)-4-oxoquinoline- and -1,8-naphthyridine-3-carboxylic Acids. Properties and Structure-Activity Relationships of Quinolones with an Azetidine Moiety Jordi Frigola, Antoni Torrens, Jose A. Castrillo, Josep Mas, David Vano, Juana M. Berrocal, Carme Calvet, Leonardo Salgado, Jordi Redondo, and et al. pp 4195 - 4210; DOI: 10.1021/jm00050a016 |
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Structure-Activity Relationships and pH Dependence of Binding of 8-Alkyl-N5-Deazapterins to Dihydrofolate Reductase Michael T. G. Ivery and Jill E. Gready pp 4211 - 4221; DOI: 10.1021/jm00050a017 |
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Latent Alkyl Isocyanates as Inhibitors of Aldehyde Dehydrogenase in vivo Herbert T. Nagasawa, James A. Elberling, David J. W. Goon, and Frances N. Shirota pp 4222 - 4226; DOI: 10.1021/jm00050a018 |
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Androgen Receptor Affinity of 5'-Acyl Furanosteroids Virendra Kumar, James H. Ackerman, Michael D. Alexander, Malcolm R. Bell, Robert G. Christiansen, Jen S. Dung, Edward P. Jaeger, John L. Herrmann Jr., Michael E. Krolski, and et al. pp 4227 - 4236; DOI: 10.1021/jm00050a019 |
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Effect of Molecular Manipulation on the Estrogenic Activity of a Brain-Targeting Estradiol Chemical Delivery System Marcus E. Brewster, M. Scott M. Bartruff, Wesley R. Anderson, Pascal J. Druzgala, Nicholas Bodor, and Emil Pop pp 4237 - 4244; DOI: 10.1021/jm00050a020 |
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Iodinated 2-Aminotetralins and 3-Amino-1-benzopyrans: Ligands for Dopamine D2 and D3 Receptors Sumalee Chumpradit, Mei-Ping Kung, Janet Vessotskie, Catherine Foulon, Mu Mu, and Hank F. Kung pp 4245 - 4250; DOI: 10.1021/jm00050a021 |
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Studies of the Active Conformation of a Novel Series of Benzamide Dopamine D2 Agonists David J. Wustrow, Lawrence D. Wise, Donna M. Cody, Robert G. MacKenzie, Lynn M. Georgic, Thomas A Pugsley, and Thomas G. Heffner pp 4251 - 4257; DOI: 10.1021/jm00050a022 |
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4-Deacetyltaxol and 10-Acetyl-4-deacetyltaxotere: Synthesis and Biological Evaluation Apurba Datta, Lalith R. Jayasinghe, and Gunda I. Georg pp 4258 - 4260; DOI: 10.1021/jm00050a023 |
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Book Reviews pp 4261 - 4262; DOI: 10.1021/jm00050a600 |
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Importance of Parallel Vectors and "Hydrophobic Collapse" of the Aligned Aromatic Rings: Discovery of a Potent Substance P Antagonist Manoj C. Desai, Lawrence A. Vincent, and James P. Rizzi pp 4263 - 4266; DOI: 10.1021/jm00051a001 |
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Novel Zinc Chelators Which Inhibit the Binding of HIV-EP1 (HIV Enhancer Binding Protein) to NF-.kappa.B Recognition Sequence Masami Otsuka, Mikako Fujita, Yukio Sugiura, Shunsuke Ishii, Tsutomu Aoki, Tadashi Yamamoto, and Jun-ichiro Inoue pp 4267 - 4269; DOI: 10.1021/jm00051a002 |
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Synthesis and Opioid Receptor Affinity of a Series of Aralkyl Ethers of 6.alpha.- and 6.beta.-Naltrexol Timothy D. Nelson, Ronda D. Davis, and Wendel L. Nelson pp 4270 - 4277; DOI: 10.1021/jm00051a003 |
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Cholinergic Agents Structurally Related to Furtrethonium. 2. Synthesis and Antimuscarinic Activity of a Series of N-[5-[(1'-Substituted-acetoxy)methyl]-2-furfuryl]dialkylamines Aldo Feriani, Giovanni Gaviraghi, Giancarlo Toson, Marco Mor, Annalisa Barbieri, Enzo Grana, Cinzia Boselli, Mario Guarneri, Daniele Simoni, and Stefano Manfredini pp 4278 - 4287; DOI: 10.1021/jm00051a004 |
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Synthesis, NMDA Receptor Antagonist Activity, and Anticonvulsant Action of 1-Aminocyclobutanecarboxylic Acid Derivatives Yehiel Gaoni, Astrid G. Chapman, Naila Parvez, Peter C.-K. Pook, David E. Jane, and Jeffrey C. Watkins pp 4288 - 4296; DOI: 10.1021/jm00051a005 |
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Synthesis, in vitro Biological Stability, and Anti-HIV Activity of 5-Halo-6-alkoxy(or azido)-5,6-dihydro-3'-azido-3'-deoxythymidine Diastereomers as Potential Prodrugs to 3'-Azido-3'-deoxythymidine (AZT) Rakesh Kumar, Lili Wang, Leonard I. Wiebe, and Edward E. Knaus pp 4297 - 4306; DOI: 10.1021/jm00051a006 |
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N6-Substituted Adenosine Receptor Agonists. Synthesis and Pharmacological Activity as Potent Antinociceptive Agents Timur Gungor, Patrice Malabre, Jean-Marie Teulon, Francoise Camborde, Joelle Meignen, Francoise Hertz, Angela Virone-Oddos, Francois Caussade, and Alix Cloarec pp 4307 - 4316; DOI: 10.1021/jm00051a007 |
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Synthesis and Molecular Modeling of 1-Phenyl-1,2,3,4-tetrahydroisoquinolines and Related 5,6,8,9-Tetrahydro-13bH-dibenzo[a,h]quinolizines as D1 Dopamine Antagonists Deborah L. Minor, Steven D. Wyrick, Paul S. Charifson, Val J. Watts, David E. Nichols, and Richard B. Mailman pp 4317 - 4328; DOI: 10.1021/jm00051a008 |
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Synthesis and Antitumor Activity of a New Class of Pyrazolo[4,3-e]pyrrolo[1,2-a][1,4]diazepinone Analogs of Pyrrolo[1,4][2,1-c]benzodiazepines Pier Giovanni Baraldi, Alberto Leoni, Barbara Cacciari, Stefano Manfredini, Daniele Simoni, Marzia Bergomi, Ernesto Menta, and Silvano Spinelli pp 4329 - 4337; DOI: 10.1021/jm00051a009 |
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DNA-Directed Alkylating Agents. 6. Synthesis and Antitumor Activity of DNA Minor Groove-Targeted Aniline Mustard Analogs of Pibenzimol (Hoechst 33258) G. Lance Gravatt, Bruce C. Baguley, William R. Wilson, and William A. Denny pp 4338 - 4345; DOI: 10.1021/jm00051a010 |
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1-(2,5-Dimethoxy-4-(trifluoromethyl)phenyl)-2-aminopropane: A Potent Serotonin 5-HT2A/2C Agonist David E. Nichols, Stewart Frescas, Danuta Marona-Lewicka, Xuemei Huang, Bryan L. Roth, Gary A. Gudelsky, and J. Frank Nash pp 4346 - 4351; DOI: 10.1021/jm00051a011 |
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Bioreductive Markers for Hypoxic Cells: 2-Nitroimidazoles with Biotinylated 1-Substituents Richard J. Hodgkiss, John Parrick, Manuchehr Porssa, and Michael R. L. Stratford pp 4352 - 4356; DOI: 10.1021/jm00051a012 |
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Inhibition of Myeloperoxidase Release from Rat Polymorphonuclear Leukocytes by a Series of Azachalcone Derivatives Michael L. Edwards, David M. Stemerick, Jeffrey S. Sabol, Keith A. Diekema, and Robert J. Dinerstein pp 4357 - 4362; DOI: 10.1021/jm00051a013 |
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Mobilization of Iron by Chiral and Achiral Anionic 3-Hydroxypyrid-4-ones John Josef Molenda, Mark M. Jones, David S. Johnston, Ernest M. Walker, and Donald J. Cannon pp 4363 - 4370; DOI: 10.1021/jm00051a014 |
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Development of a Model for the .delta. Opioid Receptor Pharmacophore. 1. Conformationally Restricted Tyr1 Replacements in the Cyclic .delta. Receptor Selective Tetrapeptide Tyr-c[D-Cys-Phe-D-Pen]OH (JOM-13) Henry I. Mosberg, Andrei L. Lomize, Chenguang Wang, Heather Kroona, Deborah L. Heyl, Katarzyna Sobczyk-Kojiro, Wenli Ma, Carol Mousigian, and Frank Porreca pp 4371 - 4383; DOI: 10.1021/jm00051a015 |
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Development of a Model for the .delta. Opioid Receptor Pharmacophore. 2. Conformationally Restricted Phe3 Replacements in the Cyclic .delta. Receptor Selective Tetrapeptide Tyr-c[D-Cys-Phe-D-Pen]OH (JOM-13) Henry I. Mosberg, John R. Omnaas, Andrei Lomize, Deborah L. Heyl, Ian Nordan, Carol Mousigian, Peg Davis, and Frank Porreca pp 4384 - 4391; DOI: 10.1021/jm00051a016 |
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Interaction of Calcium Channel Antagonists with Calcium: Structural Studies on Nicardipine and Its Ca2+ Complex Marie-Paula Belciug and Vettai S. Ananthanarayanan pp 4392 - 4399; DOI: 10.1021/jm00051a017 |
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Structure-Distribution Relationships for Metal-Labeled Myocardial Imaging Agents: Comparison of a Series of Cationic Gallium(III) Complexes with Hexadentate Bis(salicylaldimine) Ligands Brenda W. Tsang, Carla J. Mathias, Phillip E. Fanwick, and Mark A. Green pp 4400 - 4406; DOI: 10.1021/jm00051a018 |
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Isolation and Structure/Activity Features of Halomon-Related Antitumor Monoterpenes from the Red Alga Portieria hornemannii Richard W. Fuller, John H. Cardellina II, Jaroslaw Jurek, Paul J. Scheuer, Belinda Alvarado-Lindner, Mary McGuire, Glenn N. Gray, Jorge Rios Steiner, Jon Clardy, and et al. pp 4407 - 4411; DOI: 10.1021/jm00051a019 |
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Furoxans as Nitric Oxide Donors. 4-Phenyl-3-furoxancarbonitrile: Thiol-Mediated Nitric Oxide Release and Biological Evaluation Claudio Medana, Giuseppe Ermondi, Roberta Fruttero, Antonella Di Stilo, Carlo Ferretti, and Alberto Gasco pp 4412 - 4416; DOI: 10.1021/jm00051a020 |
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Bis-Catechol-Substituted Redox-Reactive Analogs of Hexamethonium and Decamethonium: Stimulated Affinity-Dependent Reactivity through Iron Peroxide Catalysis Yuqi Gu, Hyosil Lee, and Richard A. Hudson pp 4417 - 4420; DOI: 10.1021/jm00051a021 |
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Protein Kinase C. Modeling of the Binding Site and Prediction of Binding Constants. [Erratum to document cited in CA121:29778] Shaomeng Wang, George W. A. Milne, Marc C. Nicklaus, Victor E. Marquez, Jeewoo Lee, and Peter M. Blumberg pp 4422 - 4422; DOI: 10.1021/jm00051a022 |
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Book Reviews pp 4421 - 4421; DOI: 10.1021/jm00051a600 |
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N-(Acyloxyalkyl)pyridinium Salts as Soluble Prodrugs of a Potent Platelet Activating Factor Antagonist Steven K. Davidsen, James B. Summers, Daniel H. Albert, James H. Holms, H. Robin Heyman, Terrance J. Magoc, Richard G. Conway, David A. Rhein, and George W. Carter pp 4423 - 4429; DOI: 10.1021/jm00052a001 |
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Inhibition of Peptidylglycine .alpha.-Amidating Monooxygenase by N-Substituted Homocysteine Analogs Mark D. Erion, Jenny Tan, Mary Wong, and Arco Y. Jeng pp 4430 - 4437; DOI: 10.1021/jm00052a002 |
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Identification, Synthesis, and Characterization of a Unique Class of N-Methyl-D-aspartate Antagonists. The 6,11-Ethanobenzo[b]quinolizinium Cation John P. Mallamo, William G. Earley, Virendra Kumar, Chakrapani Subramanyam, John A. Jr. Dority, Matthew S. Miller, Diane L. DeHaven-Hudkins, Brian Ault, John L. Herrmann, and et al. pp 4438 - 4448; DOI: 10.1021/jm00052a003 |
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Carbonyl-Containing Bisphosphonate Esters as Novel Antiinflammatory and Antiarthritic Agents Richard A. Nugent, Stephen T. Schlachter, Megan Murphy, Colin J. Dunn, Nigel D. Staite, Louise A. Galinet, Sharon K. Shields, Haiyan Wu, Danielle G. Aspar, and Karen A. Richard pp 4449 - 4454; DOI: 10.1021/jm00052a004 |
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Ligands for Brain Cholinergic Channel Receptors: Synthesis and in Vitro Characterization of Novel Isoxazoles and Isothiazoles as Bioisosteric Replacements for the Pyridine Ring in Nicotine David S. Garvey, James T. Wasicak, Richard L. Elliott, Suzanne Lebold, Ann-Marie Hettinger, George M. Carrera, Nan-Horng Lin, Yun He, Mark W. Holladay, and et al. pp 4455 - 4463; DOI: 10.1021/jm00052a005 |
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Triazolinone Biphenylsulfonamides as Angiotensin II Receptor Antagonists with High Affinity for Both the AT1 and AT2 Subtypes Linda L. Chang, Wallace T. Ashton, Kelly L. Flanagan, Tsing-Bau Chen, Stacey S. O'Malley, Gloria J. Zingaro, Peter K. S. Siegl, Salah D. Kivlighn, Victor J. Lotti, and et al. pp 4464 - 4478; DOI: 10.1021/jm00052a006 |
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The Discovery of Novel, Structurally Diverse Protein Kinase C Agonists through Computer 3D-Database Pharmacophore Search. Molecular Modeling Studies Shaomeng Wang, Daniel W. Zaharevitz, Rajiv Sharma, Victor E. Marquez, Nancy E. Lewin, Linh Du, Peter M. Blumberg, and G. W. A. Milne pp 4479 - 4489; DOI: 10.1021/jm00052a007 |
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.kappa. Opioid Receptor Selective Affinity Labels: Electrophilic Benzeneacetamides as .kappa.-Selective Opioid Antagonists An-Chih Chang, Akira E. Takemori, William H. Ojala, William B. Gleason, and Philip S. Portoghese pp 4490 - 4498; DOI: 10.1021/jm00052a008 |
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A Conformationally Defined 6-s-trans-Retinoic Acid Isomer: Synthesis, Chemopreventive Activity, and Toxicity Michael F. Vaezi, Muzaffar Alam, Brahma P. Sani, Tina S. Rogers, Linda Simpson-Herren, John J. Wille, Donald L. Hill, Thomas I. Doran, Wayne J. Brouillette, and Donald D. Muccio pp 4499 - 4507; DOI: 10.1021/jm00052a009 |
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Structural Evolution and Pharmacology of a Novel Series of Triacid Angiotensin II Receptor Antagonists Alan D. Palkowitz, Mitchell I. Steinberg, K. Jeff Thrasher, Jon K. Reel, Kenneth L. Hauser, Karen M. Zimmerman, Sally A. Wiest, Celia A. Whitesitt, Richard L. Simon, and et al. pp 4508 - 4521; DOI: 10.1021/jm00052a010 |
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2,4-Diamino-5-chloroquinazoline Analogs of Trimetrexate and Piritrexim: Synthesis and Antifolate Activity Andre Rosowsky, Clara E. Mota, Joel E. Wright, and Sherry F. Queener pp 4522 - 4528; DOI: 10.1021/jm00052a011 |
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Structure of a Covalent DNA Minor Groove Adduct with a Pyrrolobenzodiazepine Dimer: Evidence for Sequence-Specific Interstrand Crosslinking Terence C. Jenkins, Laurence H. Hurley, Stephen Neidle, and David E. Thurston pp 4529 - 4537; DOI: 10.1021/jm00052a012 |
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Inhibition of Human Neutrophil Elastase with Peptidyl Electrophilic Ketones. 2. Orally Active PG-Val-Pro-Val Pentafluoroethyl Ketones Michael R. Angelastro, Larry E. Baugh, Philippe Bey, Joseph P. Burkhart, Teng-Man Chen, Sherrie L. Durham, C. Michelle Hare, Edward W. Huber, Michael J. Janusz, and et al. pp 4538 - 4553; DOI: 10.1021/jm00052a013 |
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Pentamidine Congeners. 2. 2-Butene-Bridged Aromatic Diamidines and Diimidazolines as Potential Anti-Pneumocystis carinii Pneumonia Agents Isaac O. Donkor, Richard R. Tidwell, and Susan K. Jones pp 4554 - 4557; DOI: 10.1021/jm00052a014 |
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A Bioactive Fullerene Peptide Claudio Toniolo, Alberto Bianco, Michele Maggini, Gianfranco Scorrano, Maurizio Prato, Mauro Marastoni, Roberto Tomatis, Susanna Spisani, Giorgio Palu, and Edward D. Blair pp 4558 - 4562; DOI: 10.1021/jm00052a015 |
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A Novel and Useful Descriptor for Hydrophobicity, Partition Coefficient Micellar-Water, and Its Application to a QSAR Study of Antiplatelet Agents Akito Tanaka, Katsuhiko Nakamura, Isao Nakanishi, and Hideaki Fujiwara pp 4563 - 4566; DOI: 10.1021/jm00052a016 |
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Synthesis and Anticonvulsant Activities of .alpha.-Acetamido-N-benzylacetamide Derivatives Containing an Electron-Deficient .alpha.-Heteroaromatic Substituent Patrick Bardel, Antoinette Bolanos, and Harold Kohn pp 4567 - 4571; DOI: 10.1021/jm00052a017 |
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Derivatives of 4-(2'-Methoxyphenyl)-1-[2'-(N-2''-pyridinyl-p-iodobenzamido)ethyl]piperazine (p-MPPI) as 5-HT1A Ligands Zhi-Ping Zhuang, Mei-Ping Kung, Sumalee Chumpradit, Mu Mu, and Hank F. Kung pp 4572 - 4575; DOI: 10.1021/jm00052a018 |
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Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor Heike A. Wieland and Hartmut Lueddens pp 4576 - 4580; DOI: 10.1021/jm00052a019 |
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Book Reviews pp 4581 - 4584; DOI: 10.1021/jm00052a600 |