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Cyclic peptides as selective tachykinin antagonists Brian J. Williams, Neil R. Curtis, Alexander T. McKnight, Janet J. Maguire, Stephen C. Young, Daniel F. Veber, and Raymond Baker pp 2 - 10; DOI: 10.1021/jm00053a001 |
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Oxidation chemistry of the endogenous central nervous system alkaloid salsolinol-1-carboxylic acid Fa Zhang and Glenn Dryhurst pp 11 - 20; DOI: 10.1021/jm00053a002 |
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Inhibitors of protein kinase C. 3. Potent and highly selective bisindolylmaleimides by conformational restriction Rino A. Bit, Peter D. Davis, Lucy H. Elliott, William Harris, Christopher H. Hill, Elizabeth Keech, Hari Kumar, Geoffrey Lawton, Anna Maw, John S. Nixon, David R. Vesey, Julie Wadsworth, and Sandra E. Wilkinson pp 21 - 29; DOI: 10.1021/jm00053a003 |
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1,3-Dioxolanylpurine nucleosides (2R,4R) and (2R,4S) with selective anti-HIV-1 activity in human lymphocytes Hea O. Kim, Raymond F. Schinazi, Satyanarayana Nampalli, Kirupathevy Shanmuganathan, Deborah L. Cannon, Antonio J. Alves, Lak S. Jeong, J. Warren Beach, and Chung K. Chu pp 30 - 37; DOI: 10.1021/jm00053a004 |
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6-[(Aminoalkyl)amino]-substituted 7H-benzo[e]perimidin-7-ones as novel antineoplastic agents. Synthesis and biological evaluation Barbara Stefanska, Maria Dzieduszycka, Sante Martelli, Jolanta Tarasiuk, Maria Bontemps-Gracz, and Edward Borowski pp 38 - 41; DOI: 10.1021/jm00053a005 |
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Synthesis of 20-hydroxy-, 20-amino-, and 20-nitro-14-hydroxy-21-nor-5.beta.,14.beta.-pregnane C-3 glycosides and related derivatives: structure-activity relationships of pregnanes that bind to the digitalis receptor John F. Templeton, Yangzhi Ling, Talal H. Zeglam, and Frank S. LaBella pp 42 - 45; DOI: 10.1021/jm00053a006 |
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S-Adenosylmethionine decarboxylase inhibitors: new aryl and heteroaryl analogs of methylglyoxal bis(guanylhydrazone) Jaroslav Stanek, Giorgio Caravatti, Hans Georg Capraro, Pascal Furet, Helmut Mett, Peter Schneider, and Urs Regenass pp 46 - 54; DOI: 10.1021/jm00053a007 |
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Structure-based design of inhibitors of purine nucleoside phosphorylase. 1. 9-(Arylmethyl) derivatives of 9-deazaguanine John A. Montgomery, Shri Niwas, Jerry D. Rose, John A. Secrist, Y. Sudhakar Babu, Charles E. Bugg, Mark D. Erion, Wayne C. Guida, and Steven E. Ealick pp 55 - 69; DOI: 10.1021/jm00053a008 |
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On the prediction of binding properties of drug molecules by comparative molecular field analysis Gerhard Klebe and Ute Abraham pp 70 - 80; DOI: 10.1021/jm00053a009 |
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Structure-activity relationship of 99mTc complexes of phenylenediamine-thiol-thioether ligands (PhAT) to brain uptake in rats Bill J. McBride, Ronald M. Baldwin, Janice M. Kerr, Jiann Long Wu, Lisa M. Schultze, Nilda E. Salazar, James M. Chinitz, and Edmund F. Byrne pp 81 - 86; DOI: 10.1021/jm00053a010 |
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Exploration of neutral endopeptidase active site by a series of new thiol-containing inhibitors Isabel Gomez-Monterrey, Serge Turcaud, Evelyne Lucas, Luce Bruetschy, Bernard P. Roques, and Marie Claude Fournie-Zaluski pp 87 - 94; DOI: 10.1021/jm00053a011 |
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Structural determinants of haloenol lactone-mediated suicide inhibition of canine myocardial calcium-independent phospholipase A2 Lori A. Zupan, Randy H. Weiss, Stanley L. Hazen, Barry L. Parnas, Karl W. Aston, Patrick J. Lennon, Daniel P. Getman, and Richard W. Gross pp 95 - 100; DOI: 10.1021/jm00053a012 |
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Nonpeptide angiotensin II antagonists: N-phenyl-1H-pyrrole derivatives are angiotensin II receptor antagonists Philippe R. Bovy, David B. Reitz, Joseph T. Collins, Timothy S. Chamberlain, Gillian M. Olins, Valerie M. Corpus, Ellen G. McMahon, Maria A. Palomo, John P. Koepke, Glen J. Smits, Dean E. McGraw, and Jeffrey F. Gaw pp 101 - 110; DOI: 10.1021/jm00053a013 |
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Synthesis and use of the n-bromododecane-1,12-diols as conformational probes for general anesthetic target sites R. Dickinson, E. H. Smith, N. P. Franks, and W. R. Lieb pp 111 - 118; DOI: 10.1021/jm00053a014 |
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Purine 2'-deoxy-2'-fluororibosides as antiinfluenza virus agents Joel V. Tuttle, Margaret Tisdale, and Thomas A. Krenitsky pp 119 - 125; DOI: 10.1021/jm00053a015 |
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Use of affinity capillary electrophoresis to determine kinetic and equilibrium constants for binding of arylsulfonamides to bovine carbonic anhydrase Luis Z. Avila, Yen Ho Chu, Erich C. Blossey, and George M. Whitesides pp 126 - 133; DOI: 10.1021/jm00053a016 |
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Pyrazoline bisphosphonate esters as novel antiinflammatory and antiarthritic agents Richard A. Nugent, Megan Murphy, Stephen T. Schlachter, Colin J. Dunn, Robert J. Smith, Nigel D. Staite, Louise A. Galinet, Sharon K. Shields, Danielle G. Aspar, Karen A. Richard, and Norman A. Rohloff pp 134 - 139; DOI: 10.1021/jm00053a017 |
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Further development of hydrogen bond functions for use in determining energetically favorable binding sites on molecules of known structure. 1. Ligand probe groups with the ability to form two hydrogen bonds Rebecca C. Wade, Kevin J. Clark, and Peter J. Goodford pp 140 - 147; DOI: 10.1021/jm00053a018 |
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Further development of hydrogen bond functions for use in determining energetically favorable binding sites on molecules of known structure. 2. Ligand probe groups with the ability to form more than two hydrogen bonds Rebecca C. Wade and Peter J. Goodford pp 148 - 156; DOI: 10.1021/jm00053a019 |
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o-Chlorobenzenesulfonamidic derivatives of (aryloxy)propanolamines as .beta.-blocking/diuretic agents Violetta Cecchetti, Arnaldo Fravolini, Fausto Schiaffella, Oriana Tabarrini, Giancarlo Bruni, and Giorgio Segre pp 157 - 161; DOI: 10.1021/jm00053a020 |
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Synthesis and structure-activity relationship of some 5-[[[(dialkylamino)alkyl]-1-piperidinyl]acetyl]-10,11-dihydro-5H-dibenzo[b,e][1,4]diazepin-11-ones as M2-selective antimuscarinics Victor I. Cohen, Jesse Baumgold, Biyun Jin, Rosanna De la Cruz, Waclaw J. Rzeszotarski, and Richard C. Reba pp 162 - 165; DOI: 10.1021/jm00053a021 |
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CCK-B agonist or antagonist activities of structurally hindered and peptidase-resistant Boc-CCK4 derivatives P. J. Corringer, J. H. Weng, B. Ducos, C. Durieux, P. Boudeau, A. Bohme, and B. P. Roques pp 166 - 172; DOI: 10.1021/jm00053a022 |
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Phosphorus-containing inhibitors of endothelin converting enzyme: effects of the electronic nature of phosphorus on inhibitor potency Stephen R. Bertenshaw, Roland S. Rogers, Michael K. Stern, Bryan H. Norman, William M. Moore, Gina M. Jerome, Linda M. Branson, John F. McDonald, Ellen G. McMahon, and Maria A. Palomo pp 173 - 176; DOI: 10.1021/jm00053a023 |
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Hemicholinium and related lipids: inhibitors of protein kinase C G. Kumaravel, Curtis L. Ashendel, and Richard D. Gandour pp 177 - 178; DOI: 10.1021/jm00053a024 |
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A remarkable change of opioid receptor selectivity on the attachment of a peptidomimetic .kappa. address element to the .delta. antagonist, natrindole: 5'-[(N2-alkylamidino)methyl]naltrindole derivatives as a novel class of .kappa. opioid receptor antagonists S. L. Olmsted, A. E. Takemori, and P. S. Portoghese pp 179 - 180; DOI: 10.1021/jm00053a025 |
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Editorial - Expansion of the Perspective Series Philip S. Portoghese pp 1 - 1; DOI: 10.1021/jm00053a600 |
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Asymmetric synthesis and biological evaluation of .beta.-L-(2R,5S)- and .alpha.-L-(2R,5R)-1,3-oxathiolane-pyrimidine and -purine nucleosides as potential anti-HIV agents Lak S. Jeong, Raymond F. Schinazi, J. Warren Beach, Hea O. Kim, Satyanarayana Nampalli, Kirupathevy Shanmuganathan, Antonio J. Alves, Angela McMillan, Chung K. Chu, and Rodney Mathis pp 181 - 195; DOI: 10.1021/jm00054a001 |
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Effects of solvation on the ionization and conformation of raclopride and other antidopaminergic 6-methoxysalicylamides: insight into the pharmacophore Ruey Shiuan Tsai, Pierre-Alain Carrupt, Bernard Testa, Patrick Gaillard, Nabil El Tayar, and Thomas Hoegberg pp 196 - 204; DOI: 10.1021/jm00054a002 |
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Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 5. Synthesis and evaluation of enantiomers of 8-[[(4-chlorophenyl)sulfonyl]amino]-4-(3-pyridinylalkyl)octanoic acid Shripad S. Bhagwat, Candido Gude, David S. Cohen, Ron Dotson, Janice Mathis, Warren Lee, and Patricia Furness pp 205 - 210; DOI: 10.1021/jm00054a003 |
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Development of selective tight-binding inhibitors of leukotriene A4 hydrolase Wei Yuan, Benito Munoz, Chi Huey Wong, Jesper Z. Haeggstroem, Anders Wetterholm, and Bengt Samuelsson pp 211 - 220; DOI: 10.1021/jm00054a004 |
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Fluorinated and iodinated dopamine agents: D2 imaging agents for PET and SPECT S. Chumpradit, M. P. Kung, J. Billings, R. Mach, and H. F. Kung pp 221 - 228; DOI: 10.1021/jm00054a005 |
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Further insights into the molecular mechanisms of action of the serotonergic neurotoxin 5,7-dihydroxytryptamine Tahereh Tabatabaie, R. N. Goyal, C. LeRoy Blank, and Glenn Dryhurst pp 229 - 236; DOI: 10.1021/jm00054a006 |
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(+)-Hemipalmitoylcarnitinium strongly inhibits carnitine palmitoyltransferase-I in intact mitochondria Richard D. Gandour, On Tai Leung, Anthony T. Greway, Rona R. Ramsay, Noirin Nic A Bhaird, Frank R. Fronczek, Bret M. Bellard, and G. Kumaravel pp 237 - 242; DOI: 10.1021/jm00054a007 |
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Phenyl-substituted prostaglandins: potent and selective antiglaucoma agents Bahram Resul, Johan Stjernschantz, Kiyo No, Charlotta Liljebris, Goeran Selen, Maria Astin, Maritha Karlsson, and Laszlo Z. Bito pp 243 - 248; DOI: 10.1021/jm00054a008 |
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Synthesis and evaluation of 2-pyridinone derivatives as specific HIV-1 reverse transcriptase inhibitors. 3. Pyridyl and phenyl analogs of 3-aminopyridin-2(1H)-one John S. Wai, Theresa M. Williams, Dona L. Bamberger, Thorsten E. Fisher, Jacob M. Hoffman, Ronald J. Hudcosky, Suzanne C. MacTough, Clarence S. Rooney, Walfred S. Saari, and et al. pp 249 - 255; DOI: 10.1021/jm00054a009 |
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Synthesis and dopamine receptor modulating activity of lactam conformationally constrained analogs of Pro-Leu-Gly-NH2 Uma Sreenivasan, Ram K. Mishra, and Rodney L. Johnson pp 256 - 263; DOI: 10.1021/jm00054a010 |
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7.alpha.-Methyl- and 11.beta.-ethoxy-substitution of iodine-125-labeled [125I]16.alpha.-iodoestradiol: effect on estrogen receptor-mediated target tissue uptake Hasrat Ali, Jacques Rousseau, and Johan E. Van Lier pp 264 - 271; DOI: 10.1021/jm00054a011 |
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Benextramine-neuropeptide Y receptor interactions: contribution of the benzylic moieties to [3H]neuropeptide Y displacement activity Michael B. Doughty, Chandra S. Chaurasia, and Ke Li pp 272 - 279; DOI: 10.1021/jm00054a012 |
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Comparative evaluation of seven oligonucleotide analogs as potential antisense agents F. Morvan, H. Porumb, G. Degols, I. Lefebvre, A. Pompon, B. S. Sproat, B. Rayner, C. Malvy, B. Lebleu, and J. L. Imbach pp 280 - 287; DOI: 10.1021/jm00054a013 |
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Discovery of a novel class of potent HIV-1 protease inhibitors containing the (R)-(hydroxyethyl)urea isostere Daniel P. Getman, Gary A. DeCrescenzo, Robert M. Heintz, Kathryn L. Reed, John J. Talley, Martin L. Bryant, Michael Clare, Kathryn A. Houseman, J. Joseph Marr, and et al. pp 288 - 291; DOI: 10.1021/jm00054a014 |
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3-Tetrahydrofuran and pyran urethanes as high-affinity P2-ligands for HIV-1 protease inhibitors Arun K. Ghosh, Wayne J. Thompson, Sean P. McKee, Tien T. Duong, Terry A. Lyle, Jenny C. Chen, Paul L. Darke, Joan A. Zugay, Emilio A. Emini, and et al. pp 292 - 294; DOI: 10.1021/jm00054a015 |
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4-Methoxy-2-methyltetrahydropyrans: chiral leukotriene biosynthesis inhibitors, related to ICI D2138, which display enantioselectivity Graham C. Crawley, Malcolm T. Briggs, Robert I. Dowell, Philip N. Edwards, Patricia M. Hamilton, John F. Kingston, Keith Oldham, David Waterson, and David P. Whalley pp 295 - 296; DOI: 10.1021/jm00054a016 |
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2'-(Trimethylammonio)ethyl 4-(hexadecyloxy)-3(S)-methoxybutane phosphonate: a novel potent antineoplastic agent Robert Bittman, Hoe Sup Byun, Brenda Mercier, and Hassan Salari pp 297 - 299; DOI: 10.1021/jm00054a017 |
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Active site-directed synthetic thrombin inhibitors: synthesis, in vitro and in vivo activity profile of BMY 44621 and analogs. An examination of the role of the amino group in the D-Phe-Pro-Arg-H series N. Balasubramanian, D. R. St. Laurent, M. E. Federici, N. A. Meanwell, J. J. Wright, W. A. Schumacher, and S. M. Seiler pp 300 - 303; DOI: 10.1021/jm00054a018 |
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Design of a functional hexapeptide antagonist of endothelin. [Erratum to document cited in CA117(13):125306v] Wayne L. Cody, Annette M. Doherty, John X. He, Patricia L. DePue, Stephen T. Rapundalo, Gary A. Hingorani, Terry C. Major, Robert L. Panek, David T. Dudley, and et al. pp 304 - 304; DOI: 10.1021/jm00054a019 |
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Enantiospecific syntheses of .alpha.-(fluoromethyl)tryptophan analogs: interactions with tryptophan hydroxylase and aromatic L-amino acid decarboxylase David E. Zembower, Judith A. Gilbert, and Matthew M. Ames pp 305 - 313; DOI: 10.1021/jm00055a001 |
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Highly selective tripeptide thrombin inhibitors Robert T. Shuman, Robert B. Rothenberger, Charles S. Campbell, Gerald F. Smith, Donetta S. Gifford-Moore, and Paul D. Gesellchen pp 314 - 319; DOI: 10.1021/jm00055a002 |
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Symmetry-based inhibitors of HIV protease. Structure-activity studies of acylated 2,4-diamino-1,5-diphenyl-3-hydroxypentane and 2,5-diamino-1,6-diphenylhexane-3,4-diol Dale J. Kempf, Lynnmarie Codacovi, Xiu Chun Wang, William E. Kohlbrenner, Norman E. Wideburg, Ayda Saldivar, Sudthida Vasavanonda, Kennan C. Marsh, Pamela Bryant, and et al. pp 320 - 330; DOI: 10.1021/jm00055a003 |
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Potent quinoxaline-spaced phosphono .alpha.-amino acids of the AP-6 type as competitive NMDA antagonists: synthesis and biological evaluation Reinhardt B. Baudy, Lynne P. Greenblatt, Ivo L. Jirkovsky, Mary Conklin, Ralph J. Russo, Donna R. Bramlett, Tracy A. Emrey, Joanne T. Simmonds, Dianne M. Kowal, and et al. pp 331 - 342; DOI: 10.1021/jm00055a004 |
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Synthesis and in vitro evaluation of 5,6,7,8,9,10-hexahydro-7,10-iminocyclohept[b]indoles: high-affinity ligands for the N,N'-di-o-tolylguanidine-labeled .sigma. binding site Richard E. Mewshaw, Ronald G. Sherrill, Rose M. Mathew, Carl Kaiser, Michael A. Bailey, and E. William Karbon pp 343 - 352; DOI: 10.1021/jm00055a005 |
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Syntheses and biological evaluations of 3'-deoxy-3'-C-branched-chain-substituted nucleosides Tai Shun Lin, Ju Liang Zhu, Ginger E. Dutschman, Yung Chi Cheng, and William H. Prusoff pp 353 - 362; DOI: 10.1021/jm00055a006 |
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Effect of N-methyl substitution of the peptide bonds in luteinizing hormone-releasing hormone agonists Fortuna Haviv, Timothy D. Fitzpatrick, Rolf E. Swenson, Charles J. Nichols, Nicholas A. Mort, Eugene N. Bush, Gilbert Diaz, Gary Bammert, A. Nguyen, and et al. pp 363 - 369; DOI: 10.1021/jm00055a007 |
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Inhibition of the tetracycline efflux antiport protein by 13-thio-substituted 5-hydroxy-6-deoxytetracyclines Mark L. Nelson, Britt H. Park, Janey S. Andrews, Vlasios A. Georgian, Richard C. Thomas, and Stuart B. Levy pp 370 - 377; DOI: 10.1021/jm00055a008 |
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Novel 6-alkoxypurine 2',3'-dideoxynucleosides as inhibitors of the cytopathic effect of the human immunodeficiency virus Charlene L. Burns, Marty H. St. Clair, Lloyd W. Frick, Thomas Spector, Devron R. Averett, Michael L. English, Timothy J. Holmes, Thomas A. Krenitsky, and George W. Koszalka pp 378 - 384; DOI: 10.1021/jm00055a009 |
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Defining structural requirements for neuropeptide Y receptors using truncated and conformationally restricted analogs Dean A. Kirby, Steven C. Koerber, A. Grey Craig, Robert D. Feinstein, Laura Delmas, Marvin R. Brown, and Jean E. Rivier pp 385 - 393; DOI: 10.1021/jm00055a010 |
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Substituted 3-(phenylmethyl)-1H-indole-5-carboxamides and 1-(phenylmethyl)indole-6-carboxamides as potent, selective, orally active antagonists of the peptidoleukotrienes Robert T. Jacobs, Frederick J. Brown, Laura A. Cronk, David Aharony, Carl K. Buckner, Edward J. Kusner, Karin M. Kirkland, and Kathleen L. Neilson pp 394 - 409; DOI: 10.1021/jm00055a011 |
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32-Methyl-32-oxylanosterols: dual-action inhibitors of cholesterol biosynthesis Leah L. Frye, Kevin P. Cusack, and Deborah A. Leonard pp 410 - 416; DOI: 10.1021/jm00055a012 |
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Dibenz[b,e]oxepin derivatives: novel antiallergic agents possessing thromboxane A2 and histamine H1 dual antagonizing activity. 1 Etsuo Ohshima, Hitoshi Takami, Hiroyuki Harakawa, Hideyuki Sato, Hiroyuki Obase, Ichiro Miki, Akio Ishii, Hidee Ishii, Yasuo Sasaki, and et al. pp 417 - 420; DOI: 10.1021/jm00055a013 |
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Nonsteroidal inhibitors of human type I steroid 5-.alpha.-reductase Charles D. Jones, James E. Audia, David E. Lawhorn, Loretta A. McQuaid, Blake L. Neubauer, Andrew J. Pike, Pamela A. Pennington, Nancy B. Stamm, Richard E. Toomey, and Kenneth S. Hirsch pp 421 - 423; DOI: 10.1021/jm00055a014 |
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Book Reviews pp 424 - 424; DOI: 10.1021/jm00055a600 |
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Bicyclic compounds as ring-constrained inhibitors of protein-tyrosine kinase p56lck Terrence R. Burke, Benjamin Lim, Victor E. Marquez, Zhen Hong Li, Joseph B. Bolen, Irena Stefanova, and Ivan D. Horak pp 425 - 432; DOI: 10.1021/jm00056a001 |
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Structure-activity relationships from molecular similarity matrices Andrew C. Good, Sung Sau So, and W. Graham Richards pp 433 - 438; DOI: 10.1021/jm00056a002 |
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Verapamil analogs with restricted molecular flexibility: synthesis and pharmacological evaluation of the four isomers of .alpha.-[1-[3-[N-[1-[2-(3,4-dimethoxyphenyl)ethyl]]-N-methylamino]cyclohexyl]]-.alpha.-isopropyl-3,4-dimethoxybenzeneacetonitrile Silvia Dei, M. Novella Romanelli, Serena Scapecchi, Elisabetta Teodori, Fulvio Gualtieri, Alberto Chiarini, Werner Voigt, and Horst Lemoine pp 439 - 445; DOI: 10.1021/jm00056a003 |
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Inactivation of monoamine oxidase B by analogs of the anticonvulsant agent milacemide [2-(n-pentylamino)acetamide] Kuniko Nishimura, Xingliang Lu, and Richard B. Silverman pp 446 - 448; DOI: 10.1021/jm00056a004 |
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Studies directed toward the design of orally active renin inhibitors. 1. Some factors influencing the absorption of small peptides Saul H. Rosenberg, Kenneth P. Spina, Keith W. Woods, Jim Polakowski, Donald L. Martin, Zhengli Yao, Herman H. Stein, Jerome Cohen, Jennifer L. Barlow, and et al. pp 449 - 459; DOI: 10.1021/jm00056a005 |
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Studies directed toward the design of orally active renin inhibitors. 2. Development of the efficacious, bioavailable renin inhibitor (2S)-2-benzyl-3-[[(1-methylpiperazin-4-yl)sulfonyl]propionyl]-3-thiazol-4-yl-L-alanine amide of (2S,3R,4S)-2-amino-1-cyclohexyl-3,4-dihydroxy-6-methylheptane (A-72517) Saul H. Rosenberg, Kenneth P. Spina, Stephen L. Condon, Jim Polakowski, Zhengli Yao, Peter Kovar, Herman H. Stein, Jerome Cohen, Jennifer L. Barlow, and et al. pp 460 - 467; DOI: 10.1021/jm00056a006 |
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Potent and selective inhibitors of an aspartyl protease-like endothelin converting enzyme identified in rat lung Kazumi Shiosaki, Andrew S. Tasker, Gerard M. Sullivan, Bryan K. Sorensen, Thomas W. von Geldern, Jinshyun R. Wu-Wong, Carol A. Marselle, and Terry J. Opgenorth pp 468 - 478; DOI: 10.1021/jm00056a007 |
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Synthesis and structure-activity relationships of 3,5-disubstituted 4,5-dihydro-6H-imidazo[1,5-a][1,4]benzodiazepin-6-ones at diazepam-sensitive and diazepam-insensitive benzodiazepine receptors Subramaniam Ananthan, Sarah D. Clayton, Steven E. Ealick, Garry Wong, Gary E. Evoniuk, and Phil Skolnick pp 479 - 490; DOI: 10.1021/jm00056a008 |
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Irreversible inactivation of macrophage and brain nitric oxide synthase by L-NG-methylarginine requires NADPH-dependent hydroxylation Paul L. Feldman, Owen W. Griffith, Hui Hong, and Dennis J. Stuehr pp 491 - 496; DOI: 10.1021/jm00056a009 |
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Novel nonopioid non-antiinflammatory analgesics: 3-(aminoalkyl)- and 3-[(4-aryl-1-piperazinyl)alkyl]oxazolo[4,5-b]pyridin-2(3H)-ones Christine Flouzat, Yvette Bresson, Anny Mattio, Jacqueline Bonnet, and Gerald Guillaumet pp 497 - 503; DOI: 10.1021/jm00056a010 |
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Specific sequestering agents for the actinides. 21. Synthesis and initial biological testing of octadentate mixed catecholate-hydroxypyridinonate ligands Linda C. Uhlir, Patricia W. Durbin, Nylan Jeung, and Kenneth N. Raymond pp 504 - 509; DOI: 10.1021/jm00056a011 |
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A trans-platinum complex showing higher antitumor activity than the cis congeners Mauro Coluccia, Anna Nassi, Francesco Loseto, Angela Boccarelli, Maria A. Mariggio, Domenico Giordano, Francesco P. Intini, Paola Caputo, and Giovanni Natile pp 510 - 512; DOI: 10.1021/jm00056a012 |
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Synthesis of a photoaffinity analog of taxol as an approach to identify the taxol binding site on microtubules Joan M. Carboni, Vittorio Farina, Srinivasa Rao, Sheila I. Hauck, Susan Band Horwitz, and Israel Ringel pp 513 - 515; DOI: 10.1021/jm00056a013 |
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4'-5'-Unsaturated 5'-halogenated nucleosides. Mechanism-based and competitive inhibitors of S-adenosyl-L-homocysteine hydrolase. [Erratum to document cited in CA114(21):207657n] Esa T. Jarvi, James R. McCarthy, Shujaath Mehdi, Donald P. Matthews, Michael L. Edwards, Nellikunja J. Prakash, Terry L. Bowlin, Prasad S. Sunkara, and Philippe Bey pp 518 - 518; DOI: 10.1021/jm00056a014 |
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Book Reviews pp 516 - 517; DOI: 10.1021/jm00056a600 |
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L-.beta.-(2S,4S)- and L-.alpha.-(2S,4R)-dioxolanyl nucleosides as potential anti-HIV agents: asymmetric synthesis and structure-activity relationships Hea O. Kim, Raymond F. Schinazi, Kirupathevy Shanmuganathan, Lak S. Jeong, J. Warren Beach, Satyanarayana Nampalli, Deborah L. Cannon, and Chung K. Chu pp 519 - 528; DOI: 10.1021/jm00057a001 |
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Synthesis and pharmacokinetics of a dihydropyridine chemical delivery system for the antiimmunodeficiency virus agent, dideoxycytidine Paul F. Torrence, Junei Kinjo, Shahrzad Khamnei, and Nigel H. Greig pp 529 - 537; DOI: 10.1021/jm00057a002 |
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Synthesis and antiviral activity of 5-thien-2-yl-2'-deoxyuridine analogs Piet Wigerinck, Luc Kerremans, Paul Claes, Robert Snoeck, Prabhat Maudgal, Erik De Clercq, and Piet Herdewijn pp 538 - 543; DOI: 10.1021/jm00057a003 |
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Antitumor agents. 139. Synthesis and biological evaluation of thiocolchicine analogs 5,6-dihydro-6(S)-acyloxy)- and 5,6-dihydro-6(S)-[(aroyloxy)methyl]-1,2,3-trimethoxy-9-(methylthio)-8H-cyclohepta[a]naphthalen-8-ones as novel cytotoxic and antimitotic agents Li Sun, Andrew T. McPhail, Ernest Hamel, Chii M. Lin, Susan B. Hastie, Jer Jang Chang, and Kuo Hsiung Lee pp 544 - 551; DOI: 10.1021/jm00057a004 |
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Cholecystokinin dipeptoid antagonists: design, synthesis, and anxiolytic profile of some novel CCK-A and CCK-B selective and mixed CCK-A/CCK-B antagonists P. R. Boden, M. Higginbottom, D. R. Hill, D. C. Horwell, J. Hughes, D. C. Rees, E. Roberts, L. Singh, N. Suman-Chauhan, and G. N. Woodruff pp 552 - 565; DOI: 10.1021/jm00057a005 |
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Synthesis and binding characteristics of potential SPECT imaging agents for .sigma.-1 and .sigma.-2 binding sites Xiao Shu He, Wayne D. Bowen, Kan Sam Lee, Wanda Williams, Daniel R. Weinberger, and Brian R. De Costa pp 566 - 571; DOI: 10.1021/jm00057a006 |
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Synthesis of 2-imidazolidinylidene propanedinitrile derivatives as stimulators of gastrointestinal motility. 1 Setsuya Sasho, Hiroyuki Obase, Shunji Ichikawa, Takio Kitazawa, Hiromi Nonaka, Rika Yoshizaki, Akio Ishii, and Katsuichi Shuto pp 572 - 579; DOI: 10.1021/jm00057a007 |
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Analogs of platelet activating factor. 8. Antagonists of PAF containing an aromatic ring linked to a pyridinium ring Michael P. Trova, Allan Wissner, Marion L. Carroll, Suresh S. Kerwar, Walter C. Pickett, Robert E. Schaub, Lawrence W. Torley, and Constance A. Kohler pp 580 - 590; DOI: 10.1021/jm00057a008 |
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Nonpeptide angiotensin II antagonists derived from 4H-1,2,4-triazoles and 3H-imidazo[1,2-b][1,2,4]triazoles Wallace T. Ashton, Christine L. Cantone, Linda L. Chang, Steven M. Hutchins, Robert A. Strelitz, Malcolm MacCoss, Raymond S. L. Chang, Victor J. Lotti, Kristie A. Faust, and et al. pp 591 - 609; DOI: 10.1021/jm00057a009 |
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Synthesis and antimuscarinic activity of some 1-cycloalkyl-1-hydroxy-1-phenyl-3-(4-substituted piperazinyl)-2-propanones and related compounds Carl Kaiser, Vicki H. Audia, J. Paul Carter, Daniel W. McPherson, Philip P. Waid, Valerie C. Lowe, and Lalita Noronha-Blob pp 610 - 616; DOI: 10.1021/jm00057a010 |
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5-HT3 Receptor antagonists. 2. 4-Hydroxy-4-quinolinecarboxylic acid derivatives Hiroaki Hayashi, Yoshikazu Miwa, Shunji Ichikawa, Nobuyuki Yoda, Ichiro Miki, Akio Ishii, Motomichi Kono, Tohru Yasuzawa, and Fumio Suzuki pp 617 - 626; DOI: 10.1021/jm00057a011 |
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Modulation of GABAA receptor function by benz[e]indenes and phenanthrenes Douglas F. Covey, Yuefei Hu, Michael G. Bouley, Katherine D. Holland, Nancy T. Rodgers-Neame, Keith E. Isenberg, and Charles F. Zorumski pp 627 - 630; DOI: 10.1021/jm00057a012 |
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Amidinium cation as a mimic of allylic carbocation: synthesis and squalene synthetase inhibitory activity of an amidinium analog of a carbocation intermediate Mahavir Prashad pp 631 - 632; DOI: 10.1021/jm00057a013 |
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(R)-(-)- and (S)-(+)-Adenallene: synthesis, absolute configuration, enantioselectivity of antiretroviral effect, and enzymic deamination. [Erratum to document cited in CA117(25):251672z] Sreenivasulu Megati, Zafrir Goren, James V. Silverton, Joel Orlina, Hisao Nishimura, Takuma Shirasaki, Hiroaki Mitsuya, and Jiri Zemlicka pp 634 - 634; DOI: 10.1021/jm00057a014 |
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Book Reviews pp 633 - 633; DOI: 10.1021/jm00057a600 |
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Modulation of leukocyte genetic expression by novel purine nucleoside analogs. A new approach to antitumor and antiviral agents Pierre A. Bonnet and Roland K. Robins pp 635 - 653; DOI: 10.1021/jm00058a001 |
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Synthesis and pharmacological evaluation of hexahydrofluorenamines as noncompetitive antagonists at the N-methyl-D-aspartate receptor Sheryl J. Hays, Perry M. Novak, Daniel F. Ortwine, Christopher F. Bigge, Norman L. Colbry, Graham Johnson, Leonard J. Lescosky, Thomas C. Malone, Andre Michael, and et al. pp 654 - 670; DOI: 10.1021/jm00058a002 |
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Centrally acting serotonergic agents. Synthesis and structure-activity relationships of C-1- or C-3-substituted derivatives of 8-hydroxy-2-(di-n-propylamino)tetralin Chiu Hong Lin, Susanne R. Haadsma-Svensson, Robert A. Lahti, Robert B. McCall, Montford F. Piercey, Peggy J. K. D. Schreur, Philip F. VonVoigtlander, and Connie G. Chidester pp 671 - 682; DOI: 10.1021/jm00058a003 |
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Substituted benzamides with conformationally restricted side chains. 5. Azabicyclo[x.y.z] derivatives as 5-HT4 receptor agonists and gastric motility stimulants Frank D. King, Michael S. Hadley, Karen T. Joiner, Roger T. Martin, Gareth J. Sanger, Duncan M. Smith, Gillian E. Smith, Paul Smith, David H. Turner, and Eric A. Watts pp 683 - 689; DOI: 10.1021/jm00058a004 |
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Structure-activity relationships in prazosin-related compounds. 2. Role of the piperazine ring on .alpha.-blocking activity Dario Giardina, Ugo Gulini, Maurizio Massi, Maria G. Piloni, Pierluigi Pompei, Giovanni Rafaiani, and Carlo Melchiorre pp 690 - 698; DOI: 10.1021/jm00058a005 |
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1,2-Cyclomethylencarboxylic monoamide hydroxamic derivatives. A novel class of non-amino acid angiotensin converting enzyme inhibitors Luigi Turbanti, Guido Cerbai, Cristina Di Bugno, Raffaello Giorgi, Giorgio Garzelli, Marco Criscuoli, Anna R. Renzetti, Alessandro Subissi, Giancarlo Bramanti, and Scott A. DePriest pp 699 - 707; DOI: 10.1021/jm00058a006 |
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A topochemical approach to explain morphiceptin bioactivity Toshimasa Yamazaki, Seonggu Ro, Murray Goodman, Nga N. Chung, and Peter W. Schiller pp 708 - 719; DOI: 10.1021/jm00058a007 |
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Epoxysuccinyl dipeptides as selective inhibitors of cathepsin B Barbara J. Gour-Salin, Paule Lachance, Celine Plouffe, Andrew C. Storer, and Robert Menard pp 720 - 725; DOI: 10.1021/jm00058a008 |
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Non-nucleoside inhibitors of HIV-1 reverse transcriptase: molecular modeling and x-ray structure investigations Wolfgang Schaefer, Walter Gunar Friebe, Herbert Leinert, Alfred Mertens, Thomas Poll, Wolfgang Von der Saal, Harald Zilch, Bernhard Nuber, and Manfred L. Ziegler pp 726 - 732; DOI: 10.1021/jm00058a009 |
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Design of thymidylate synthase inhibitors using protein crystal structures: the synthesis and biological evaluation of a novel class of 5-substituted quinazolinones Stephen E. Webber, Ted M. Bleckman, John Attard, Judith G. Deal, Vinit Kathardekar, Katherine M. Welsh, Stephanie Webber, Cheryl A. Janson, David A. Matthews, and et al. pp 733 - 746; DOI: 10.1021/jm00058a010 |
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Systematic substitution of an oxytocin antagonist with D-amino acids; unexpected high antagonistic potency of the D-Cys6-substituted analog George Flouret, Tadeusz Majewski, William Brieher, and Laird Wilson pp 747 - 749; DOI: 10.1021/jm00058a011 |
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Design and synthesis of highly potent and selective cyclic dynorphin A analogs. 2. New analogs Andrew M. Kawasaki, Richard J. Knapp, Thomas H. Kramer, Amanda Walton, William S. Wire, Shinicki Hashimoto, Henry I. Yamamura, Frank Porreca, Thomas F. Burks, and Victor J. Hruby pp 750 - 757; DOI: 10.1021/jm00058a012 |
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Synthesis and tubulin binding of novel C-10 analogs of colchicine Marianne E. Staretz and Susan Bane Hastie pp 758 - 764; DOI: 10.1021/jm00058a013 |
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2-Substituted 1,2-dihydro-3H-dibenz[de,h]isoquinoline-1,3-diones. A new class of antitumor agent Salah M. Sami, Robert T. Dorr, David S. Alberts, and William A. Remers pp 765 - 770; DOI: 10.1021/jm00058a014 |
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Orally active .beta.-lactam inhibitors of human leukocyte elastase. 2. Effect of C-4 substitution William K. Hagmann, Amy L. Kissinger, Shrenik K. Shah, Paul E. Finke, Conrad P. Dorn, Karen A. Brause, Bonnie M. Ashe, Hazel Weston, Alan L. Maycock, and et al. pp 771 - 777; DOI: 10.1021/jm00058a015 |
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Neuraminidase-resistant hemagglutination inhibitors: acrylamide copolymers containing a C-glycoside of N-acetylneuraminic acid Michelle A. Sparks, Kevin W. Williams, and George M. Whitesides pp 778 - 783; DOI: 10.1021/jm00058a016 |
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Structure-activity relationship of glycine betaine analogs on osmotolerance of enteric bacteria Yasser S. Abdel-Ghany, Michael A. Ihnat, Duane D. Miller, Calvin M. Kunin, and Hua H. Tong pp 784 - 789; DOI: 10.1021/jm00058a017 |
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Book Reviews pp 790 - 790; DOI: 10.1021/jm00058a600 |
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Design, synthesis, and pharmacology of 3-substituted sodium azulene-1-sulfontes and related compounds: non-prostanoid thromboxane A2 receptor antagonists Tsuyoshi Tomiyama, Masayuki Yokota, Shuichi Wakabayashi, Kazuhiro Kosakai, and Takashi Yanagisawa pp 791 - 800; DOI: 10.1021/jm00059a001 |
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7-Azetidinylquinolones as antibacterial agents. Synthesis and structure-activity relationships Jordi Frigola, Juan Pares, Jordi Corbera, David Vano, Ramon Merce, Antoni Torrens, Josep Mas, and Eduard Valenti pp 801 - 810; DOI: 10.1021/jm00059a002 |
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Applications of neural networks in structure-activity relationships of a small number of molecules I. V. Tetko, A. I. Luik, and G. I. Poda pp 811 - 814; DOI: 10.1021/jm00059a003 |
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Synthesis and pharmacological evaluation of (nitrooxy)alkyl apovincaminate Yutaka Kawashima, Tomoyuki Ikemoto, Akiyo Horiguchi, Masatoshi Hayashi, Keita Matsumoto, Kimiko Kawarasaki, Ryuzaburo Yamazaki, Shigeru Okuyama, and Katsuo Hatayama pp 815 - 819; DOI: 10.1021/jm00059a004 |
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Modeling of human thromboxane A2 receptor and analysis of the receptor-ligand interaction Yoshio Yamamoto, Kazuhide Kamiya, and Shinji Terao pp 820 - 825; DOI: 10.1021/jm00059a005 |
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Synthesis and anti-HIV evaluation of D4T and D4T 5'-monophosphate prodrugs C. Sergheraert, C. Pierlot, A. Tartar, Y. Henin, and M. Lemaitre pp 826 - 830; DOI: 10.1021/jm00059a006 |
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Uniformly modified 2'-deoxy-2'-fluoro-phosphorothioate oligonucleotides as nuclease-resistant antisense compounds with high affinity and specificity for RNA targets Andrew M. Kawasaki, Martin D. Casper, Susan M. Freier, Elena A. Lesnik, Maryann C. Zounes, Lendell L. Cummins, Carolyn Gonzalez, and P. Dan Cook pp 831 - 841; DOI: 10.1021/jm00059a007 |
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Design, synthesis, and neurochemical evaluation of 5-(3-alkyl-1,2,4-oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidines as M1 muscarinic receptor agonists Philip G. Dunbar, Graham J. Durant, Zheng Fang, Yahaya F. Abuh, Afif A. El-Assadi, Dan O. Ngur, Sumudra Periyasamy, Wayne P. Hoss, and William S. Messer pp 842 - 847; DOI: 10.1021/jm00059a008 |
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Synthesis and biodistribution of iodine-125-labeled 1-azabicyclo[2.2.2]oct-3-yl .alpha.-hydroxy-.alpha.-(1-iodo-1-propen-3-yl)-.alpha.-phenylacetate. A new ligand for the potential imaging of muscarinic receptors by single photon emission computed tomography D. W. McPherson, D. L. DeHaven-Hudkins, A. P. Callahan, and F. F. Knapp pp 848 - 854; DOI: 10.1021/jm00059a009 |
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Substituted 3-phenyltropane analogs of cocaine: synthesis, inhibition of binding at cocaine recognition sites, and positron emission tomography imaging P. C. Meltzer, A. Y. Liang, A. L. Brownell, D. R. Elmaleh, and B. K. Madras pp 855 - 862; DOI: 10.1021/jm00059a010 |
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In vitro cytotoxicity of GC sequence directed alkylating agents related to distamycin Moses Lee, Andrea L. Rhodes, Michael D. Wyatt, Maurizio D'Incalci, Stephen Forrow, and John A. Hartley pp 863 - 870; DOI: 10.1021/jm00059a011 |
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Quinolone antibacterials containing the new 7-[3-(1-aminoethyl)-1-pyrrolidinyl] side chain: the effects of the 1-aminoethyl moiety and its stereochemical configurations on potency and in vivo efficacy John M. Domagala, Susan E. Hagen, Themis Joannides, John S. Kiely, Edgardo Laborde, Mel C. Schroeder, Josephine A. Sesnie, Martin A. Shapiro, Mark J. Suto, and Steven Vanderroest pp 871 - 882; DOI: 10.1021/jm00059a012 |
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Adenosine-5'-carboxaldehyde: a potent inhibitor of S-adenosyl-L-homocysteine hydrolase Siming Liu, Stanislaw F. Wnuk, Chongsheng Yuan, Morris J. Robins, and Ronald T. Borchardt pp 883 - 887; DOI: 10.1021/jm00059a013 |
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Position 2 and position 2/Ala15-substituted analogs of bovine growth hormone-releasing factor (bGRF) with enhanced metabolic stability and improved in vivo bioactivity Teresa M. Kubiak, Alan R. Friedman, Roger A. Martin, Avneet K. Ichhpurani, Glenn R. Alaniz, William H. Claflin, Martha C. Goodwin, Diane L. Cleary, Colleen R. Kelly, and et al. pp 888 - 897; DOI: 10.1021/jm00059a014 |
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Glycosylated derivatives of benzophenone, benzhydrol and benzhydril as potential venous antithrombotic agents Francois Bellamy, Derek Horton, Jean Millet, Francois Picart, Soth Samreth, and Jean Bernard Chazan pp 898 - 903; DOI: 10.1021/jm00059a015 |
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Synthesis and biological activities of angiotensin II, sarilesin, and sarmesin analogs containing Aze or Pip at position 7 John M. Matsoukas, George Agelis, John Hondrelis, Raghav Yamdagni, Qiao Wu, Renee Ganter, Diana Moore, Graham J. Moore, and Julian R. Smith pp 904 - 911; DOI: 10.1021/jm00059a016 |
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Synthesis and dopamine antagonist activity of 2-thioether derivatives of the ergoline ring system David E. Tupper, Ian A. Pullar, James A. Clemens, John Fairhurst, Francesca C. Risius, Graham H. Timms, and Susan Wedley pp 912 - 918; DOI: 10.1021/jm00059a017 |
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Prodrugs of doxorubicin and melphalan and their activation by a monoclonal antibody-penicillin-G amidase conjugate Vivekananda M. Vrudhula, Peter D. Senter, Keith J. Fischer, and Philip M. Wallace pp 919 - 923; DOI: 10.1021/jm00059a018 |
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Cyclic sulfolanes as novel and high-affinity P2 ligands for HIV-1 protease inhibitors Arun K. Ghosh, Wayne J. Thompson, Hee Yoon Lee, Sean P. McKee, Peter M. Munson, Tien T. Duong, Paul L. Darke, Joan A. Zugay, Emilio A. Emini, and et al. pp 924 - 927; DOI: 10.1021/jm00059a019 |
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The effect of NMeTyr5 substitution in luteinizing hormone-releasing hormone antagonists Fortuna Haviv, Timothy D. Fitzpatrick, Charles J. Nichols, Rolf E. Swenson, Nicholas A. Mort, Eugene N. Bush, Gilbert Diaz, A. T. Nguyen, Mark R. Holst, and et al. pp 928 - 933; DOI: 10.1021/jm00059a020 |
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Signal transduction by a 5-HT2 receptor: a mechanistic hypothesis from molecular dynamics simulations of the three-dimensional model of the receptor complexed to ligands Daqun Zhang and Harel Weinstein pp 934 - 938; DOI: 10.1021/jm00059a021 |
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Structure-activity relationships of imidazo[4,5-f]quinoline partial structures and analogs. Discovery of pyrazolo[3,4-f]quinoline derivatives as potent immunostimulants. [Erratum to document cited in CA118(21):212958y] Mikel P. Moyer, Frederick H. Weber, and Jonathan L. Gross pp 940 - 940; DOI: 10.1021/jm00059a022 |
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Book Reviews pp 939 - 939; DOI: 10.1021/jm00059a600 |
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Inhibitors of the protease from human immunodeficiency virus: synthesis, enzyme inhibition, and antiviral activity of a series of compounds containing the dihydroxyethylene transition-state isostere Suvit Thaisrivongs, Steve R. Turner, Joseph W. Strohbach, Ruth E. TenBrink, W. Gary Tarpley, Thomas J. McQuade, Robert L. Heinrikson, Alfredo G. Tomasselli, John O. Hui, and W. Jeffrey Howe pp 941 - 952; DOI: 10.1021/jm00060a001 |
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Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 4. 3-[2-(Benzoxazol-2-yl)ethyl]-5-ethyl-6-methylpyridin-2(1H)-one and analogs Jacob M. Hoffman, Anthony M. Smith, Clarence S. Rooney, Thorsten E. Fisher, John S. Wai, Craig M. Thomas, Dona L. Bamberger, James L. Barnes, Theresa M. Williams, and et al. pp 953 - 966; DOI: 10.1021/jm00060a002 |
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Binding-site modeling of the muscarinic m1 receptor: a combination of homology-based and indirect approaches Gunnar Nordvall and Uli Hacksell pp 967 - 976; DOI: 10.1021/jm00060a003 |
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Structure-activity relationships in the trans-hexahydroindolo[4,3-ab]phenanthridine ("benzergoline") series. 2. Resolution, absolute configuration, and dopaminergic activity of the selective D1 agonist CY 208-243 and its implication for an "extended rotamer-based dopamine receptor model" Max P. Seiler, Philipp Floersheim, Rudolf Markstein, and Armin Widmer pp 977 - 984; DOI: 10.1021/jm00060a004 |
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Nonsymmetrical bipiperidyls as inhibitors of vesicular acetylcholine storage S. M. N. Efange, A. Khare, S. M. Parsons, R. Bau, and T. Metzenthin pp 985 - 989; DOI: 10.1021/jm00060a005 |
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Design and modeling of new platelet-activating factor antagonists. 1. Synthesis and biological activity of 1,4-bis(3',4',5'-trimethoxybenzoyl)-2-[[(substituted carbonyl and carbamoyl)oxy]methyl]piperazines Aazdine Lamouri, Francoise Heymans, Fabrice Tavet, Georges Dive, Jean Pierre Batt, Nicole Blavet, Pierre Braquet, and Jean Jacques Godfroid pp 990 - 1000; DOI: 10.1021/jm00060a006 |
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Synthesis and evaluation of imidazo[1,5-a][1,4]benzodiazepine esters with high affinities and selectivities at "diazepam-insensitive" benzodiazepine receptors Zi Qiang Gu, Garry Wong, Celia Dominguez, Brian R. de Costa, Kenner C. Rice, and Phil Skolnick pp 1001 - 1006; DOI: 10.1021/jm00060a007 |
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Mechanistic interpretation of the genotoxicity of nitrofurans (antibacterial agents) using quantitative structure-activity relationships and comparative molecular field analysis Asim Kumar Debnath, Corwin Hansch, Ki H. Kim, and Yvonne C. Martin pp 1007 - 1016; DOI: 10.1021/jm00060a008 |
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Interaction of calcium channel antagonists with calcium: structural studies on verapamil and its Ca2+ complex Steve Tetreault and Vettai S. Ananthanarayanan pp 1017 - 1023; DOI: 10.1021/jm00060a009 |
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Nucleosides. 5. Synthesis of guanine and formycin B derivatives as potential inhibitors of purine nucleoside phosphorylase Ji Wang Chern, Horng Yuh Lee, Chien Shu Chen, Donna S. Shewach, Peter E. Daddona, and Leroy B. Townsend pp 1024 - 1031; DOI: 10.1021/jm00060a010 |
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Dicarboxylate diamide dimercaptide (N2S2) technetium-99m complexes: synthesis and biological evaluation as potential renal radiopharmaceuticals Daniel J. Canney, Jeffrey Billings, Lynn C. Francesconi, Yu Zhi Guo, Brian S. Haggerty, Arnold L. Rheingold, and Hank F. Kung pp 1032 - 1040; DOI: 10.1021/jm00060a011 |
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(Imidazolylphenyl)pyrrol-2-one inhibitors of cardiac cAMP phosphodiesterase John W. Lampe, Yuo Ling Chou, Reda G. Hanna, Susan V. Di Meo, Paul W. Erhardt, Alfred A. Hagedorn, William R. Ingebretsen, and Elinor Cantor pp 1041 - 1047; DOI: 10.1021/jm00060a012 |
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Intracellular delivery of bioactive AZT nucleotides by aryl phosphate derivatives of AZT Christopher McGuigan, Ranjith N. Pathirana, Jan Balzarini, and Erik De Clercq pp 1048 - 1052; DOI: 10.1021/jm00060a013 |
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Centrally acting serotonergic and dopaminergic agents. 1. Synthesis and structure-activity relationships of 2,3,3a,4,5,9b-hexahydro-1H-benz[e]indole derivatives Chiu Hong Lin, Susanne R. Haadsma-Svensson, Robert A. Lahti, Robert B. McCall, Montford F. Piercey, Peggy J. K. D. Schreur, Phillip F. Von Voigtlander, Martin W. Smith, and Connie G. Chidester pp 1053 - 1068; DOI: 10.1021/jm00060a014 |
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Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives Chiu Hong Lin, Susanne R. Haadsma-Svensson, Gillian Phillips, Robert A. Lahti, Robert B. McCall, Montford F. Piercey, Peggy J. K. D. Schreur, Phillip F. Von Voigtlander, Martin W. Smith, and Connie G. Chidester pp 1069 - 1083; DOI: 10.1021/jm00060a015 |
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Inhibition studies of some serine and thiol proteinases by new leupeptin analogs Rose M. McConnell, J. Lyndal York, Donna Frizzell, and Carole Ezell pp 1084 - 1089; DOI: 10.1021/jm00060a016 |
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Design of 5-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,3,4-thiadiazoles, -1,3,4-oxadiazoles, and -1,2,4-triazoles as orally active, nonulcerogenic antiinflammatory agents Michael D. Mullican, Michael W. Wilson, David T. Conner, Catherine R. Kostlan, Denis J. Schrier, and Richard D. Dyer pp 1090 - 1099; DOI: 10.1021/jm00060a017 |
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Synthesis and opioid activity of dynorphin A-(1-13)NH2 analogs containing cis- and trans-4-aminocyclohexanecarboxylic acid Kristin R. Snyder, Thomas F. Murray, Gary E. DeLander, and Jane V. Aldrich pp 1100 - 1103; DOI: 10.1021/jm00060a018 |
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N-(1-Methyl-5-indolyl)-N'-(3-pyridyl)urea hydrochloride: the first selective 5-HT1C receptor antagonist Ian T. Forbes, Guy A. Kennett, Angela Gadre, Peter Ham, Clare J. Hayward, Roger T. Martin, Mervyn Thompson, Martyn D. Wood, Gordon S. Baxter, and et al. pp 1104 - 1107; DOI: 10.1021/jm00060a019 |
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HIV inhibitory natural products. Part 7. The calanolides, a novel HIV-inhibitory class of coumarin derivatives from the tropical rainforest tree, Calophyllum lanigerum. [Erratum to document cited in CA117(11):108101g] Yoel Kashman, Kirk R. Gustafson, Richard W. Fuller, John H. Cardellina, James B. McMahon, Michael J. Currens, Robert W. Buckheit, Stephen H. Hughes, Gordon M. Cragg, and Michael R. Boyd pp 1110 - 1110; DOI: 10.1021/jm00060a020 |
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Book Reviews pp 1108 - 1109; DOI: 10.1021/jm00060a600 |
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Progestin 16.alpha.,17.alpha.-dioxolane ketals as molecular probes for the progesterone receptor: synthesis, binding affinity, and photochemical evaluation Philip R. Kym, Kathryn E. Carlson, and John A. Katzenellenbogen pp 1111 - 1119; DOI: 10.1021/jm00061a001 |
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Fluorine-18 labeled progestin ketals: synthesis and target tissue uptake selectivity of potential imaging agents for receptor-positive breast tumors Monica J. Kochanny, Henry F. VanBrocklin, Philip R. Kym, Kathryn E. Carlson, James P. O'Neil, Thomas A. Bonasera, Michael J. Welch, and John A. Katzenellenbogen pp 1120 - 1127; DOI: 10.1021/jm00061a002 |
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Bioactive ryanoids from nucleophilic additions to 4,12-seco-4,12-dioxoryanodine Phillip R. Jefferies, Elisabeth Lehmberg, Wing Wah Lam, and John E. Casida pp 1128 - 1135; DOI: 10.1021/jm00061a003 |
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Development of a pharmacophore for inhibition of human liver cytochrome P-450 2D6: molecular modeling and inhibition studies Gunter R. Strobl, Stephanie von Kruedener, Joachim Stoeckigt, F. Peter Guengerich, and Thomas Wolff pp 1136 - 1145; DOI: 10.1021/jm00061a004 |
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Synthesis and cytotoxicity of 1,6,7,8-substituted 2-(4'-substituted phenyl)-4-quinolones and related compounds: identification as antimitotic agents interacting with tubulin Sheng Chu Kuo, Hong Zin Lee, Jung Pin Juang, Yih Tyng Lin, Tian Shung Wu, Jer Jang Chang, Dan Lednicer, Kenneth D. Paull, Chii M. Lin, and et al. pp 1146 - 1156; DOI: 10.1021/jm00061a005 |
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5-[4-(Benzyloxy)phenyl]-1,3,4-oxadiazol-2(3H)-one derivatives and related analogs: new reversible, highly potent, and selective monoamine oxidase type B inhibitors Fathi Mazouz, Salah Gueddari, Claude Burstein, Daniel Mansuy, and Rene Milcent pp 1157 - 1167; DOI: 10.1021/jm00061a006 |
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Crystal and molecular structure and in vitro antiproliferative and antitumor activity of two organotin(IV) carbohydrate compounds Francesco Caruso, Marianne Bol-Schoenmakers, and Andre H. Penninks pp 1168 - 1174; DOI: 10.1021/jm00061a007 |
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Synthesis and structure-activity relationships of novel benzimidazole and imidazo[4,5-b]pyridine acid derivatives as thromboxane A2 receptor antagonists Eric Nicolai, Joel Goyard, Thierry Benchetrit, Jean Marie Teulon, Francois Caussade, Angela Virone, Chantal Delchambre, and Alix Cloarec pp 1175 - 1187; DOI: 10.1021/jm00061a008 |
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Synthesis and biological evaluation of 1-[1-(2-benzo[b]thienyl)cyclohexyl]piperidine homologs at dopamine-uptake and phencyclidine-, and .sigma.-binding sites Xiao Shu He, Lionel P. Raymon, Mariena V. Mattson, Mohyee E. Eldefrawi, and Brian R. de Costa pp 1188 - 1193; DOI: 10.1021/jm00061a009 |
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New indole derivatives as potent and selective serotonin uptake inhibitors Jean Luc Malleron, Claude Gueremy, Serge Mignani, Jean Francois Peyronel, Alain Truchon, Jean Charles Blanchard, Adam Doble, Pierre Laduron, Odile Piot, and et al. pp 1194 - 1202; DOI: 10.1021/jm00061a010 |
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Structure-function studies of amphiphilic antibacterial peptides Roberto Bessalle, Alfred Gorea, Itamar Shalit, Joerg W. Metzger, Chhabil Dass, Dominic M. Desiderio, and Mati Fridkin pp 1203 - 1209; DOI: 10.1021/jm00061a011 |
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Synthesis and phosphodiesterase activity of carboxylic acid mimetics of cyclic guanosine 3',5'-monophosphate Deen Tulshian, Michael Czarniecki, Ronald J. Doll, and Ho Sam Ahn pp 1210 - 1220; DOI: 10.1021/jm00061a012 |
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Synthesis and antiviral activity of novel isonucleoside analogs Joseph A. Tino, Junius M. Clark, A. Kirk Field, Glenn A. Jacobs, Karen A. Lis, Teresa L. Michalik, Bridgette McGeever-Rubin, William A. Slusarchyk, Steven H. Spergel, and et al. pp 1221 - 1229; DOI: 10.1021/jm00061a013 |
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Molecular shape comparison of angiotensin II receptor antagonists Brian B. Masek, Arshad Merchant, and James B. Matthew pp 1230 - 1238; DOI: 10.1021/jm00061a014 |
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Hybrids of antibiotics inhibiting protein synthesis. Synthesis and biological activity Jiri Zemlicka, M. C. Fernandez-Moyano, Mario Ariatti, Gary E. Zurenko, Joseph E. Grady, and Juan P. G. Ballesta pp 1239 - 1244; DOI: 10.1021/jm00061a015 |
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New nonpeptide angiotensin II receptor antagonists. 3. Synthesis, biological properties, and structure-activity relationships of 2-alkyl-4-(biphenylylmethoxy)pyridine derivatives Robert H. Bradbury, Christopher P. Allott, Michael Dennis, J. Alan Girdwood, Peter W. Kenny, John S. Major, Alec A. Oldham, Arnold H. Ratcliffe, Janet E. Rivett, and et al. pp 1245 - 1254; DOI: 10.1021/jm00061a016 |
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Site-specific conjugation of a radioiodinated phenethylamine derivative to a monoclonal antibody results in increased radioactivity localization in tumor Mark Kurth, Andre Pelegrin, Keith Rose, Robin E. Offord, Sibylle Pochon, Jean Pierre Mach, and Franz Buchegger pp 1255 - 1261; DOI: 10.1021/jm00061a017 |
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Benzylamine antioxidants: relationship between structure, peroxyl radical scavenging, lipid peroxidation inhibition and cytoprotection Melvin J. Yu, Jefferson R. McCowan, Lee A. Phebus, Richard D. Towner, Peter P. K. Ho, Priscilla T. Keith, Charlotte A. Luttman, Royal D. Saunders, Kenneth J. Ruterbories, and et al. pp 1262 - 1271; DOI: 10.1021/jm00061a018 |
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Thyroid hormone uptake by hepatocytes: structure-activity relationships of phenylanthranilic acids with inhibitory activity David K. Chalmers, Gerhard H. Scholz, Duncan J. Topliss, Emily Kolliniatis, Sharon L. A. Munro, David J. Craik, Magdy N. Iskander, and Jan R. Stockigt pp 1272 - 1277; DOI: 10.1021/jm00061a019 |
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Molecular size and flexibility as determinants of selectivity in the oxidation of N-methyl-4-phenyl-1,2,3,6-tetrahydropyridine analogs by monoamine oxidase A and B S. M. N. Efange, R. H. Michelson, A. K. Tan, M. J. Krueger, and T. P. Singer pp 1278 - 1283; DOI: 10.1021/jm00061a020 |
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Design and synthesis of 18F-labeled neurotoxic analogs of MPTP Marc S. Berridge, Lawrence M. Sayre, Pramod K. Arora, Andrew H. Terris, Naji J. Riachi, and Sami I. Harik pp 1284 - 1290; DOI: 10.1021/jm00061a021 |
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5-Chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase Theresa M. Williams, Terrence M. Ciccarone, Suzanne C. MacTough, Clarence S. Rooney, Suresh K. Balani, Jon H. Condra, Emilio A. Emini, Mark E. Goldman, William J. Greenlee, and et al. pp 1291 - 1294; DOI: 10.1021/jm00061a022 |
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Statistics using neural networks: chance effects David J. Livingstone and David T. Manallack pp 1295 - 1297; DOI: 10.1021/jm00061a023 |
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Book Reviews pp 1298 - 1300; DOI: 10.1021/jm00061a600 |
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Comparison of 5-HT1A and dopamine D2 pharmacophores. X-ray structures and affinities of conformationally constrained ligands Connie G. Chidester, Chiu Hong Lin, Robert A. Lahti, Susanne R. Haadsma-Svensson, and Martin W. Smith pp 1301 - 1315; DOI: 10.1021/jm00062a001 |
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Preparation and pharmacological evaluation of enantiomers of certain nonoxygenated aporphines: (+)- and (-)-aporphine and (+)- and (-)-10-methylaporphine Joseph G. Cannon, Revathi Raghupathi, Scott T. Moe, Alan K. Johnson, and John Paul Long pp 1316 - 1318; DOI: 10.1021/jm00062a002 |
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Amino- and guanidinoacylryanodines: basic ryanodine esters with enhanced affinity for the sarcoplasmic reticulum calcium (2+)-release channel Koert Gerzon, Rod A. Humerickhouse, Henry R. Besch, Keshore R. Bidasee, Jeffrey T. Emmick, Roger W. Roeske, Zhenping Tian, Luc Ruest, and John L. Sutko pp 1319 - 1323; DOI: 10.1021/jm00062a003 |
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Interaction of calcium channel antagonists with calcium: spectroscopic and modeling studies on diltiazem and its Ca2+ complex V. S. Ananthanarayanan, Steve Tetreault, and Andre Saint-Jean pp 1324 - 1332; DOI: 10.1021/jm00062a004 |
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Structure-activity relationships of 8-styrylxanthines as A2-selective adenosine antagonists Kenneth A. Jacobson, Carola Gallo-Rodriguez, Neli Melman, Bilha Fischer, Michel Maillard, Andrew van Bergen, Philip J. M. van Galen, and Yishai Karton pp 1333 - 1342; DOI: 10.1021/jm00062a005 |
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Novel acyclonucleotides: synthesis and antiviral activity of alkenylphosphonic acid derivatives of purines and a pyrimidine Michael R. Harnden, Ann Parkin, Martin J. Parratt, and Robert M. Perkins pp 1343 - 1355; DOI: 10.1021/jm00062a006 |
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Quinolone antimicrobial agents substituted with morpholines at the 7-position. Syntheses and structure-activity relationships Kazuhiko Araki, Tsuyoshi Kuroda, Satoru Uemori, Akihiko Moriguchi, Yoshifumi Ikeda, Fumihiro Hirayama, Yoshito Yokoyama, Eiji Iwao, and Takashi Yakushiji pp 1356 - 1363; DOI: 10.1021/jm00062a007 |
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Synthesis and antitumor activity of isodoxorubicin analogs Jean Claude Florent, Gilbert Gaudel, Claude Monneret, Dieter Hoffmann, and Hans Peter Kraemer pp 1364 - 1368; DOI: 10.1021/jm00062a008 |
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Synthesis and analgesic effects of N-[3-[(hydroxyamino)carbonyl]-1-oxo-2(R)-benzylpropyl]-L-isoleucyl-L-leucine, a new potent inhibitor of multiple neurotensin/neuromedin N degrading enzymes Sylvie Doulut, Isabelle Dubuc, M. Rodriguez, F. Vecchini, H. Fulcrand, H. Barelli, F. Checler, E. Bourdel, A. Aumelas, and et al. pp 1369 - 1379; DOI: 10.1021/jm00062a009 |
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Bronchodilator activity of xanthine derivatives substituted with functional groups at the 1- or 7-position Kenichi Miyamoto, Yasunori Yamamoto, Mariko Kurita, Ryosuke Sakai, Kayo Konno, Fujiko Sanae, Taeyuki Ohshima, Kenzo Takagi, Takaaki Hasegawa, and et al. pp 1380 - 1386; DOI: 10.1021/jm00062a010 |
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Cyclic nucleotide phosphodiesterase inhibition by imidazopyridines: analogs of sulmazole and isomazole as inhibitors of the cGMP specific phosphodiesterase William J. Coates, Brendan Connolly, Dashyant Dhanak, Sean T. Flynn, and Angela Worby pp 1387 - 1392; DOI: 10.1021/jm00062a011 |
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Aromatase inhibitors: synthesis, biological activity, and binding mode of azole-type compounds P. Furet, C. Batzl, A. Bhatnagar, E. Francotte, G. Rihs, and M. Lang pp 1393 - 1400; DOI: 10.1021/jm00062a012 |
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Interphenylene 7-oxabicyclo[2.2.1]heptane oxazoles. Highly potent, selective, and long-acting thromboxane A2 receptor antagonists Raj N. Misra, Baerbel R. Brown, Philip M. Sher, Manorama M. Patel, Steven E. Hall, Wen Ching Han, Joel C. Barrish, Octavian Kocy, Don N. Harris, and et al. pp 1401 - 1417; DOI: 10.1021/jm00062a013 |
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Mechanism-based inhibitors of prostaglandin .omega.-hydroxylase: (R)- and (S)-12-hydroxy-16-heptadecynoic acid and 2,2-dimethyl-12-hydroxy-16-heptadecynoic acid Alain Burger, Joan E. Clark, Masazumi Nishimoto, A. Scott Muerhoff, Bettie Sue Siler Masters, and Paul R. Ortiz de Montellano pp 1418 - 1424; DOI: 10.1021/jm00062a014 |
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Novel heterocyclic analogs of the new potent class of calcium entry blockers: 1-[[4-(aminoalkoxy)phenyl]sulfonyl]indolizines Jean Gubin, Hendrik de Vogelaer, Henri Inion, Christian Houben, Jean Lucchetti, Jean Mahaux, Gilbert Rosseels, Maurits Peiren, Martine Clinet, and et al. pp 1425 - 1433; DOI: 10.1021/jm00062a015 |
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2'-Substituted chalcone derivatives as inhibitors of interleukin-1 biosynthesis Douglas G. Batt, Robin Goodman, David G. Jones, Janet S. Kerr, Lisa R. Mantegna, Candice McAllister, Robert C. Newton, Sherrill Nurnberg, Patricia K. Welch, and Maryanne B. Covington pp 1434 - 1442; DOI: 10.1021/jm00062a016 |
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Application of the hypersurface iterative projection method to bicyclic pyrazolidinone antibacterial agents Donald B. Boyd pp 1443 - 1449; DOI: 10.1021/jm00062a017 |
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NMR and computational evidence that high-affinity bradykinin receptor antagonists adopt C-terminal .beta.-turns Donald J. Kyle, Paul R. Blake, Damon Smithwick, Lora M. Green, Jennifer A. Martin, Jacqueline A. Sinsko, and Michael F. Summers pp 1450 - 1460; DOI: 10.1021/jm00062a018 |
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Structure-activity relationship for mitomycins. Application of the distance and charge analysis method Nobuyuki Yoda and Noriaki Hirayama pp 1461 - 1464; DOI: 10.1021/jm00062a019 |
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Long-chain-substituted uric acid and 5,6-diaminouracil derivatives as novel agents against free radical processes: synthesis and in vitro activity Laurent Fraisse, Jean Baptiste Verlhac, Beatrice Roche, Marie Claude Rascle, Alain Rabion, and Jean Louis Seris pp 1465 - 1473; DOI: 10.1021/jm00062a020 |
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Antitumor agents. 141. Synthesis and biological evaluation of novel thiocolchicine analogs: N-acyl, N-aroyl-, and N-(substituted benzyl)deacetylthiocolchicines as potent cytotoxic and antimitotic compounds Li Sun, Ernest Hamel, Chii M. Lin, Susan B. Hastie, Amy Pyluck, and Kuo Hsiung Lee pp 1474 - 1479; DOI: 10.1021/jm00062a021 |
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Synthesis and biological activity of spirocyclic benzopyran imidazolone potassium channel openers Robert C. Gadwood, Bharat V. Kamdar, Loretta A. Cipkus Dubray, Mark L. Wolfe, Michael P. Smith, William Watt, Stephen A. Mizsak, and Vincent E. Groppi pp 1480 - 1487; DOI: 10.1021/jm00062a022 |
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Bridged .gamma.-carbolines and derivatives possessing selective and combined affinity for 5-HT2 and D2 receptors Richard E. Mewshaw, Lisa S. Silverman, Rose M. Mathew, Carl Kaiser, Ronald G. Sherrill, Menyan Cheng, Carol W. Tiffany, E. William Karbon, Michael A. Bailey, and et al. pp 1488 - 1495; DOI: 10.1021/jm00062a023 |
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Orally active water-soluble N,O-acyl transfer products of a .beta.,.gamma.-bishydroxyl amide containing renin inhibitor Timothy R. Hurley, Charles E. Colson, Gary Hicks, and Michael J. Ryan pp 1496 - 1498; DOI: 10.1021/jm00062a024 |
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Synthesis of (.+-.)-2'-trans-7-hydroxy-2-[N-(3'-iodo-2'-propenyl)-N-n-propylamino]tetralin (trans-7-OH-PIPAT): a new D3 dopamine receptor ligand Catherine Foulon, Mei Ping Kung, and Hank F. Kung pp 1499 - 1500; DOI: 10.1021/jm00062a025 |
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N-(Arylalkyl)farnesylamines: new potent squalene synthetase inhibitors Mahavir Prashad, F. G. Kathawala, and T. Scallen pp 1501 - 1504; DOI: 10.1021/jm00062a026 |
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Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogs and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)carbonyl]-4-[3-[(1-methylethyl)amino]pyridinyl]piperazinemonomethanesulfonate (U-90152S), a second-generation clinical candidate Donna L. Romero, Raymond A. Morge, Michael J. Genin, Carolyn Biles, Mariano Busso, Lionel Resnick, Irene W. Althaus, Fritz Reusser, Richard C. Thomas, and William G. Tarpley pp 1505 - 1508; DOI: 10.1021/jm00062a027 |
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(S)-N-tert-Butyl-3-(4-(2-methoxyphenyl)piperazin-1-yl)-2-phenylpropanamide [(S)-WAY-100135]: a selective antagonist at presynaptic and postsynaptic 5-HT1A receptors Ian A. Cliffe, Christopher I. Brightwell, Allan Fletcher, Elaine A. Forster, Howard L. Mansell, Yvonne Reilly, Carol Routledge, and Alan C. White pp 1509 - 1510; DOI: 10.1021/jm00062a028 |
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Synthesis and amnesia-reversal activity of a series of 7- and 5-membered 3-acylamino lactams Luciano Angelucci, Pina Calvisi, Roberto Catini, Ugo Cosentino, Roberto Cozzolino, Paolo De Witt, Orlando Ghirardi, Fabio Giannessi, Alessandro Giuliani, and et al. pp 1511 - 1519; DOI: 10.1021/jm00063a001 |
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Structure-activity relationships in 1,4-benzodioxan-related compounds. 4. Effect of aryl and alkyl substituents at position 3 on .alpha.-adrenoreceptor blocking activity Wilma Quaglia, Maria Pigini, Seyed K. Tayebati, Alessandro Piergentili, Mario Giannella, Gabriella Marucci, and Carlo Melchiorre pp 1520 - 1528; DOI: 10.1021/jm00063a002 |
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Synthesis and serotonergic activity of 5-(oxadiazolyl)tryptamines: potent agonists for 5-HT1D receptors Leslie J. Street, Raymond Baker, Jose L. Castro, Mark S. Chambers, Alexander R. Guiblin, Sarah C. Hobbs, Victor G. Matassa, Austin J. Reeve, Margaret S. Beer, and et al. pp 1529 - 1538; DOI: 10.1021/jm00063a003 |
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New mechanism-based inactivators of trypsin-like proteinases. Selective inactivation of urokinase by functionalized cyclopeptides incorporating a sulfoniomethyl-substituted m-aminobenzoic acid residue Michel Wakselman, Juan Xie, Jean Paul Mazaleyrat, Nicole Boggetto, Anne Cecile Vilain, Jean Jacques Montagne, and Michele Reboud-Ravaux pp 1539 - 1547; DOI: 10.1021/jm00063a004 |
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A molecular dynamics study of the bis-intercalation complexes of echinomycin with d(ACGT)2 and d(TCGA)2: rationale for sequence-specific Hoogsteen base pairing Jose Gallego, Angel R. Ortiz, and Federico Gago pp 1548 - 1561; DOI: 10.1021/jm00063a005 |
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Modeling the anticancer action of some retinoid compounds by making use of the OASIS method D. Bonchev, C. F. Mountain, W. A. Seitz, and A. T. Balaban pp 1562 - 1569; DOI: 10.1021/jm00063a006 |
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Synthesis of 2'-deoxyuridine and 5-fluoro-2'-deoxyuridine derivatives and evaluation in antibody targeting studies Thomas F. G. Henn, Martin C. Garnett, Siri Ram Chhabra, Barrie W. Bycroft, and Robert W. Baldwin pp 1570 - 1579; DOI: 10.1021/jm00063a007 |
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3-Quinolinecarboxamides. A series of novel orally-active antiherpetic agents Mark P. Wentland, Robert B. Perni, Peter H. Dorff, R. Pauline Brundage, Michael J. Castaldi, Thomas R. Bailey, Philip M. Carabateas, Edward R. Bacon, Dorothy C. Young, and et al. pp 1580 - 1596; DOI: 10.1021/jm00063a008 |
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A novel series of N-(1-aminoalkylidene)carboximidamides as potential hypoglycemia agents Henry J. Breslin, Michael J. Kukla, Robert W. Tuman, Mary C. Rebarchak, and Charles R. Bowden pp 1597 - 1603; DOI: 10.1021/jm00063a009 |
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Syntheses and biological activities of potent potassium channel openers derived from (.+-.)-2-oxo-1-pyridin-3-yl-cyclohexanecarbothioic acid methylamide: new potassium channel openers Thomas J. Brown, Robert F. Chapman, Jonathan S. Mason, Malcolm N. Palfreyman, Nigel Vicker, and Roger J. A. Walsh pp 1604 - 1612; DOI: 10.1021/jm00063a010 |
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Dibenzoxepin derivatives: thromboxane A2 synthase inhibition and thromboxane A2 receptor antagonism combined in one molecule Etsuo Ohshima, Hideyuki Sato, Hiroyuki Obase, Ichiro Miki, Akio Ishii, Michiyo Kawakage, Shiro Shirakura, Akira Karasawa, and Kazuhiro Kubo pp 1613 - 1618; DOI: 10.1021/jm00063a011 |
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16.beta.-([18F]Fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors Henry F. VanBrocklin, Kathryn E. Carlson, John A. Katzenellenbogen, and Michael J. Welch pp 1619 - 1629; DOI: 10.1021/jm00063a012 |
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Structure-activity relationship of N-[2-(dimethylamino)-6-[3-(5-methyl-4-phenyl-1H-imidazol-1-yl)propoxy]phenyl]-N'-pentylurea and analogs. Novel potent inhibitors of acyl-CoA:cholesterol O-acyltransferase with antiatherosclerotic activity Teiji Kimura, Yasutaka Takase, Kenji Hayashi, Hiroshi Tanaka, Issei Ohtsuka, Takao Saeki, Motoji Kogushi, Toshie Yamada, Tohru Fujimori, and et al. pp 1630 - 1640; DOI: 10.1021/jm00063a013 |
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Structure-activity relationship of a series of phenylureas linked to 4-phenylimidazole. Novel potent inhibitors of acyl-CoA:cholesterol O-acyltransferase with antiatherosclerotic activity. 2 Teiji Kimura, Nobuhisa Watanabe, Makoto Matsui, Kenji Hayashi, Hiroshi Tanaka, Issei Ohtsuka, Takao Saeki, Motoji Kogushi, Hiroko Kabayashi, and et al. pp 1641 - 1653; DOI: 10.1021/jm00063a014 |
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Tetrapeptide tachykinin antagonists: synthesis and modulation of the physicochemical and pharmacological properties of a new series of partially cyclic analogs Nathalie Kucharczyk, Christophe Thurieau, Joseph Paladino, Angela D. Morris, Jacqueline Bonnet, Emmanuel Canet, James E. Krause, Domenico Regoli, Rejean Couture, and Jean Luc Fauchere pp 1654 - 1661; DOI: 10.1021/jm00063a015 |
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Inhibitors of acyl-CoA:cholesterol acyltransferase (ACAT). 2. Modification of fatty acid anilide ACAT inhibitors: bioisosteric replacement of the amide bond W. Howard Roark, Bruce D. Roth, Ann Holmes, Bharat K. Trivedi, Karen A. Kieft, Arnold D. Essenburg, Brian R. Krause, and Richard L. Stanfield pp 1662 - 1668; DOI: 10.1021/jm00063a016 |
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Structure-activity relationship studies at benzodiazepine receptor (BZR): a comparison of the substituent effects of pyrazoloquinolinone analogs R. Ian Fryer, Puwen Zhang, Roberto Rios, Zi Qiang Gu, Anthony S. Basile, and Phil Skolnick pp 1669 - 1673; DOI: 10.1021/jm00063a017 |
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A new candidate for an anti-HIV-1 agent: modified cyclodextrin sulfate (mCDS71) Tamon Moriya, Kiyosi Saito, Hironori Kurita, Kazuo Matsumoto, Toru Otake, Haruyo Mori, Motoko Morimoto, Noboru Ueba, and Nobuharu Kunita pp 1674 - 1677; DOI: 10.1021/jm00063a018 |
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Effects of solvation on the ionization and conformation of raclopride and other antidopaminergic 6-methoxysalicylamides: insight into the pharmacophore. [Erratum to document cited in CA118(7):51870w] Ruey Shiuan Tsai, Pierre Alain Carrupt, Bernard Testa, Patrick Gaillard, Nabil El Tayar, and Thomas Hoegberg pp 1680 - 1680; DOI: 10.1021/jm00063a019 |
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Book Review pp 1678 - 1679; DOI: 10.1021/jm00063a600 |
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Synthesis of human CCK26-33 and CCK-33 related analogs on 2,4-DMBHA and TMBHA Maria Teresa Machini Miranda, Rodger A. Liddle, and Jean E. Rivier pp 1681 - 1688; DOI: 10.1021/jm00064a001 |
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Antitumor agents. 3. Synthesis and biological activity of 4.beta.-alkyl derivatives containing hydroxy, amino, and amido groups of 4'-O-demethyl-4-desoxypodophyllotoxin as antitumor agents Tadafumi Terada, Katsuhiko Fujimoto, Makoto Nomura, Junichi Yamashita, Konstanty Wierzba, Ryoko Yamazaki, Jiro Shibata, Yoshikazu Sugimoto, Yuji Yamada, and et al. pp 1689 - 1699; DOI: 10.1021/jm00064a002 |
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GroupBuild: a fragment-based method for de novo drug design Sergio H. Rotstein and Mark A. Murcko pp 1700 - 1710; DOI: 10.1021/jm00064a003 |
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Transformation of monoamine oxidase-B primary amine substrates into time-dependent inhibitors. Tertiary amine homologs of primary amine substrates Charles Z. Ding, Xingliang Lu, Kuniko Nishimura, and Richard B. Silverman pp 1711 - 1715; DOI: 10.1021/jm00064a004 |
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The synthesis of novel GABA uptake inhibitors. 1. Elucidation of the structure-activity studies leading to the choice of (R)-1-[4,4-bis(3-methyl-2-thienyl)-3-butenyl]-3-piperidinecarboxylic acid (Tiagabine) as an anticonvulsant drug candidate Knud Erik Andersen, Claus Braestrup, Frederik C. Groenwald, Anker S. Joergensen, Erik B. Nielsen, Ursula Sonnewald, Per O. Soerensen, Peter D. Suzdak, and Lars J. S. Knutsen pp 1716 - 1725; DOI: 10.1021/jm00064a005 |
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Design, synthesis, and pharmacological evaluation of potent xanthone dicarboxylic acid leukotriene B4 receptor antagonists William T. Jackson, Robert J. Boyd, Larry L. Froelich, D. Mark Gapinski, Barbara E. Mallett, and J. Scott Sawyer pp 1726 - 1734; DOI: 10.1021/jm00064a006 |
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Nonpeptide angiotensin II receptor antagonists. 1. Synthesis and in vitro structure-activity relationships of 4-[[[(1H-pyrrol-1-ylacetyl)amino]phenyl]methyl]imidazole derivatives as angiotensin II receptor antagonists Ila Sircar, R. Thomas Winters, John Quin, Gina H. Lu, Terry C. Major, and Robert L. Panek pp 1735 - 1745; DOI: 10.1021/jm00064a007 |
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Structure, DNA minor groove binding, and base pair specificity of alkyl- and aryl-linked bis(amidinobenzimidazoles) and bis(amidinoindoles) Terri A. Fairley, Richard R. Tidwell, Isaac Donkor, Noreen A. Naiman, Kwasi A. Ohemeng, Richard J. Lombardy, James A. Bentley, and Michael Cory pp 1746 - 1753; DOI: 10.1021/jm00064a008 |
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Synthesis and tissue distribution of iodine-125-labeled (m-[125I]iodobenzyl)trozamicol ([125I]MIBT): potential radioligand for mapping central cholinergic innervation S. M. N. Efange, R. H. Michelson, A. B. Khare, and J. R. Thomas pp 1754 - 1760; DOI: 10.1021/jm00064a009 |
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Characterization of a region of steric interference at the cannabinoid receptor using the active analog approach Patricia H. Reggio, Al M. Panu, and Scott Miles pp 1761 - 1771; DOI: 10.1021/jm00064a010 |
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Nonpeptide angiotensin II receptor antagonists. Synthesis and biological activity of benzimidazoles Keiji Kubo, Yoshiyuki Inada, Yasuhisa Kohara, Yoshihiro Sugiura, Mami Ojima, Katsuhiko Itoh, Yoshiyasu Furukawa, Kohei Nishikawa, and Takehiko Naka pp 1772 - 1784; DOI: 10.1021/jm00064a011 |
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Nucleoside conjugates. 13. Synthesis and antitumor activity of 1-.beta.-D-arabinofuranosylcytosine conjugates of thioether lipids with improved water solubility Chung Il Hong, Alexander Nechaev, Alan J. Kirisits, Rakesh Vig, and Charles R. West pp 1785 - 1790; DOI: 10.1021/jm00064a012 |
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Synthesis, characterization, and anticancer activities of the first platinum complexes from sucrose Navzer D. Sachinvala, Hong Chen, Walter P. Niemczura, Eiichi Furusawa, Roger E. Cramer, John J. Rupp, and Iraj Ganjian pp 1791 - 1795; DOI: 10.1021/jm00064a013 |
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Book Reviews pp 1796 - 1796; DOI: 10.1021/jm00064a600 |
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Synthesis and evaluation of the antitumor activity of 4,5-diamino-substituted 1,2-benzoquinones Zhen Dong Huang, Ying Nan Chen, Krishna Menon, and Beverly A. Teicher pp 1797 - 1801; DOI: 10.1021/jm00065a001 |
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1,3,4-Oxadiazole, 1,3,4-thiadiazole, and 1,2,4-triazole analogs of the fenamates: in vitro inhibition of cyclooxygenase and 5-lipoxygenase activities Diane H. Boschelli, David T. Connor, Dirk A. Bornemeier, Richard D. Dyer, John A. Kennedy, Paul J. Kuipers, Godwin C. Okonkwo, Denis J. Schrier, and Clifford D. Wright pp 1802 - 1810; DOI: 10.1021/jm00065a002 |
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Potent in vitro and in vivo inhibitors of platelet aggregation based upon the Arg-Gly-Asp-Phe sequence of fibrinogen. A proposal on the nature of the binding interaction between the Arg-guanidine of RGDX mimetics and the platelet GP IIb-IIIa receptor Jeffery A. Zablocki, Masateru Miyano, Robert B. Garland, Daisy Pireh, Lori Schretzman, Shashidhar N. Rao, Richard J. Lindmark, Susan G. Panzer-Knodle, Nancy S. Nicholson, and et al. pp 1811 - 1819; DOI: 10.1021/jm00065a003 |
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Synthetic and computer-assisted analysis of the structural requirements for selective, high-affinity ligand binding to diazepam-insensitive benzodiazepine receptors Garry Wong, Konrad F. Koehler, Phil Skolnick, Zi Qiang Gu, Subramaniam Ananthan, Peter Schonholzer, Walter Hunkeler, Weijiang Zhang, and James M. Cook pp 1820 - 1830; DOI: 10.1021/jm00065a004 |
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The solution conformation of (D)Phe-Pro-containing peptides: implications on the activity of Ac-(D)Phe-Pro-boroArg-OH, a potent thrombin inhibitor Marguerita S. L. Lim, Eric R. Johnston, and Charles A. Kettner pp 1831 - 1838; DOI: 10.1021/jm00065a005 |
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Hypoxia-selective antitumor agents. 7. Metal complexes of aliphatic mustards as a new class of hypoxia-selective cytotoxins. Synthesis and evaluation of cobalt(III) complexes of bidentate mustards David C. Ware, Brian D. Palmer, William R. Wilson, and William A. Denny pp 1839 - 1846; DOI: 10.1021/jm00065a006 |
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Structure-based design of inhibitors of purine nucleoside phosphorylase. 2. 9-Alicyclic and 9-heteroalicyclic derivatives of 9-deazaguanine John A. Secrist, Shri Niwas, Jerry D. Rose, Y. Sudhakar Babu, Charles E. Bugg, Mark D. Erion, Wayne C. Guida, Steven E. Ealick, and John A. Montgomery pp 1847 - 1854; DOI: 10.1021/jm00065a007 |
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NAD analogs. 1. Synthesis of isosteric analogs of nicotinamide adenine dinucleotide containing C-nucleotide of nicotinamide or picolinamide Krzysztof W. Pankiewicz, Joanna Zeidler, Lech A. Ciszewski, J. Ellis Bell, Barry M. Goldstein, Hiremagalur N. Jayaram, and Kyoichi A. Watanabe pp 1855 - 1859; DOI: 10.1021/jm00065a008 |
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Non-peptide ligands for opioid receptors. Design of .kappa.-specific agonists G. Ronsisvalle, L. Pasquinucci, M. S. Pappalardo, F. Vittorio, G. Fronza, C. Romagnoli, E. Pistacchio, S. Spampinato, and S. Ferri pp 1860 - 1865; DOI: 10.1021/jm00065a009 |
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Molecular model of the interaction of bee venom phospholipase A2 with manoalide Angel R. Ortiz, M. Teresa Pisabarro, and Federico Gago pp 1866 - 1879; DOI: 10.1021/jm00065a010 |
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Potent nonpeptide angiotensin II receptor antagonists. 2. 1-(Carboxybenzyl)imidazole-5-acrylic acids Richard M. Keenan, Joseph Weinstock, Joseph A. Finkelstein, Robert G. Franz, Dimitri E. Gaitanopoulos, Gerald R. Girard, David T. Hill, Tina M. Morgan, James M. Samanen, and et al. pp 1880 - 1892; DOI: 10.1021/jm00065a011 |
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Inhibition and inactivation of presynaptic cholinergic markers using redox-reactive choline analogs Phenil J. Patel, William S. Messer, and Richard A. Hudson pp 1893 - 1901; DOI: 10.1021/jm00065a012 |
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Multiple binding modes for the receptor-bound conformations of cyclic AII agonists Krystina Plucinska, Takahiro Kataoka, Mitsuaki Yodo, Wayne L. Cody, J. X. He, Christine Humblet, G. H. Lu, Elizabeth Lunney, Terry C. Major, and et al. pp 1902 - 1913; DOI: 10.1021/jm00065a013 |
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Enantioselectivity of cocaine recognition sites: binding of (1S)- and (1R)-2.beta.-carbomethoxy-3.beta.-(4-iodophenyl)tropane (.beta.-CIT) to monoamine transporters Shaoyin Wang, Yigong Gao, Marc Laruelle, Ronald M. Baldwin, B. Ellen Scanley, Robert B. Innis, and John L. Neumeyer pp 1914 - 1917; DOI: 10.1021/jm00065a014 |
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(.+-.)-3-Amino-6-carboxamido-1,2,3,4-tetrahydrocarbazole: a conformationally restricted analog of 5-carboxamidotryptamine with selectivity for the serotonin 5-HT1D receptor Frank D. King, Anthony M. Brown, Laramie M. Gaster, Alberto J. Kaumann, Andrew D. Medhurst, Stephen G. Parker, Andrew A. Parsons, Tracey L. Patch, and Pravin Raval pp 1918 - 1919; DOI: 10.1021/jm00065a015 |
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Book Reviews pp 1920 - 1920; DOI: 10.1021/jm00065a600 |
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Additions and Corrections - Studies on Pyridonecarboxylic Acids. 1. Synthesis and Antibacterial Evaluation of 7-Substituted-6-halo-4-oxo-4H-[1,3]thiazeto[3,2-α]quinoline-3-carboxylic Acids. Jun Segawa, Mashiko Kitano, Kenji Kazuno, Masato Matsuoka, Ichiro Shirahase, Masakuni Ozaki, Masato Matsuda, Yoshifumi Tomii, and Masahiro Kise pp 1921 - 1921; DOI: 10.1021/jm00065a601 |
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Additions and Corrections - Synthesis and Opioid Activity of Dynorphin-A-(1-13)NH2 Analogues Containing cis- and trans-4-Aminocyclohexanecarboxylic Acid Kristin R. Snyder, Thomas F. Murray, Gary E. DeLander, and Jane V. Aldrich pp 1921 - 1922; DOI: 10.1021/jm00065a602 |
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Current concepts in antisense drug design John F. Milligan, Mark D. Matteucci, and John C. Martin pp 1923 - 1937; DOI: 10.1021/jm00066a001 |
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10,5-(Iminomethano)-10,11-dihydro-5H-dibenzo[a,d]cycloheptene and derivatives. Potent PCP receptor ligands Kyle R. Gee, Peter Barmettler, Michael R. Rhodes, Robert N. McBurney, N. Laxma Reddy, Lain Yen Hu, Ronald E. Cotter, Philip N. Hamilton, Eckard Weber, and John F. W. Keana pp 1938 - 1946; DOI: 10.1021/jm00066a002 |
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Synthesis and anticonvulsant activity of enaminones. 2. Further structure-activity correlations K. R. Scott, Ivan O. Edafiogho, Erica L. Richardson, Vida A. Farrar, Jacqueline A. Moore, Elizabeth I. Tietz, Christine N. Hinko, Hyejung Chang, Afif El-Assadi, and Jesse M. Nicholson pp 1947 - 1955; DOI: 10.1021/jm00066a003 |
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Synthesis and biochemical evaluation of the CBI-PDE-I-dimer, a benzannelated analog of (+)-CC-1065 that also produces delayed toxicity in mice Paul A. Aristoff, Paul D. Johnson, Daekyu Sun, and Laurence H. Hurley pp 1956 - 1963; DOI: 10.1021/jm00066a004 |
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Quinolone antibacterials: synthesis and biological activity of carbon isosteres of the 1-piperazinyl and 3-amino-1-pyrrolidinyl side chains Edgardo Laborde, John S. Kiely, Townley P. Culbertson, and Lawrence E. Lesheski pp 1964 - 1970; DOI: 10.1021/jm00066a005 |
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Discovery and structure-activity relationship of a series of 1-carba-1-dethiacephems exhibiting activity against methicillin-resistant Staphylococcus aureus Robert J. Ternansky, Susan E. Draheim, Andrew J. Pike, F. William Bell, Sarah J. West, Christopher L. Jordan, C. Y. Ernie Wu, David A. Preston, William Alborn Jr., and et al. pp 1971 - 1976; DOI: 10.1021/jm00066a006 |
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Synthesis and pharmacological evaluation of 4a-phenanthrenamine derivatives acting at the phencyclidine binding site of the N-methyl-D-aspartate receptor complex Christopher F. Bigge, Thomas C. Malone, Sheryl J. Hays, Graham Johnson, Perry M. Novak, Leonard J. Lescosky, Daniel M. Retz, Daniel F. Ortwine, Albert W. Probert Jr., and et al. pp 1977 - 1995; DOI: 10.1021/jm00066a007 |
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Structure-activity relationship studies with symmetric naphthalenesulfonic acid derivatives. Synthesis and influence of spacer and naphthalenesulfonic acid moiety on anti-HIV-1 activity Prem Mohan, Man Fai Wong, Sandeep Verma, Peggy P. Huang, Anura Wickramasinghe, and Masanori Baba pp 1996 - 2003; DOI: 10.1021/jm00066a008 |
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Synthesis of and radioligand binding studies with a tritiated pinacidil analog: receptor interactions of structurally different classes of potassium channel openers and blockers Paul W. Manley, Ulrich Quast, Hendrik Andres, and Katharine Bray pp 2004 - 2010; DOI: 10.1021/jm00066a009 |
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Orally active, nonpeptide vasopressin V1 antagonists. A novel series of 1-(1-substituted 4-piperidyl)-3,4-dihydro-2(1H)-quinolinones Hidenori Ogawa, Yoshitaka Yamamura, Hisashi Miyamoto, Kazumi Kondo, Hiroshi Yamashita, Kenji Nakaya, Tomihiko Chihara, Toyoki Mori, Michiaki Tominaga, and Youichi Yabuuchi pp 2011 - 2017; DOI: 10.1021/jm00066a010 |
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Synthesis of phosphocholine and quaternary amine ether lipids and evaluation of in vitro antineoplastic activity Susan L. Morris-Natschke, Fatma Gumus, Canio J. Marasco, Karen L. Meyer, Michael Marx, Claude Piantadosi, Matthew D. Layne, and Edward J. Modest pp 2018 - 2025; DOI: 10.1021/jm00066a011 |
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Synthesis and biological evaluation of antiplatelet 2-aminochromones Joel Morris, Donn G. Wishka, Alice H. Lin, William R. Humphrey, Ann L. Wiltse, Ronald B. Gammill, Thomas M. Judge, Sharon N. Bisaha, Nancy L. Olds, and et al. pp 2026 - 2032; DOI: 10.1021/jm00066a012 |
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Synthesis and antiherpes virus activity of 1,5-anhydrohexitol nucleosides Ilse Verheggen, Arthur Van Aerschot, Suzanne Toppet, Robert Snoeck, Gerard Janssen, Jan Balzarini, Erik De Clercq, and Piet Herdewijn pp 2033 - 2040; DOI: 10.1021/jm00066a013 |
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Toward a novel metal-based chemotherapy against tropical diseases. 1. Enhancement of the efficacy of clotrimazole against Trypanosoma cruzi by complexation to ruthenium in RuCl2(clotrimazole)2 Roberto A. Sanchez-Delgado, Keyla Lazardi, Luis Rincon, Julio A. Urbina, Andre J. Hubert, and Alfred N. Noels pp 2041 - 2043; DOI: 10.1021/jm00066a014 |
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N-Acyl-L-tryptophan benzyl esters: potent substance P receptor antagonists Angus M. MacLeod, Kevin J. Merchant, Margaret A. Cascieri, Sharon Sadowski, Elzbieta Ber, Christopher J. Swain, and Raymond Baker pp 2044 - 2045; DOI: 10.1021/jm00066a015 |
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(3SR,4aRS,6RS,8aRS)-6-[2-(1H-Tetrazol-5-yl)ethyl]decahydroisoquinoline-3-carboxylic acid: a structurally novel, systemically active, competitive AMPA receptor antagonist Paul L. Ornstein, M. Brian Arnold, Nancy K. Augenstein, David Lodge, J. David Leander, and Darryle D. Schoepp pp 2046 - 2048; DOI: 10.1021/jm00066a016 |
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Design and conformational analysis of several highly potent bradykinin receptor antagonists. [Erratum to document cited in CA114(15):144010y] Donald J. Kyle, Jennifer A. Martin, Stephen G. Farmer, and Ronald M. Burch pp 2050 - 2050; DOI: 10.1021/jm00066a017 |
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Book Reviews pp 2049 - 2049; DOI: 10.1021/jm00066a600 |
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Excursions in drug discovery Arthur A. Patchett pp 2051 - 2058; DOI: 10.1021/jm00067a001 |
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(S)- and (R)-8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1-carbaldehyde: a new class of orally active 5-HT1A-receptor agonists Peter Stjernloef, Maria Gullme, Thomas Elebring, Bengt Andersson, Haakan Wikstroem, Soeren Lagerquist, Kjell Svensson, Agneta Ekman, Arvid Carlsson, and Staffan Sundell pp 2059 - 2065; DOI: 10.1021/jm00067a002 |
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Novel 2-substituted tetrahydro-3H-benz[e]indolamines: highly potent and selective agonists acting at the 5-HT1A receptor as possible anxiolytics and antidepressants Arthur G. Romero, Jeffrey A. Leiby, Robert B. McCall, Montford F. Piercey, Martin W. Smith, and Fusen Han pp 2066 - 2074; DOI: 10.1021/jm00067a003 |
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A potent new class of .kappa.-receptor agonist: 4-substituted 1-(arylacetyl)-2-[(dialkylamino)methyl]piperazines Alan Naylor, Duncan B. Judd, Jane E. Lloyd, David I. C. Scopes, Ann G. Hayes, and Philip J. Birch pp 2075 - 2083; DOI: 10.1021/jm00067a004 |
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Synthesis and antitumor properties of an anthraquinone bisubstituted by the copper chelating peptide Gly-Gly-L-His Elisabeth Morier-Teissier, Nezha Boitte, Nicole Helbecque, Jean Luc Bernier, Nicole Pommery, Jean Loup Duvalet, Charles Fournier, Bernard Hecquet, Jean Pierre Catteau, and Jean Pierre Henichart pp 2084 - 2090; DOI: 10.1021/jm00067a005 |
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Reductive activation of potential antitumor mitosene compounds Marc Maliepaard, Nico J. de Mol, Lambert H. M. Janssen, Joop C. Hoogvliet, Wouter van der Neut, Willem Verboom, and David N. Reinhoudt pp 2091 - 2097; DOI: 10.1021/jm00067a006 |
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N-Phosphoryl derivatives of bisantrene. Antitumor prodrugs with enhanced solubility and reduced potential for toxicity K. C. Murdock, Ving J. Lee, Ronald V. Citarella, Frederick E. Durr, Gabriela Nicolau, and Michael Kohlbrenner pp 2098 - 2101; DOI: 10.1021/jm00067a007 |
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Syntheses of 5'-substituted analogs of carbocyclic 3-deazaadenosine as potential antivirals John A. Secrist, Robert N. Comber, Rita J. Gray, Robin B. Gilroy, and John A. Montgomery pp 2102 - 2106; DOI: 10.1021/jm00067a008 |
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New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study Jean Francois F. Liegeois, Jacques Bruhwyler, Jacques Damas, Thuy Phuong Nguyen, Eric M. G. Chleide, Michel G. A. Mercier, Francoise A. Rogister, and Jacques E. Delarge pp 2107 - 2114; DOI: 10.1021/jm00067a009 |
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Synthesis and structure-activity relationships of phenyl-substituted benzylamine antimycotics: a novel benzylbenzylamine antifungal agent for systemic treatment Peter Nussbaumer, Gerhard Dorfstaetter, Maximilian A. Grassberger, Ingrid Leitner, Josef G. Meingassner, Klaus Thirring, and Anton Stuetz pp 2115 - 2120; DOI: 10.1021/jm00067a010 |
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2,2-Dialkylnaphthalen-1-ones as new potassium channel activators Carmen Almansa, Luis A. Gomez, Fernando L. Cavalcanti, Ricardo Rodriguez, Elena Carceller, Javier Bartroli, Julian Garcia-Rafanell, and Javier Forn pp 2121 - 2133; DOI: 10.1021/jm00067a011 |
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Sulfonylmethanesulfonamide inhibitors of carbonic anhydrase Thomas H. Scholz, John M. Sondey, William C. Randall, Harvey Schwam, Wayne J. Thompson, Pierre J. Mallorga, Michael F. Sugrue, and Samuel L. Graham pp 2134 - 2141; DOI: 10.1021/jm00067a012 |
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Multiple copy simultaneous search and construction of ligands in binding sites: application to inhibitors of HIV-1 aspartic proteinase Amedeo Caflisch, Andrew Miranker, and Martin Karplus pp 2142 - 2167; DOI: 10.1021/jm00067a013 |
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4-Amidinoindan-1-one 2'-amidinohydrazone: a new potent and selective inhibitor of S-adenosylmethionine decarboxylase Jaroslav Stanek, Giorgio Caravatti, Jorg Frei, Pascal Furet, Helmut Mett, Peter Schneider, and Urs Regenass pp 2168 - 2171; DOI: 10.1021/jm00067a014 |
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Synthesis and structure-activity relationships of nonpeptide, potent triazolone-based angiotensin II receptor antagonists Horng Chih Huang, David B. Reitz, Timothy S. Chamberlain, Gillian M. Olins, Valerie M. Corpus, Ellen G. McMahon, Maria A. Palomo, John P. Koepke, Glenn J. Smits, and et al. pp 2172 - 2181; DOI: 10.1021/jm00067a015 |
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Nonpeptide angiotensin II receptor antagonists. Synthesis and biological activity of benzimidazolecarboxylic acids Keiji Kubo, Yasuhisa Kohara, Eiko Imamiya, Yoshihiro Sugiura, Yoshiyuki Inada, Yoshiyasu Furukawa, Kohei Nishikawa, and Takehiko Naka pp 2182 - 2195; DOI: 10.1021/jm00067a016 |
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Studies on quinazolines. 5. 2,3-Dihydroimidazo[1,2-c]quinazoline derivatives: a novel class of potent and selective .alpha.1-adrenoceptor antagonists and antihypertensive agents Ji Wang Chern, Pao Luh Tao, Mao Hsiung Yen, Guan Yu Lu, Chia Yang Shiau, Yue Jun Lai, Su Lan Chien, and Chao Han Chan pp 2196 - 2207; DOI: 10.1021/jm00067a017 |
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Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro-3-propyl-1H-benz[e]indole-9-carboxamide: A potent and selective 5-HT1A receptor agonist with good oral availability Chiu Hong Lin, Susanne R. Haadsma-Svensson, Gillian Phillips, Robert B. McCall, Montford F. Piercey, Martin W. Smith, Kjell Svensson, Arvid Carlsson, Connie G. Chidester, and Phillip F. Von Voigtlander pp 2208 - 2218; DOI: 10.1021/jm00067a018 |
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Biologically active conformers of phenothiazines and thioxanthenes. Further evidence for a ligand model of dopamine D2 receptor antagonists Mark Froimowitz and Vivian Cody pp 2219 - 2227; DOI: 10.1021/jm00067a019 |
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Synthesis and antitumor activity of 10-propargyl-10-deazaaminopterin Joseph I. DeGraw, William T. Colwell, James R. Piper, and Francis M. Sirotnak pp 2228 - 2231; DOI: 10.1021/jm00067a020 |
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1-Carboranyl-3-(2-methylaziridino)-2-propanol. Synthesis, selective uptake by B-16 melanoma, and selective cytotoxicity toward cancer cells Yoshinori Yamamoto and Hiroyuki Nakamura pp 2232 - 2234; DOI: 10.1021/jm00067a021 |
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Selective inhibition of mammalian lanosterol 14.alpha.-demethylase: a possible strategy for cholesterol lowering Keith A. M. Walker, Denis J. Kertesz, David M. Rotstein, David C. Swinney, Pamela W. Berry, On Yee So, Austin S. Webb, David M. Watson, Amy Y. Mak, and et al. pp 2235 - 2237; DOI: 10.1021/jm00067a022 |
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Hydroxyurea derivatives as hypoglycemic agents Steven W. Goldstein, Ruth E. McDermott, E. Michael Gibbs, and Ralph W. Stevenson pp 2238 - 2240; DOI: 10.1021/jm00067a023 |
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New indole derivatives as potent and selective serotonin uptake inhibitors. [Erratum to document cited in CA119(2):8726n] Jean Luc Malleron, Claude Gueremy, Serge Mignani, Jean Francois Peyronel, Alain Truchon, Jean Charles Blanchard, Adam Doble, Pierre Laduron, Odile Piot, and et al. pp 2242 - 2242; DOI: 10.1021/jm00067a024 |
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Phenyl-substituted prostaglandins: potent and selective antiglaucoma agents. [Erratum to document cited in CA118(11):101683k] Bahram Resul, Johan Stjernschantz, Kiyo No, Charlotta Liljebris, Goeran Selen, Maria Astin, Maritha Karlsson, and Laszlo Z. Bito pp 2242 - 2242; DOI: 10.1021/jm00067a025 |
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Book Reviews pp 2241 - 2241; DOI: 10.1021/jm00067a600 |
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Anticonvulsant activities of some arylsemicarbazones displaying potent oral activity in the maximal electroshock screen in rats accompanied by high protection indices J. R. Dimmock, K. K. Sidhu, R. S. Thayer, P. Mack, M. J. Duffy, R. S. Reid, J. W. Quail, U. Pugazhenthi, A. Ong, and et al. pp 2243 - 2252; DOI: 10.1021/jm00068a001 |
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Nonpeptide angiotensin II receptor antagonists. 2. Design, synthesis, and structure-activity relationships of 2-alkyl-4-(1H-pyrrol-l-yl)-1H-imidazole derivatives: profile of 2-propyl-1-[[2'-(1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl]-methyl]-4-[2-(trifluoroacetyl)-1H-pyrrol-1-yl]-1H-imidazole-5-carboxylic acid (CI-996) Ila Sircar, John C. Hodges, John Quin, III, Amy M. Bunker, R. Thomas Winters, Jeremy J. Edmunds, Catherine R. Kostlan, Cleo Connolly, Stephen J. Kesten, and et al. pp 2253 - 2265; DOI: 10.1021/jm00068a002 |
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Studies on neurokinin antagonists. 3. Design and structure-activity relationships of new branched tripeptides N.alpha.-(substituted L-aspartyl, L-ornithyl, or L-lysyl)-N-methyl-N-(phenylmethyl)-L-phenylalaninamides as substance P antagonists Daijiro Hagiwara, Hiroshi Miyake, Kenji Murano, Hiroshi Morimoto, Masako Murai, Takashi Fujii, Isao Nakanishi, and Masaaki Matsuo pp 2266 - 2278; DOI: 10.1021/jm00068a003 |
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Benzoquinazoline inhibitors of thymidylate synthase: enzyme inhibitory activity and cytotoxicity of some 3-amino- and 3-methylbenzo[f]quinazolin-1(2H)-ones William Pendergast, Jay V. Johnson, Scott H. Dickerson, Inderjit K. Dev, David S. Duch, Robert Ferone, William R. Hall, Joan Humphreys, Joseph M. Kelly, and David C. Wilson pp 2279 - 2291; DOI: 10.1021/jm00068a004 |
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Synthesis and structure-activity studies of a series of spirooxazolidine-2,4-diones: 4-oxa-analogs of the muscarinic agonist 2-ethyl-8-methyl-2,8-diazaspiro[4.5]decane-1,3-dione Shinichi Tsukamoto, Masato Ichihara, Fumikazu Wanibuchi, Shinji Usuda, Kazuyuki Hidaka, Masatomi Harada, and Toshinari Tamura pp 2292 - 2299; DOI: 10.1021/jm00068a005 |
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Potent HIV protease inhibitors: the development of tetrahydrofuranylglycines as novel P2-ligands and pyrazine amides as P3-ligands Arun K. Ghosh, Wayne J. Thompson, M. Katharine Holloway, Sean P. McKee, Tien T. Duong, Hee Yoon Lee, Peter M. Munson, Anthony M. Smith, Jenny M. Wai, and et al. pp 2300 - 2310; DOI: 10.1021/jm00068a006 |
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Synthesis and evaluation of conformationally restricted N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(1-pyrrolidinyl)ethylamines at .sigma. receptors. 2. Piperazines, bicyclic amines, bridged bicyclic amines, and miscellaneous compounds Brian R. de Costa, Xiaoshu He, Joannes T. M. Linders, Celia Dominguez, Zi Qiang Gu, Wanda Williams, and Wayne Bowen pp 2311 - 2320; DOI: 10.1021/jm00068a007 |
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A novel constrained reduced-amide inhibitor of HIV-1 protease derived from the sequential incorporation of .gamma.-turn mimetics into a model substrate Kenneth A. Newlander, James F. Callahan, Michael L. Moore, Thaddeus A. Tomaszek, and William F. Huffman pp 2321 - 2331; DOI: 10.1021/jm00068a008 |
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Synthesis and anaerobic activity of novel 1-carba-1-dethiacephalosporins Robert J. Ternansky, Christopher L. Jordan, Judy A. Eudaly, and Jeffrey S. Kasher pp 2332 - 2334; DOI: 10.1021/jm00068a009 |
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Quinoxaline N-oxide containing potent angiotensin II receptor antagonists: synthesis, biological properties, and structure-activity relationships Kyoung Soon Kim, Ligang Qian, J. Eileen Bird, Kenneth E. J. Dickinson, Suzanne Moreland, Thomas R. Schaeffer, Thomas L. Waldron, Carol L. Delaney, Harold N. Weller, and Arthur V. Miller pp 2335 - 2342; DOI: 10.1021/jm00068a010 |
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Nonpeptide angiotensin II receptor antagonists. Synthesis and biological activity of potential prodrugs of benzimidazole-7-carboxylic acids Keiji Kubo, Yasuhisa Kohara, Yoshinobu Yoshimura, Yoshiyuki Inada, Yumiko Shibouta, Yoshiyasu Furukawa, Takeshi Kato, Kohei Nishikawa, and Takehiko Naka pp 2343 - 2349; DOI: 10.1021/jm00068a011 |
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Characterization of the interaction between human .alpha.-thrombin and methyl 3-(2-methyl-1-oxopropoxy) [1]benzothieno[3,2-b]furan-2-carboxylate (LY806303) using electrospray mass spectrometry and tandem mass spectrometry Daniel J. Sall and Raymond E. Kaiser pp 2350 - 2355; DOI: 10.1021/jm00068a012 |
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Bicyclic thiazolidine lactam peptidomimetics of the dopamine receptor modulating peptide Pro-Leu-Gly-NH2 Nalin L. Subasinghe, Roger J. Bontems, Edward McIntee, Ram K. Mishra, and Rodney L. Johnson pp 2356 - 2361; DOI: 10.1021/jm00068a013 |
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Analogs of capsaicin with agonist activity as novel analgesic agents; structure-activity studies. 1. The aromatic "A-region" Christopher S. J. Walpole, Roger Wrigglesworth, Stuart Bevan, Elizabeth A. Campbell, Andy Dray, Iain F. James, Martin N. Perkins, Derek J. Reid, and Janet Winter pp 2362 - 2372; DOI: 10.1021/jm00068a014 |
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Analogs of capsaicin with agonist activity as novel analgesic agents; structure-activity studies. 2. The amide bond "B-region" Christopher S. J. Walpole, Roger Wrigglesworth, Stuart Bevan, Elizabeth A. Campbell, Andy Dray, Iain F. James, Kay J. Masdin, Martin N. Perkins, and Janet Winter pp 2373 - 2380; DOI: 10.1021/jm00068a015 |
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Analogs of capsaicin with agonist activity as novel analgesic agents; structure-activity studies. 3. The hydrophobic side-chain "C-region" Christopher S. J. Walpole, Roger Wrigglesworth, Stuart Bevan, Elizabeth A. Campbell, Andy Dray, Iain F. James, Kay J. Masdin, Martin N. Perkins, and Janet Winter pp 2381 - 2389; DOI: 10.1021/jm00068a016 |
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3D-QSAR(Three-Dimensional Quantitative Structure)-Activity Relationship Of Angiotensin-Converting Enzyme And Thermolysin Inhibitors. II. A Comparison Of CoMFA Models Incorporating Molecular Orbital Fields And Desolvation Free Energies Based On Active-Analog And Complementary-Receptor-Field Alignment Rules Chris L. Waller and Garland R. Marshall pp 2390 - 2403; DOI: 10.1021/jm00068a017 |
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Synthesis of new 11.beta.-substituted spirolactone derivatives. Relationship with affinity for mineralocorticoid and glucocorticoid receptors Michel Claire, Hassane Faraj, Gerard Grassy, Andre Aumelas, Anne Rondot, and Gilles Auzou pp 2404 - 2407; DOI: 10.1021/jm00068a018 |
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A mechanism-based inactivation study of neutral endopeptidase 24.11 Odile E. Levy, Pascale Taibi, Shahriar Mobashery, and Soumitra S. Ghosh pp 2408 - 2411; DOI: 10.1021/jm00068a019 |
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Synthesis and .kappa.-opioid antagonist selectivity of a norbinaltorphimine congener. Identification of the address moiety required for .kappa.-antagonist activity Chia En Lin, Akira E. Takemori, and Philip S. Portoghese pp 2412 - 2415; DOI: 10.1021/jm00068a020 |
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2,5-Dimethoxy congeners of (+)- and (-)-3-(3-hydroxyphenyl)-N-n-propylpiperidine Joseph G. Cannon, Karen S. Kirschbaum, Victor E. D. Amoo, Alan K. Johnson, and John Paul Long pp 2416 - 2419; DOI: 10.1021/jm00068a021 |
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Application of a conformationally restricted Phe-Leu dipeptide mimetic to the design of a combined inhibitor of angiotensin I-converting enzyme and neutral endopeptidase 24.11 Gary A. Flynn, Douglas W. Beight, Shujaath Mehdi, Jack R. Koehl, Eugene L. Giroux, John F. French, Paul W. Hake, and Richard C. Dage pp 2420 - 2423; DOI: 10.1021/jm00068a022 |
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Application of the hypersurface iterative projection method to bicyclic pyrazolidinone antibacterial agents. [Erratum to document cited in CA118(23):224933z] Donald B. Boyd pp 2430 - 2430; DOI: 10.1021/jm00068a023 |
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Book Reviews pp 2424 - 2429; DOI: 10.1021/jm00068a600 |
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Activated ketone based inhibitors of human renin Dinesh V. Patel, Katherine Rielly-Gauvin, Denis E. Ryono, Charles A. Free, Sandra A. Smith, and Edward W. Petrillo pp 2431 - 2447; DOI: 10.1021/jm00069a001 |
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Synthesis, physicochemical properties, and biological evaluation of N-substituted 2-alkyl-3-hydroxy-4(1H)-pyridinones: orally active iron chelators with clinical potential Paul S. Dobbin, Robert C. Hider, Adrian D. Hall, Paul D. Taylor, Patience Sarpong, John B. Porter, Gaoyi Xiao, and Dick van der Helm pp 2448 - 2458; DOI: 10.1021/jm00069a002 |
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Tyrosine kinase inhibitors. 1. Structure-activity relationships for inhibition of epidermal growth factor receptor tyrosine kinase activity by 2,3-dihydro-2-thioxo-1H-indole-3-alkanoic acids and 2,2'-dithiobis(1H-indole-3-alkanoic acids) Andrew M. Thompson, Gordon W. Rewcastle, Moana Tercel, Ellen M. Dobrusin, David W. Fry, Alan J. Kraker, and William A. Denny pp 2459 - 2469; DOI: 10.1021/jm00069a003 |
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Synthesis and antiviral activity of novel 5-(1-azido-2-haloethyl) and 5-(1-azido-, amino-, or methoxyethyl) analogs of 2'-deoxyuridine Rakesh Kumar, Leonard I. Wiebe, and Edward E. Knaus pp 2470 - 2474; DOI: 10.1021/jm00069a004 |
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A pharmacological, crystallographic, and quantum chemical study of new inotropic agents P. Dorigo, R. M. Gaion, P. Belluco, D. Fraccarollo, I. Maragno, G. Bombieri, F. Benetollo, L. Mosti, and F. Orsini pp 2475 - 2484; DOI: 10.1021/jm00069a005 |
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Antihyperglycemic activity of novel naphthalenylmethyl-3H-1,2,3,5-oxathiadiazole 2-oxides John W. Ellingboe, Louis J. Lombardo, Thomas R. Alessi, Thomas T. Nguyen, Frieda Guzzo, Charles J. Guinosso, James Bullington, Eric N. C. Browne, Jehan F. Bagli, and et al. pp 2485 - 2493; DOI: 10.1021/jm00069a006 |
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Mono- and bis(aminomethyl)phenylacetic acid esters as short-acting antiarrhythmic agents. 2 Robert J. Chorvat, Lawrence A. Black, Vasant V. Ranade, Cynthia Barcelon-Yang, David M. Stout, Barry S. Brown, Herman F. Stampfli, and Check Y. Quon pp 2494 - 2498; DOI: 10.1021/jm00069a007 |
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Synthesis and binding properties of MK-801 isothiocyanates; (+)-3-isothiocyanato-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine hydrochloride: a new, potent and selective electrophilic affinity ligand for the NMDA receptor-coupled phencyclidine binding site Joannes T. M. Linders, James A. Monn, Mariena V. Mattson, Clifford George, Arthur E. Jacobson, and Kenner C. Rice pp 2499 - 2507; DOI: 10.1021/jm00069a008 |
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Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-[(R)-phenylisopropyl]adenosine-induced cognitive disturbance Fumio Suzuki, Junichi Shimada, Shizuo Shiozaki, Shunji Ichikawa, Akio Ishii, Joji Nakamura, Hiromi Nonaka, Hiroyuki Kobayashi, and Eiichi Fuse pp 2508 - 2518; DOI: 10.1021/jm00069a009 |
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Antagonism of 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane stimulus with a newly identified 5-HT2- versus 5-HT1C-selective antagonist Abd M. Ismaiel, Joseph De Los Angeles, Milt Teitler, Stacy Ingher, and Richard A. Glennon pp 2519 - 2525; DOI: 10.1021/jm00069a010 |
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Selective non-nucleoside HIV-1 reverse transcriptase inhibitors. New 2,3-dihydrothiazolo[2,3-a]isoindol-5(9bH)-ones and related compounds with anti-HIV-1 activity Alfred Mertens, Harald Zilch, Bernhard Koenig, Wolfgang Schaefer, Thomas Poll, Wolfgang Kampe, Hans Seidel, Ulrike Leser, and Herbert Leinert pp 2526 - 2535; DOI: 10.1021/jm00069a011 |
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Synthesis and biological activity of C-terminally truncated fragments of human-.alpha.-calcitonin gene-related peptide D. David Smith, Jianzhong Li, Qiming Wang, Richard F. Murphy, Thomas E. Adrian, Yvonne Elias, Charles S. Bockman, and Peter W. Abel pp 2536 - 2541; DOI: 10.1021/jm00069a012 |
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Synthesis and pharmacological evaluation of 1-phenyl-3-amino-1,2,3,4-tetrahydronaphthalenes as ligands for a novel receptor with .sigma.-like neuromodulatory activity Steven D. Wyrick, Raymond G. Booth, Andrew M. Myers, Constance E. Owens, Nora S. Kula, Ross J. Baldessarini, Andrew T. McPhail, and Richard B. Mailman pp 2542 - 2551; DOI: 10.1021/jm00069a013 |
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Synthesis and antimalarial activity of some 9-substituted artemisinin derivatives Nancy Acton, Jean M. Karle, and Robert E. Miller pp 2552 - 2557; DOI: 10.1021/jm00069a014 |
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Triazolinones as nonpeptide angiotensin II antagonists. 1. Synthesis and evaluation of potent 2,4,5-trisubstituted triazolinones Linda L. Chang, Wallace T. Ashton, Kelly L. Flanagan, Robert A. Strelitz, Malcolm MacCoss, William J. Greenlee, Raymond S. L. Chang, Victor J. Lotti, Kristie A. Faust, and et al. pp 2558 - 2568; DOI: 10.1021/jm00069a015 |
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Design of potent, cyclic peptide bradykinin receptor antagonists from conformationally constrained linear peptides Sarvajit Chakravarty, Deidre Wilkins, and Donald J. Kyle pp 2569 - 2571; DOI: 10.1021/jm00069a016 |
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A selective .delta.1 opioid receptor agonist derived from oxymorphone. Evidence for separate recognition sites for .delta.1 opioid receptor agonists and antagonists P. S. Portoghese, S. T. Moe, and A. E. Takemori pp 2572 - 2574; DOI: 10.1021/jm00069a017 |
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Peptidomimetic HIV protease inhibitors: phosphate prodrugs with improved biological activities Kong Teck Chong, Mary J. Ruwart, Roger R. Hinshaw, Karen F. Wilkinson, Bob D. Rush, Mark F. Yancey, Joseph W. Strohbach, and Suvit Thaisrivongs pp 2575 - 2577; DOI: 10.1021/jm00069a018 |
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Nitrobenzyl mustard quaternary salts: a new class of hypoxia-selective cytotoxins showing very high in vitro selectivity Moana Tercel, William R. Wilson, and William A. Denny pp 2578 - 2579; DOI: 10.1021/jm00069a019 |
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Ethyl substitution at the 7 position extends the half-life of 10-hydroxycamptothecin in the presence of human serum albumin Thomas G. Burke and Zihou Mi pp 2580 - 2582; DOI: 10.1021/jm00069a020 |
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Design of potent non-peptide competitive antagonists of the human bradykinin B2 receptor Joseph M. Salvino, Peter R. Seoane, Brent D. Douty, Mohamad M. A. Awad, Roland E. Dolle, Wayne T. Houck, David M. Faunce, and David G. Sawutz pp 2583 - 2584; DOI: 10.1021/jm00069a021 |
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Structure-activity relationships of C-terminal endothelin hexapeptide antagonists A. M. Doherty, W. L. Cody, P. L. DePue, J. X. He, L. A. Waite, D. M. Leonard, N. L. Leitz, D. T. Dudley, S. T. Rapundalo, and et al. pp 2585 - 2594; DOI: 10.1021/jm00070a001 |
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Vanilloids. 1. Analogs of capsaicin with antinociceptive and antiinflammatory activity John M. Janusz, Brian L. Buckwalter, Patricia A. Young, Thomas R. LaHann, Ralph W. Farmer, Gerald B. Kasting, Maurice E. Loomans, Gary A. Kerckaert, Cherie S. Maddin, and et al. pp 2595 - 2604; DOI: 10.1021/jm00070a002 |
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Conformational effects on retinoid receptor selectivity. 1. Effect of 9-double bond geometry on retinoid X receptor activity Ling Jong, Jurgen M. Lehmann, Peter D. Hobbs, Eli Harlev, John C. Huffman, Magnus Pfahl, and Marcia I. Dawson pp 2605 - 2613; DOI: 10.1021/jm00070a003 |
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Specificity in the binding of inhibitors to the active site of human/primate aspartic proteinases: analysis of P2-P1-P1'-P2' variation Chetana M. Rao, Paula E. Scarborough, John Kay, Brian Batley, Stephen Rapundalo, Sylvester Klutchko, Michael D. Taylor, Elizabeth A. Lunney, Christine C. Humblet, and Ben M. Dunn pp 2614 - 2620; DOI: 10.1021/jm00070a004 |
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Synthesis and antibacterial activity of a new series of tetracyclic pyridone carboxylic acids Yoshikazu Jinbo, Hirosato Kondo, Yoshimasa Inoue, Masahiro Taguchi, Hideki Tsujishita, Yasuo Kotera, Fumio Sakamoto, and Goro Tsukamoto pp 2621 - 2626; DOI: 10.1021/jm00070a005 |
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Structure-activity relationships of .beta.-D-(2S,5R)- and .alpha.-D-(2S,5S)-1,3-oxathiolanyl nucleosides as potential anti-HIV agents Lak S. Jeong, Raymond F. Schinazi, J. Warren Beach, Hea O. Kim, Kirupathevy Shanmuganathan, Satyanarayana Nampalli, Moon W. Chun, Won Keun Chung, Bo G. Choi, and Chung K. Chu pp 2627 - 2638; DOI: 10.1021/jm00070a006 |
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Effect of trifluoromethyl and other substituents on activity of xanthines at adenosine receptors Kenneth A. Jacobson, Dan Shi, Carola Gallo-Rodriguez, Malcolm Manning, Christa Muller, John W. Daly, John L. Neumeyer, Leonidas Kiriasis, and Wolfgang Pfleiderer pp 2639 - 2644; DOI: 10.1021/jm00070a007 |
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2-(Quinuclidin-3-yl)pyrido[4,3-b]indol-1-ones and isoquinolin-1-ones. Potent conformationally restricted 5-HT3 receptor antagonists Robin D. Clark, Aaron B. Miller, Jacob Berger, David B. Repke, Klaus K. Weinhardt, Bruce A. Kowalczyk, Richard M. Eglen, Douglas W. Bonhaus, Chi Ho Lee, and et al. pp 2645 - 2657; DOI: 10.1021/jm00070a008 |
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A conformational study by proton NMR of a cyclic pentapeptide antagonist of endothelin Murray Coles, Victoria Sowemimo, Denis Scanlon, Sharon L. A. Munro, and David J. Craik pp 2658 - 2665; DOI: 10.1021/jm00070a009 |
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Peracid oxidation of an N-hydroxyguanidine compound: a chemical model for the oxidation of N.omega.-hydroxy-L-arginine by nitric oxide synthase Jon M. Fukuto, Dennis J. Stuehr, Paul L. Feldman, Michael P. Bova, and Patrick Wong pp 2666 - 2670; DOI: 10.1021/jm00070a010 |
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Amesergide and structurally related nor-D-ergolines: 5HT2 receptor interactions in the rat Michael J. Martinelli, William Bloomquist, Barry C. Peterson, and Marlene L. Cohen pp 2671 - 2675; DOI: 10.1021/jm00070a011 |
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2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists Martin Winn, Biswanath De, Thomas M. Zydowsky, Robert J. Altenbach, Fatima Z. Basha, Steven A. Boyd, Michael E. Brune, Steven A. Buckner, DeAnne Crowell, and et al. pp 2676 - 2688; DOI: 10.1021/jm00070a012 |
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Plant antitumor agents. 30. Synthesis and structure activity of novel camptothecin analogs Monroe E. Wall, Mansukh C. Wani, Allan W. Nicholas, Govindarajan Manikumar, Chhagan Tele, Linda Moore, Anne Truesdale, Peter Leitner, and Jeffrey M. Besterman pp 2689 - 2700; DOI: 10.1021/jm00070a013 |
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Keto/enol epoxy steroids: a new structural class of HIV-1 tat inhibitors William F. Michne, Joseph D. Schroeder, Thomas R. Bailey, Dorothy C. Young, Joseph V. Hughes, and Frank J. Dutko pp 2701 - 2702; DOI: 10.1021/jm00070a014 |
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(E)-3-[[[[6-(2-Carboxyethenyl)-5-[[8-(4-methoxyphenyl)octyl]oxy]-2-pyridinyl]methyl]thio]methyl]benzoic acid: a novel high-affinity leukotriene B4 receptor antagonist Robert A. Daines, Pamela A. Chambers, Israil Pendrak, Dalia R. Jakas, Henry M. Sarau, James J. Foley, Dulcie B. Schmidt, Don E. Griswold, Lenox D. Martin, and et al. pp 2703 - 2705; DOI: 10.1021/jm00070a015 |
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Synthesis and metabotropic receptor activity of the novel rigidified glutamate analogs (+)- and (-)-trans-azetidine-2,4-dicarboxylic acid and their N-methyl derivatives A. P. Kozikowski, W. Tuckmantel, Y. Liao, H. Manev, S. Ikonomovic, and J. T. Wroblewski pp 2706 - 2708; DOI: 10.1021/jm00070a016 |
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Book Reviews pp 2709 - 2710; DOI: 10.1021/jm00070a600 |
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Synthesis of antimicrobial agents. 5. In vivo metabolism of 7-(4-hydroxypiperazin-1-yl)quinolones Toshio Uno, Toshimi Okuno, Kiyotaka Kawakami, Fumio Sakamoto, and Goro Tsukamoto pp 2711 - 2715; DOI: 10.1021/jm00071a001 |
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Preparation of substituted N-phenyl-4-aryl-2-pyrimidinamines as mediator release inhibitors Rolf Paul, William A. Hallett, John W. Hanifin, Marvin F. Reich, Bernard D. Johnson, Robert H. Lenhard, John P. Dusza, Suresh S. Kerwar, Yang I Lin, and et al. pp 2716 - 2725; DOI: 10.1021/jm00071a002 |
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Synthesis and antiviral activity of 2'-substituted 9-[2-(phosphonomethoxy)ethyl]guanine analogs Kuo Long Yu, Joanne J. Bronson, Hyekyung Yang, Amy Patick, Masud Alam, Vera Brankovan, Roelf Datema, Michael J. M. Hitchcock, and John C. Martin pp 2726 - 2738; DOI: 10.1021/jm00071a003 |
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Discovery and synthesis of methyl 2,5-dimethyl-4-[2-(phenylmethyl)benzoyl]-1H-pyrrole-3-carboxylate (FPL 64176) and analogs: the first examples of a new class of calcium channel activator Andrew J. G. Baxter, John Dixon, Francis Ince, Carol N. Manners, and Simon J. Teague pp 2739 - 2744; DOI: 10.1021/jm00071a004 |
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Novel antagonists of 5-HT3 receptors. Synthesis and biological evaluation of piperazinylquinoxaline derivatives A. Monge, J. A. Palop, J. C. Del Castillo, J. M. Caldero, J. Roca, G. Romero, J. Del Rio, and B. Lasheras pp 2745 - 2750; DOI: 10.1021/jm00071a005 |
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Structure-affinity relationship studies on 5-HT1A receptor ligands. 1. Heterobicyclic phenylpiperazines with N4-alkyl substituents Bart J. van Steen, Ineke van Wijngaarden, Martin T. M. Tulp, and Willem Soudijn pp 2751 - 2760; DOI: 10.1021/jm00071a006 |
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Stereospecific and selective 5-HT2 antagonism in a series of 5-substituted trans-1-piperazino-3-phenylindans Klaus P. Boegesoe, Joern Arnt, John Hyttel, and Henrik Pedersen pp 2761 - 2770; DOI: 10.1021/jm00071a007 |
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Substituted thiopyrano[2,3,4-c,d]indoles as potent, selective, and orally active inhibitors of 5-lipoxygenase. Synthesis and biological evaluation of L-691,816 J. H. Hutchinson, D. Riendeau, C. Brideau, C. Chan, D. Delorme, D. Denis, J. P. Falgueyret, R. Fortin, J. Guay, and et al. pp 2771 - 2787; DOI: 10.1021/jm00071a008 |
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Renin inhibitors containing a pyridyl amino diol derived C-terminus Holger Heitsch, Rainer Henning, Heinz Werner Kleemann, Wolfgang Linz, Wolf Ulrich Nickel, Dieter Ruppert, Hansjoerg Urbach, and Adalbert Wagner pp 2788 - 2800; DOI: 10.1021/jm00071a009 |
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Mammalian topoisomerase II inhibitory activity of 1-cyclopropyl-6,8-difluoro-1,4-dihydro-7-(2,6-dimethyl-4-pyridinyl)-4-oxo-3-quinolinecarboxylic acid and related derivatives Mark P. Wentland, George Y. Lesher, Michael Reuman, Monte D. Gruett, Baldev Singh, Suzanne C. Aldous, Peter H. Dorff, James B. Rake, and Susan A. Coughlin pp 2801 - 2809; DOI: 10.1021/jm00071a010 |
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Synthesis and structure-activity relationships of naphthalene-substituted derivatives of the allylamine antimycotic terbinafine Peter Nussbaumer, Gerhard Dorfstaetter, Ingrid Leitner, Karin Mraz, Hermann Vyplel, and Anton Stuetz pp 2810 - 2816; DOI: 10.1021/jm00071a011 |
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Synthesis and evaluation of a series of benzylaniline hydrochlorides as potential cytotoxic and antimitotic agents acting by inhibition of tubulin polymerization Mark Cushman, Hu Ming He, Chii M. Lin, and Ernest Hamel pp 2817 - 2821; DOI: 10.1021/jm00071a012 |
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Iron(III)-chelating resins. 3. Synthesis, iron(III)-chelating properties, and in vitro antibacterial activity of compounds containing 3-hydroxy-2-methyl-4(1H)-pyridinone ligands Min Hua Feng, Leen van der Does, and Adriaan Bantjes pp 2822 - 2827; DOI: 10.1021/jm00071a013 |
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Inhibition of bone resorption by H+/K+-ATPase inhibitors Reinhard Sarges, Andrea Gallagher, Timothy J. Chambers, and Li-An Yeh pp 2828 - 2830; DOI: 10.1021/jm00071a014 |
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Book Reviews pp 2831 - 2831; DOI: 10.1021/jm00071a600 |
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Additions and Corrections - Long-Chain-Substituted Uric Acid and 5,6-Diaminouracil Derivatives as Novel Agents against Free Radical Processes: Synthesis and in Vitro Activity. Laurent Fraisse, Jean-Baptiste Verlhac, Béatrice Roche, Marie Claude Rascle, Alain Rabion, and Jean Louis Seris pp 2832 - 2832; DOI: 10.1021/jm00071a601 |
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Additions and Corrections - Modeling the Anticancer Action of Some Retinoid Compounds by Making Use of the Oasis Method. D. Bonchev, C. F. Mountain, W. A. Seitz, and A. T. Balaban pp 2832 - 2832; DOI: 10.1021/jm00071a602 |
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Structure-activity relationships of trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine antagonists for .mu.- and .kappa.-opioid receptors Dennis M. Zimmerman, J. David Leander, Buddy E. Cantrell, Jon K. Reel, John Snoddy, Laurane G. Mendelsohn, Bryan G. Johnson, and Charles H. Mitch pp 2833 - 2841; DOI: 10.1021/jm00072a001 |
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3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity Charles H. Mitch, J. David Leander, Laurane G. Mendelsohn, Walter N. Shaw, David T. Wong, Buddy E. Cantrell, Bryan G. Johnson, John K. Reel, John D. Snoddy, and et al. pp 2842 - 2850; DOI: 10.1021/jm00072a002 |
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Single point D-substituted corticotropin-releasing factor analogs: effects on potency and physicochemical characteristics Jean Rivier, Catherine Rivier, Robert Galyean, Antonio Miranda, Charleen Miller, A. Grey Craig, Gayle Yamamoto, Marvin Brown, and Wylie Vale pp 2851 - 2859; DOI: 10.1021/jm00072a003 |
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Synthesis and relative potencies of new constrained CRF antagonists Jean Francois Hernandez, Wayne Kornreich, Catherine Rivier, Antonio Miranda, Gayle Yamamoto, John Andrews, Yvette Tache, Wylie Vale, and Jean Rivier pp 2860 - 2867; DOI: 10.1021/jm00072a004 |
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Cholecystokinin peptidomimetics as selective CCK-B antagonists: Design, synthesis, and in vitro and in vivo biochemical properties Armand G. S. Blommaert, Jian Hui Weng, Agnes Dorville, Isabelle McCort, Bertrand Ducos, Christine Durieux, and Bernard P. Roques pp 2868 - 2877; DOI: 10.1021/jm00072a005 |
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A structure-activity study of four dopamine D-1 and D-2 receptor antagonists, representing the phenylindan, -indene, and -indole structural classes of compounds Jonas Palm, Klaus P. Boegesoe, and Tommy Liljefors pp 2878 - 2885; DOI: 10.1021/jm00072a006 |
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3-Aryl-2-(3'-substituted-1',2',4'-oxadiazol-5'-yl)tropane analogs of cocaine: affinities at the cocaine binding site at the dopamine, serotonin, and norepinephrine transporters F. Ivy Carroll, Jeffrey L. Gray, Philip Abraham, Michael A. Kuzemko, Anita H. Lewin, John W. Boja, and Michael J. Kuhar pp 2886 - 2890; DOI: 10.1021/jm00072a007 |
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2-Amido-8-methoxytetralins: A series of nonindolic melatonin-like agents Swier Copinga, Pieter G. Tepper, Cor J. Grol, Alan S. Horn, and Margarita L. Dubocovich pp 2891 - 2898; DOI: 10.1021/jm00072a008 |
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3-Substituted 3-(4-pyridinylmethyl)-1,3-dihydro-1-phenyl-2H-indol-2-ones as acetylcholine release enhancers: synthesis and SAR Wendell W. Wilkerson, Ahmed A. Kergaye, and S. William Tam pp 2899 - 2907; DOI: 10.1021/jm00072a009 |
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Chemistry, binding affinities, and behavioral properties of a new class of "antineophobic" mitochondrial DBI receptor complex (mDRC) ligands A. P. Kozikowski, D. Ma, James Brewer, S. Sun, E. Costa, E. Romeo, and A. Guidotti pp 2908 - 2920; DOI: 10.1021/jm00072a010 |
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Confirmation of usefulness of a structure construction program based on three-dimensional receptor structure for rational lead generation Yoshihiko Nishibata and Akiko Itai pp 2921 - 2928; DOI: 10.1021/jm00072a011 |
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QSAR's from similarity matrices. Technique validation and application in the comparison of different similarity evaluation methods Andrew C. Good, Stephen J. Peterson, and W. Graham Richards pp 2929 - 2937; DOI: 10.1021/jm00072a012 |
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Antiviral activity of C-alkylated purine nucleosides obtained by cross-coupling with tetraalkyltin reagents Arthur A. Van Aerschot, Petros Mamos, Nancy J. Weyns, Satoru Ikeda, Erik De Clercq, and Piet A. Herdewijn pp 2938 - 2942; DOI: 10.1021/jm00072a013 |
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Inhibitors of acyl-CoA:cholesterol acyltransferase. 5. Identification and structure-activity relationships of novel .beta.-keto amides as hypocholesterolemic agents Corinne E. Augelli-Szafran, C. John Blankley, Bruce D. Roth, Bharat K. Trivedi, Richard F. Bousley, Arnold D. Essenburg, Katherine L. Hamelehle, Brian R. Krause, and Richard L. Stanfield pp 2943 - 2949; DOI: 10.1021/jm00072a014 |
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Synthesis and protein-tyrosine kinase inhibitory activity of polyhydroxylated stilbene analogs of piceatannol Kshitij Thakkar, Robert L. Geahlen, and Mark Cushman pp 2950 - 2955; DOI: 10.1021/jm00072a015 |
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Novel hypotensive agents from Verbesina caracasana. 2. Synthesis and pharmacology of caracasanamide Giuliano Delle Monache, Bruno Botta, Franco Delle Monache, Romulo Espinal, Stella C. De Bonnevaux, Carlo De Luca, Maurizio Botta, Federico Corelli, and Marco Carmignani pp 2956 - 2963; DOI: 10.1021/jm00072a016 |
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Imidazol-1-yl and pyridin-3-yl derivatives of 4-phenyl-1,4-dihydropyridines combining Ca2+ antagonism and thromboxane A2 synthase inhibition Paolo Cozzi, Germano Carganico, Domenico Fusar, Mauro Grossoni, Maria Menichincheri, Vittorio Pinciroli, Roberto Tonani, Fabrizio Vaghi, and Patricia Salvati pp 2964 - 2972; DOI: 10.1021/jm00072a017 |
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Steroidal affinity labels of the estrogen receptor. 1. 17.alpha.-(Bromoacetoxy)alkyl/alkynylestradiols Driss El Garrouj, Andre Aumelas, and Jean Louis Borgna pp 2973 - 2983; DOI: 10.1021/jm00072a018 |
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Synthesis and structure-activity relationships of 1-acyl-4-((2-methyl-3-pyridyl)cyanomethyl)piperazines as PAF antagonists Elena Carceller, Manuel Merlos, Marta Giral, Carmen Almansa, Javier Bartroli, Julian Garcia-Rafanell, and Javier Forn pp 2984 - 2997; DOI: 10.1021/jm00072a019 |
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Synthesis and evaluation of unsymmetrically substituted polyamine analogs as modulators of human spermidine/spermine-N1-acetyltransferase (SSAT) and as potential antitumor agents Nada H. Saab, Edward E. West, Nella C. Bieszk, Charles V. Preuss, Amy R. Mank, Robert A. Casero, and Patrick M. Woster pp 2998 - 3004; DOI: 10.1021/jm00072a020 |
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Inhibition of herpes simplex virus type 1 ribonucleotide reductase by substituted tetrapeptide derivatives Neil Moss, R. Deziel, J. Adams, N. Aubry, M. Bailey, M. Baillet, P. Beaulieu, J. DiMaio, J. S. Duceppe, and et al. pp 3005 - 3009; DOI: 10.1021/jm00072a021 |
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Non-amine based analogs of lavendustin A as protein-tyrosine kinase inhibitors Mark S. Smyth, Irena Stefanova, Frank Hartmann, Ivan D. Horak, Nir Osherov, Alexander Levitzki, and Terrence R. Burke pp 3010 - 3014; DOI: 10.1021/jm00072a022 |
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Hydroxylated 2-(5'-salicyl)naphthalenes as protein-tyrosine kinase inhibitors Mark S. Smyth, Irena Stefanova, Ivan D. Horak, and Terrence R. Burke pp 3015 - 3020; DOI: 10.1021/jm00072a023 |
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Synthesis and biological evaluation of cholecystokinin analogs in which the Asp-Phe-NH2 moiety has been replaced by a 3-amino-7-phenylheptanoic acid or a 3-amino-6-(phenyloxy)hexanoic acid Muriel Amblard, Marc Rodriguez, Marie Francoise Lignon, Marie Christine Galas, Nicole Bernad, Anne Marie Artis-Noel, Leticia Hauad, Jeanine Laur, Jean Christophe Califano, and et al. pp 3021 - 3028; DOI: 10.1021/jm00072a024 |
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N-(Carboxymethyl)-N-[3,5-bis(decyloxy)phenyl]glycine (Ro 23-9358): a potent inhibitor of secretory phospholipases A2 with antiinflammatory activity Ronald A. LeMahieu, Mathew Carson, Ru Jen Han, Vincent S. Madison, William C. Hope, Ting Chen, Douglas W. Morgan, and H. Stewart Hendrickson pp 3029 - 3031; DOI: 10.1021/jm00072a025 |
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Two new unsaturated fatty acid ethanolamides in brain that bind to the cannabinoid receptor Lumir Hanus, Asher Gopher, Shlomo Almog, and Raphael Mechoulam pp 3032 - 3034; DOI: 10.1021/jm00072a026 |
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Deoxygenated inositol 1,4,5-trisphosphate analogs and their interaction with metabolic enzymes. (1R,2R,4R)-Cyclohexane-1,2,4-tris(methylenesulfonate): a potent selective 5-phosphatase inhibitor Alan P. Kozikowski, Vassil I. Ognyanov, Chinpiao Chen, Abdul H. Fauq, Stephen T. Safrany, Robert A. Wilcox, and Stefan R. Nahorski pp 3035 - 3038; DOI: 10.1021/jm00072a027 |
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Concepts and progress in the development of peptide mimetics Gary L. Olson, David R. Bolin, Mary Pat Bonner, Michael Bos, Charles M. Cook, David C. Fry, Bradford J. Graves, Marcos Hatada, David E. Hill, and et al. pp 3039 - 3049; DOI: 10.1021/jm00073a001 |
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Pyrrolo[1,2-a]benzimidazole-based aziridinyl quinones. A new class of DNA cleaving agent exhibiting G and A base specificity Edward B. Skibo and William G. Schulz pp 3050 - 3055; DOI: 10.1021/jm00073a002 |
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Solution conformation of the antitumor drug streptonigrin Margaret M. Harding, Georgina V. Long, and Christopher L. Brown pp 3056 - 3060; DOI: 10.1021/jm00073a003 |
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Synthesis of A-ring fluorinated derivatives of iodine-125-labeled (17.alpha.,20E/Z)-iodovinylestradiols: effect on receptor binding and receptor-mediated target tissue uptake Hasrat Ali, Jacques Rousseau, and Johan E. van Lier pp 3061 - 3072; DOI: 10.1021/jm00073a004 |
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Examination of the D2/5-HT2 affinity ratios of resolved 5,6,7,8,9,10-hexahydro-7,10-iminocyclohept[b]indoles: an enantioselective approach toward the design of potential atypical antipsychotics Richard E. Mewshaw, Mary E. Abreu, Lisa S. Silverman, Rose M. Mathew, Carol W. Tiffany, Michael A. Bailey, E. William Karbon, John W. Ferkany, and Carl Kaiser pp 3073 - 3076; DOI: 10.1021/jm00073a005 |
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Conformationally restrained analogs of sympathomimetic catecholamines. Synthesis, conformational analysis and adrenergic activity of isochroman derivatives Bruno Macchia, Aldo Balsamo, Maria Cristina Breschi, Grazia Chiellini, Annalina Lapucci, Marco Macchia, Clementina Manera, Adriano Martinelli, Claudia Martini, and et al. pp 3077 - 3086; DOI: 10.1021/jm00073a006 |
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Catalytic functionalization of polymers: a novel approach to site-specific delivery of misoprostol to the stomach Samuel J. Tremont, Paul W. Collins, William E. Perkins, Rick L. Fenton, Denis Forster, Martin P. McGrath, Grace M. Wagner, Alan F. Gasiecki, Robert G. Bianchi, and et al. pp 3087 - 3097; DOI: 10.1021/jm00073a007 |
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Structural modification of 5-aryl-2,3-dihydroimidazo[2,1-a]isoquinoline platelet activating factor receptor antagonists William J. Houlihan, Seung H. Cheon, Vincent A. Parrino, Dean A. Handley, and Douglas A. Larson pp 3098 - 3102; DOI: 10.1021/jm00073a008 |
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2,4-Diaminothieno[2,3-d]pyrimidine analogs of trimetrexate and piritrexim as potential inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase Andre Rosowsky, Clara E. Mota, Joel E. Wright, James H. Freisheim, James J. Heusner, John J. McCormack, and Sherry F. Queener pp 3103 - 3112; DOI: 10.1021/jm00073a009 |
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A series of penicillin-derived C2-symmetric inhibitors of HIV-1 proteinase: structural and modeling studies Alan Wonacott, Robert Cooke, Fiona R. Hayes, Michael M. Hann, Harren Jhoti, Peter McMeekin, Anil Mistry, Peter Murray-Rust, Onkar M. P. Singh, and Malcolm P. Weir pp 3113 - 3119; DOI: 10.1021/jm00073a010 |
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A series of penicillin-derived C2-symmetric inhibitors of HIV-1 proteinase: synthesis, mode of interaction, and structure-activity relationships David C. Humber, Mark J. Bamford, Richard C. Bethell, Nicholas Cammack, Kevin Cobley, Derek N. Evans, Norman M. Gray, Michael M. Hann, David C. Orr, and et al. pp 3120 - 3128; DOI: 10.1021/jm00073a011 |
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Synthesis and structure-activity relationships of a series of penicillin-derived HIV proteinase inhibitors containing a stereochemically unique peptide isostere Duncan S. Holmes, Richard C. Bethell, Nicholas Cammack, Ian R. Clemens, John Kitchin, Peter McMeekin, Chi L. Mo, David C. Orr, Binakumari Patel, and et al. pp 3129 - 3136; DOI: 10.1021/jm00073a012 |
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Azulenic retinoids: novel nonbenzenoid aromatic retinoids with anticancer activity Alfred E. Asato, Ao Peng, Mohammad Z. Hossain, Taraneh Mirzadegan, and John S. Bertram pp 3137 - 3147; DOI: 10.1021/jm00073a013 |
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Synthesis and antibacterial activity of a new series of tetracyclic pyridone carboxylic acids. 2 Yoshikazu Jinbo, Masahiro Taguchi, Yoshimasa Inoue, Hirosato Kondo, Tomohiro Miyasaka, Hideki Tsujishita, Fumio Sakamoto, and Goro Tsukamoto pp 3148 - 3153; DOI: 10.1021/jm00073a014 |
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14.beta.-[(p-Nitrocinnamoyl)amino]morphinones, 14.beta.-[(p-nitrocinnamoyl)amino]-7,8-dihydromorphinones, and their codeinone analogs: synthesis and receptor activity Alice Sebastian, Jean M. Bidlack, Qi Jiang, Darlene Deecher, Milton Teitler, Stanley D. Glick, and Sydney Archer pp 3154 - 3160; DOI: 10.1021/jm00073a015 |
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Synthesis of (R,S)-trans-8-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'-propenyl)amino]tetralin (trans 8-OH-PIPAT): a new 5-HT1A receptor ligand Zhi Ping Zhuang, Mei Ping Kung, and Hank F. Kung pp 3161 - 3165; DOI: 10.1021/jm00073a016 |
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The interaction of ammonium, sulfonium, and sulfide analogs of metoclopramide with the dopamine D2 receptor Marc W. Harrold, Anong Sriburi, Kazuhisa Matsumoto, Duane D. Miller, Tahira Farooqui, and Norman Uretsky pp 3166 - 3170; DOI: 10.1021/jm00073a017 |
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Voronoi modeling: the binding of triazines and pyrimidines to L. casei dihydrofolate reductase Mary P. Bradley and Gordon M. Crippen pp 3171 - 3177; DOI: 10.1021/jm00073a018 |
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Efficient inhibition of human leukocyte elastase and cathepsin G by saccharin derivatives William C. Groutas, Nadene Houser-Archield, Lee S. Chong, Radhika Venkataraman, Jeffrey B. Epp, He Huang, and Jerald J. McClenahan pp 3178 - 3181; DOI: 10.1021/jm00073a019 |
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TIPP[.psi.]: a highly potent and stable pseudopeptide .delta. opioid receptor antagonist with extraordinary .delta. selectivity Peter W. Schiller, Grazyna Weltrowska, Thi M. D. Nguyen, Brian C. Wilkes, Nga N. Chung, and Carole Lemieux pp 3182 - 3187; DOI: 10.1021/jm00073a020 |
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Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists Clas Sonesson, Nicholas Waters, Kjell Svensson, Arvid Carlsson, Martin W. Smith, Montford F. Piercey, Eddi Meier, and Haakan Wikstroem pp 3188 - 3196; DOI: 10.1021/jm00073a021 |
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Synthesis, in vitro binding profile, and autoradiographic analysis of [3H]-cis-3-[(2-methoxybenzyl)amino]-2-phenylpiperidine, a highly potent and selective nonpeptide substance P receptor antagonist radioligand Terry Rosen, Thomas F. Seeger, Stafford McLean, Manoj C. Desai, Karen J. Guarino, Dianne Bryce, Kara Pratt, James Heym, Philip M. Chalabi, and et al. pp 3197 - 3201; DOI: 10.1021/jm00073a022 |
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Troeger's base. An alternate synthesis and a structural analog with thromboxane A2 synthetase inhibitory activity Roy A. Johnson, Robert R. Gorman, Richard J. Wnuk, Norman J. Crittenden, and James W. Aiken pp 3202 - 3206; DOI: 10.1021/jm00073a023 |
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A potent, orally active, balanced affinity angiotensin II AT1 antagonist and AT2 binding inhibitor Stephen E. de Laszlo, Carol S. Quagliato, William J. Greenlee, Arthur A. Patchett, Raymond S. L. Chang, Victor J. Lotti, Tsing Bau Chen, Stacey A. Scheck, Kristi A. Faust, and et al. pp 3207 - 3210; DOI: 10.1021/jm00073a024 |
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3-(Alkylamino)-4H-pyrido[4,3-e]1,2,4-thiadiazine 1,1-dioxides as powerful inhibitors of insulin release from rat pancreatic B-cells: a new class of potassium channel openers? Bernard Pirotte, Pascal de Tullio, Philippe Lebrun, Marie Helene Antoine, Jeanine Fontaine, Bernard Masereel, Marc Schynts, Leon Dupont, Andre Herchuelz, and Jacques Delarge pp 3211 - 3213; DOI: 10.1021/jm00073a025 |
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Synthesis and biological activity of N6-(p-sulfophenyl)alkyl and N6-sulfoalkyl derivatives of adenosine: water-soluble and peripherally selective adenosine agonists. [Erratum to document cited in CA117(23):234413y] Kenneth A. Jacobson, Olga Nikodijevic, Xiao Duo Ji, Deborah A. Berkich, David Eveleth, Reginald L. Dean, Kenichiro Hiramatsu, Neal F. Kassell, Philip J. M. Van Galen, and et al. pp 3218 - 3218; DOI: 10.1021/jm00073a026 |
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(.+-.)-3-Amino-6-carboxamido-1,2,3,4-tetrahydrocarbazole: A conformationally restricted analog of 5-carboxamidotryptamine with selectivity for the serotonin 5-HT1D receptor. [Erratum to document cited in CA119(11):117079z] Frank D. King, Anthony M. Brown, Laramie M. Gaster, Alberto J. Kaumann, Andrew D. Medhurst, Stephen G. Parker, Andrew A. Parsons, Tracey L. Patch, and Pravin Raval pp 3218 - 3218; DOI: 10.1021/jm00073a027 |
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Book Reviews pp 3214 - 3217; DOI: 10.1021/jm00073a600 |
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Structure-activity relationship within a series of pyrazolidinone antibacterial agents. 1. Effect of nuclear modification on in vitro activity Robert J. Ternansky and Susan E. Draheim pp 3219 - 3223; DOI: 10.1021/jm00074a001 |
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Structure-activity relationship within a series of pyrazolidinone antibacterial agents. 2. Effect of side-chain modification on in vitro activity and pharmacokinetic parameters Robert J. Ternansky, Susan E. Draheim, Andrew J. Pike, Fred T. Counter, Judy A. Eudaly, and Jeffrey S. Kasher pp 3224 - 3229; DOI: 10.1021/jm00074a002 |
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TSAO analogs. 3. Synthesis and anti-HIV-1 activity of 2',5'-bis-O-(tert-butyldimethylsilyl)-.beta.-D-ribofuranosyl 3'-spiro-5"-(4"-amino-1",2"-oxathiole 2",2"-dioxide) purine and purine-modified nucleosides Sonsoles Velazquez, Ana San-Felix, Maria Jesus Perez-Perez, Jan Balzarini, Erik De Clercq, and Maria Jose Camarasa pp 3230 - 3239; DOI: 10.1021/jm00074a003 |
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Antipicornavirus activity of tetrazole analogs related to disoxaril Guy D. Diana, David Cutcliffe, Deborah L. Volkots, John P. Mallamo, Thomas R. Bailey, Niranjan Vescio, Richard C. Oglesby, Theodore J. Nitz, Joseph Wetzel, and et al. pp 3240 - 3250; DOI: 10.1021/jm00074a004 |
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Inhibitors of blood platelet cAMP phosphodiesterase. 4. Structural variation of the side-chain terminus of water-soluble 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-one derivatives Nicholas A. Meanwell, Piyasena Hewawasam, Jeanine A. Thomas, J. J. Kim Wright, John W. Russell, Marianne Gamberdella, Harold J. Goldenberg, Steven M. Seiler, and George B. Zavoico pp 3251 - 3264; DOI: 10.1021/jm00074a005 |
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Conformational analysis of a highly potent dicyclic gonadotropin-releasing hormone antagonist by nuclear magnetic resonance and molecular dynamics Rachelle J. Bienstock, Josep Rizo, Steven C. Koerber, Jean E. Rivier, Arnold T. Hagler, and Lila M. Gierasch pp 3265 - 3273; DOI: 10.1021/jm00074a006 |
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Crystal structure, absolute configuration, and phosphodiesterase inhibitory activity of (+)-1-(4-bromobenzyl)-4-[(3-cyclopentyloxy)-4-methoxyphenyl]-2-pyrrolidinone Paul W. Baures, Drake S. Eggleston, Karl F. Erhard, Lenora B. Cieslinski, Theodore J. Torphy, and Siegfried B. Christensen pp 3274 - 3277; DOI: 10.1021/jm00074a007 |
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Non-steroidal glucocorticoid-like substances: receptor binding and in vivo activity Virendra Kumar, Malcolm R. Bell, Joseph R. Wetzel, John L. Herrmann, Ruthann McGarry, H. Phillip Schane, Richard C. Winneker, Ben W. Snyder, and Anthony J. Anzalone pp 3278 - 3285; DOI: 10.1021/jm00074a008 |
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5-HT3 Receptor antagonists. 3. Quinoline derivatives which may be effective in the therapy of irritable bowel syndrome Nobuyuki Kishibayashi, Yoshikazu Miwa, Hiroaki Hayashi, Akio Ishii, Shunji Ichikawa, Hiromi Nonaka, Toshihide Yokoyama, and Fumio Suzuki pp 3286 - 3292; DOI: 10.1021/jm00074a009 |
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N-Substituted dibenzoxazepines as analgesic PGE2 antagonists E. Ann. Hallinan, Timothy J. Hagen, Robert K. Husa, Sofya Tsymbalov, Shashidhar N. Rao, Jean Pierre vanHoeck, Michael F. Rafferty, Awilda Stapelfeld, Michael A. Savage, and Melvin Reichman pp 3293 - 3299; DOI: 10.1021/jm00074a010 |
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Inhibitors of acyl-CoA:cholesterol acyltransferase. 4. A novel series of urea ACAT inhibitors as potential hypocholesterolemic agents Bharat K. Trivedi, Ann Holmes, Terri L. Stoeber, C. John Blankley, W. Howard Roark, Joseph A. Picard, Mary K. Shaw, Arnold D. Essenburg, Richard L. Stanfield, and Brian R. Krause pp 3300 - 3307; DOI: 10.1021/jm00074a011 |
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Synthesis of structural analogs of leukotriene B4 and their receptor binding activity William D. Kingsbury, Israil Pendrak, Jack D. Leber, Jeffery C. Boehm, Brenda Mallet, Henry M. Sarau, James J. Foley, Dulcie B. Schmidt, and Robert A. Daines pp 3308 - 3320; DOI: 10.1021/jm00074a012 |
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Trisubstituted pyridine leukotriene B4 receptor antagonists: synthesis and structure-activity relationships Robert A. Daines, Pamela A. Chambers, Israil Pendrak, Dalia R. Jakas, Henry M. Sarau, James J. Foley, Dulcie B. Schmidt, and William D. Kingsbury pp 3321 - 3332; DOI: 10.1021/jm00074a013 |
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Synthesis and LTB4 receptor antagonist activities of the naturally occurring LTB4 receptor antagonist leucettamine A and related analogs Jeffrey C. Boehm, John G. Gleason, Israil Pendrak, Henry M. Sarau, Dulcie B. Schmidt, James J. Foley, and William D. Kingsbury pp 3333 - 3340; DOI: 10.1021/jm00074a014 |
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Synthesis of paraxanthine analogs (1,7-disubstituted xanthines) and other xanthines unsubstituted at the 3-position: structure-activity relationships at adenosine receptors Christa E. Mueller, Dan Shi, Malcolm Manning, and John W. Daly pp 3341 - 3349; DOI: 10.1021/jm00074a015 |
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Synthesis and anticonvulsant activities of .alpha.-heterocyclic .alpha.-acetamido-N-benzylacetamide derivatives Harold Kohn, Kailash N. Sawhney, Patrick Bardel, David W. Robertson, and J. David Leander pp 3350 - 3360; DOI: 10.1021/jm00074a016 |
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4,5-Dihydro-1-phenyl-1H-2,4-benzodiazepines: Novel antiarrhythmic agents Robert E. Johnson, Eugene R. Baizman, Carolyn Becker, Eric A. Bohnet, Rebecca H. Bell, Nancy C. Birsner, Carl A. Busacca, Philip M. Carabateas, Christopher C. Chadwick, and et al. pp 3361 - 3370; DOI: 10.1021/jm00074a017 |
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A new series of imidazolones: highly specific and potent nonpeptide AT1 angiotensin II receptor antagonists Claude A. Bernhart, Pierre M. Perreaut, Bernard P. Ferrari, Yvette A. Muneaux, Jean Louis A. Assens, Jacques Clement, Frederique Haudricourt, Claude F. Muneaux, Joelle E. Taillades, and et al. pp 3371 - 3380; DOI: 10.1021/jm00074a018 |
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Synthesis, optical resolution, absolute configuration, and preliminary pharmacology of (+)- and (-)-cis-2,3,3a,4,5,9b-hexahydro-1-methyl-1H-pyrrolo[3,2-h]isoquinoline, a structural analog of nicotine William Glassco, John Suchocki, Clifford George, Billy R. Martin, and Everette L. May pp 3381 - 3385; DOI: 10.1021/jm00074a019 |
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3-Acyl-4-hydroxyquinolin-2(1H)-ones. Systemically active anticonvulsants acting by antagonism at the glycine site of the N-methyl-D-aspartate receptor complex Michael Rowley, Paul D. Leeson, Graeme I. Stevenson, Angela M. Moseley, Ian Stansfield, Ian Sanderson, Lesley Robinson, Raymond Baker, John A. Kemp, and et al. pp 3386 - 3396; DOI: 10.1021/jm00074a020 |
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3-Nitro-3,4-dihydro-2(1H)-quinolones. Excitatory amino acid antagonists acting at glycine-site NMDA and (RS)-.alpha.-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors Robert W. Carling, Paul D. Leeson, Kevin W. Moore, Julian D. Smith, Christopher R. Moyes, Ian M. Mawer, Steven Thomas, Tony Chan, Raymond Baker, and et al. pp 3397 - 3408; DOI: 10.1021/jm00074a021 |
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Orally active central dopamine and serotonin receptor ligands: 5-, 6-, 7-, and 8-[[(trifluoromethyl)sulfonyl]oxy]-2-(di-n-propylamino)tetralins and the formation of active metabolites in vivo Clas Sonesson, Maria Boije, Kjell Svensson, Agneta Ekman, Arvid Carlsson, Arthur G. Romero, Iain J. Martin, J. Neil Duncan, Laurence J. King, and Hakan Wikstrom pp 3409 - 3416; DOI: 10.1021/jm00074a022 |
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Conformationally restricted analogs of remoxipride as potential antipsychotic agents Mark H. Norman, James L. Kelley, and Elizabeth B. Hollingsworth pp 3417 - 3423; DOI: 10.1021/jm00074a023 |
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New adenosine kinase inhibitors with oral antiinflammatory activity: synthesis and biological evaluation Howard B. Cottam, D. Bruce Wasson, Hsien C. Shih, Anil Raychaudhuri, Gene Di Pasquale, and Dennis A. Carson pp 3424 - 3430; DOI: 10.1021/jm00074a024 |
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Alkylpurines as immunopotentiating agents. Synthesis and antiviral activity of certain alkylguanines Maged A. Michael, Howard B. Cottam, Donald F. Smee, Roland K. Robins, and Ganesh D. Kini pp 3431 - 3436; DOI: 10.1021/jm00074a025 |
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Synthesis of 5-methyl-5-deaza nonclassical antifolates as inhibitors of dihydrofolate reductases and as potential antipneumocystis, antitoxoplasma, and antitumor agents Aleem Gangjee, Jufang Shi, Sherry F. Queener, Louis R. Barrows, and Roy L. Kisliuk pp 3437 - 3443; DOI: 10.1021/jm00074a026 |
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Fluorocyclopropyl quinolones. 1. Synthesis and structure-activity relationships of 1-(2-fluorocyclopropyl)-3-pyridonecarboxylic acid antibacterial agents Shohgo Atarashi, Masazumi Imamura, Youichi Kimura, Atomi Yoshida, and Isao Hayakawa pp 3444 - 3448; DOI: 10.1021/jm00074a027 |
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Quinolinecarboxylic acids. 3. Synthesis and antibacterial evaluation of 2-substituted 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids related to rufloxacin Violetta Cecchetti, Arnaldo Fravolini, Pier Giuseppe Pagella, Angela Savino, and Oriana Tabarrini pp 3449 - 3454; DOI: 10.1021/jm00074a028 |
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9-[(Phosphonoalkyl)benzyl]guanines. Multisubstrate analog inhibitors of human erythrocyte purine nucleoside phosphorylase James L. Kelley, James A. Linn, Ed W. McLean, and Joel V. Tuttle pp 3455 - 3463; DOI: 10.1021/jm00074a029 |
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Benzoquinazoline inhibitors of thymidylate synthase: enzyme inhibitory activity and cytotoxicity of some sulfonamidobenzoylglutamate and related derivatives William Pendergast, Scott H. Dickerson, Jay V. Johnson, Inderjit K. Dev, Robert Ferone, David S. Duch, and Gary K. Smith pp 3464 - 3471; DOI: 10.1021/jm00074a030 |
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Peptide .alpha.-keto ester, .alpha.-keto amide, and .alpha.-keto acid inhibitors of calpains and other cysteine proteases Zhaozhao Li, Girish S. Patil, Zbigniew E. Golubski, Hitoshi Hori, Kamin Tehrani, J. E. Foreman, David D. Eveleth, Raymond T. Bartus, and James C. Powers pp 3472 - 3480; DOI: 10.1021/jm00074a031 |
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Dopamine receptor modulation by a highly rigid spiro bicyclic peptidomimetic of Pro-Leu-Gly-NH2 Michael J. Genin, Ram K. Mishra, and Rodney L. Johnson pp 3481 - 3483; DOI: 10.1021/jm00074a032 |
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A tight binding inhibitor of 5-aminoimidazole ribonucleotide carboxylase Steven M. Firestine and V. Jo Davisson pp 3484 - 3486; DOI: 10.1021/jm00074a033 |
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Book Reviews pp 3487 - 3488; DOI: 10.1021/jm00074a600 |
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On the mechanism of HRV-14 antiviral compounds: slow growth as a conformational search procedure Michael Guha-Biswas, Michael Holder, and B. Montgomery Pettitt pp 3489 - 3495; DOI: 10.1021/jm00075a001 |
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Synthesis and evaluation of 1-acyl-1,2-bis(methylsulfonyl)-2-(2-chloroethyl)hydrazines as antineoplastic agents Krishnamurthy Shyam, Philip G. Penketh, Alan A. Divo, Regina H. Loomis, William C. Rose, and Alan C. Sartorelli pp 3496 - 3502; DOI: 10.1021/jm00075a002 |
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Isosteres of the DNA polymerase inhibitor aphidicolin as potential antiviral agents against human herpes viruses David L. Selwood, S. Richard Challand, John N. Champness, Janet Gillam, Deborah K. Hibberd, K. Singh Jandu, Denise Lowe, Michael Pether, John Selway, and George E. Trantor pp 3503 - 3510; DOI: 10.1021/jm00075a003 |
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Comparative molecular field analysis of in vitro growth inhibition of L1210 and HCT-8 cells by some pyrazoloacridines Jerome P. Horwitz, Irina Massova, Thomas E. Wiese, Antoinette J. Wozniak, Thomas H. Corbett, Judith S. Sebolt-Leopold, David B. Capps, and Wilbur R. Leopold pp 3511 - 3516; DOI: 10.1021/jm00075a004 |
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Synthesis and calculated log P correlation of imidooxy anticonvulsants Vida A. Farrar, M. Ciechanowicz-Rutkowska, J. Grochowski, P. Serda, T. Pilati, G. Filippini, Christine N. Hinko, Afif El-Assadi, Jacqueline A. Moore, and et al. pp 3517 - 3525; DOI: 10.1021/jm00075a005 |
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(R)-1,2,3,4-Tetrahydro[1]benzothieno[2,3-c]pyridines: novel optically active compounds with strong 5-HT1A receptor binding ability exhibiting anticonflict activity and lessening of memory impairment Hiromu Kawakubo, Seiji Takagi, Yuuji Yamaura, Shinichi Katoh, Yumiko Ishimoto, Tadashi Nagatani, Daisuke Mochizuki, Tomoko Kamata, and Yasuharu Sasaki pp 3526 - 3532; DOI: 10.1021/jm00075a006 |
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The synthesis and biochemical pharmacology of enantiomerically pure methylated oxotremorine derivatives Eugene J. Trybulski, Jing Zhang, Richard H. Kramss, and Richard M. Mangano pp 3533 - 3541; DOI: 10.1021/jm00075a007 |
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Aminoacyl analogs of chloramphenicol: examination of the kinetics of inhibition of peptide bond formation Denis Drainas, Petros Mamos, and Charalambos Coutsogeorgopoulos pp 3542 - 3545; DOI: 10.1021/jm00075a008 |
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Preparation and anti-HIV activity of O-acylated heparin and dermatan sulfate derivatives with low anticoagulant effect Tereza Barzu, Michel Level, Maurice Petitou, Jean Claude Lormeau, Jean Choay, Dominique Schols, Masanori Baba, Rudi Pauwels, Myriam Witvrouw, and Erik De Clercq pp 3546 - 3555; DOI: 10.1021/jm00075a009 |
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Tyrphostins. 3. Structure-activity relationship studies of .alpha.-substituted benzylidenemalononitrile 5-S-aryltyrphostins Aviv Gazit, Nir Osherov, Israel Posner, Allan Bar-Sinai, Chaim Gilon, and Alexander Levitzki pp 3556 - 3564; DOI: 10.1021/jm00075a010 |
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A Unified Framework for Using Neural Networks To Build QSARs Ajay pp 3565 - 3571; DOI: 10.1021/jm00075a011 |
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Analysis of cocaine receptor site ligand binding by three-dimensional Voronoi site modeling approach Sanjay Srivastava and Gordon M. Crippen pp 3572 - 3579; DOI: 10.1021/jm00075a012 |
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Substituted chromenes as potent, orally active 5-lipoxygenase inhibitors Yoshitaka Satoh, James L. Stanton, Alan J. Hutchison, Adam H. Libby, Timothy J. Kowalski, Warren H. Lee, D. Hope White, and Earl F. Kimble pp 3580 - 3594; DOI: 10.1021/jm00075a013 |
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Nonpeptide angiotensin II antagonists derived from 1H-pyrazole-5-carboxylates and 4-aryl-1H-imidazole-5-carboxylates Wallace T. Ashton, Steven M. Hutchins, William J. Greenlee, George A. Doss, Raymond S. L. Chang, Victor J. Lotti, Kristie A. Faust, Tsing Bau Chen, Gloria J. Zingaro, and et al. pp 3595 - 3605; DOI: 10.1021/jm00075a014 |
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Transformation of heterocyclic reversible monoamine oxidase-B inactivators into irreversible inactivators by N-methylation Charles Z. Ding and Richard B. Silverman pp 3606 - 3610; DOI: 10.1021/jm00075a015 |
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2-Thio derivatives of dUrd and 5-fluoro-dUrd and their 5'-monophosphates: synthesis, interaction with tumor thymidylate synthase, and in vitro antitumor activity Maria Bretner, Tadeusz Kulikowski, Jolanta M. Dzik, Malgorzata Balinska, Wojciech Rode, and David Shugar pp 3611 - 3617; DOI: 10.1021/jm00075a016 |
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Synthesis, chemical reactivity, and antitumor evaluation of congeners of carmethizole hydrochloride, an experimental acylated vinylogous carbinolamine tumor inhibitor Mark A. Jarosinski, Peech S. Reddy, and Wayne K. Anderson pp 3618 - 3627; DOI: 10.1021/jm00075a017 |
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Synthesis and evaluation of 3-modified 1D-myo-inositols as inhibitors and substrates of phosphatidylinositol synthase and inhibitors of myo-inositol uptake by cells Stephen C. Johnson, Jean Dahl, Tzenge Lien Shih, David J. A. Schedler, Laurens Anderson, Thomas L. Benjamin, and David C. Baker pp 3628 - 3635; DOI: 10.1021/jm00075a018 |
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Protonation of phosphoramide mustard and other phosphoramides Michael P. Gamcsik, Susan M. Ludeman, Ellen M. Shulman-Roskes, Ian J. McLennan, Michael E. Colvin, and O. Michael Colvin pp 3636 - 3645; DOI: 10.1021/jm00075a019 |
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Inhibitors of cholesterol biosynthesis. 1. 3,5-Dihydroxy-7-(N-imidazolyl)-6-heptenoates and -heptanoates, a novel series of 3-hydroxy-3-methylglutarate-CoA reductase inhibitors Chuen Chan, Esme J. Bailey, C. David Hartley, David F. Hayman, Julie L. Hutson, Graham G. A. Inglis, Paul S. Jones, Suzanne E. Keeling, Barrie E. Kirk, and et al. pp 3646 - 3657; DOI: 10.1021/jm00075a020 |
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Inhibitors of cholesterol biosynthesis. 2. 3,5-Dihydroxy-7-(N-pyrrolyl)-6-heptenoates, a novel series of HMG-CoA reductase inhibitors Panayiotis A. Procopiou, Christopher D. Draper, Julie L. Hutson, Graham G. A. Inglis, Barry C. Ross, and Nigel S. Watson pp 3658 - 3662; DOI: 10.1021/jm00075a021 |
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Preparation, characterization, cytotoxicity, and mutagenicity of a pair of enantiomeric platinum(II) complexes with the potential to bind enantioselectively to DNA Kymberley Vickery, Antonio M. Bonin, Ronald R. Fenton, Shaun O'Mara, Pamela J. Russell, Lorraine K. Webster, and Trevor W. Hambley pp 3663 - 3668; DOI: 10.1021/jm00075a022 |
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Possible contribution of a glutathione conjugate to the long-duration action of .beta.-funaltrexamine D. L. Larson, M. Hua, A. E. Takemori, and P. S. Portoghese pp 3669 - 3673; DOI: 10.1021/jm00075a023 |
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HMG-CoA reductase inhibitors: design, synthesis, and biological activity of tetrahydroindazole-substituted 3,5-dihydroxy-6-heptenoic acid sodium salts Peter J. Connolly, Claudia D. Westin, Deborah A. Loughney, and Lisa K. Minor pp 3674 - 3685; DOI: 10.1021/jm00075a024 |
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Synthesis and evaluation of new 6-amino- substituted benzo[c]phenanthridine derivatives Yves L. Janin, Alain Croisy, Jean Francois Riou, and Emile Bisagni pp 3686 - 3692; DOI: 10.1021/jm00075a025 |
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Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annulated indole derivatives. 1 Ineke van Wijngaarden, Derk Hamminga, Rolf van Hes, Piet J. Standaar, Jacobus Tipker, Martin T. M. Tulp, Frans Mol, Berend Olivier, and Adriaan de Jonge pp 3693 - 3699; DOI: 10.1021/jm00075a026 |
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Synthesis and pharmacological examination of benzofuran, indan, and tetralin analogs of 3,4-(methylenedioxy)amphetamine Aaron P. Monte, Danuta Marona-Lewicka, Nicholas V. Cozzi, and David E. Nichols pp 3700 - 3706; DOI: 10.1021/jm00075a027 |
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Fluorine-18 labeled benzamides for studying the dopamine D2 receptor with positron emission tomography Robert H. Mach, Robert R. Leudtke, Christopher D. Unsworth, Virginia A. Boundy, Peggy A. Nowak, James G. Scripko, S. Todd Elder, Joseph R. Jackson, Patricia L. Hoffman, and et al. pp 3707 - 3720; DOI: 10.1021/jm00075a028 |
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Synthesis and binding properties of 2-amino-5-phosphono-3-pentenoic acid photoaffinity ligands as probes for the glutamate recognition site of the NMDA receptor Roland Heckendorn, Hans Allgeier, Jaqueline Baud, Wilfried Gunzenhauser, and Christof Angst pp 3721 - 3726; DOI: 10.1021/jm00075a029 |
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Synthesis and antiviral activity of 5'-deoxypyrazofurin Xing Chen, Stewart W. Schneller, Satoru Ikeda, Robert Snoeck, Graciela Andrei, Jan Balzarini, and Erik De Clercq pp 3727 - 3730; DOI: 10.1021/jm00075a030 |
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Photoisomerization of a potent and selective adenosine A2 antagonist, (E)-1,3-dipropyl-8-(3,4-dimethoxystyryl)-7-methylxanthine Yoshiko Nonaka, Junichi Shimada, Hiromi Nonaka, Nobuaki Koike, Noboru Aoki, Hiroyuki Kobayashi, Hiroshi Kase, Kazuo Yamaguchi, and Fumio Suzuki pp 3731 - 3733; DOI: 10.1021/jm00075a031 |
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Synthesis and biological activity of some methoctramine-related tetraamines bearing an 11-acetyl-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one moiety as antimuscarinics: a second generation of highly selective M2 muscarinic receptor antagonists Carlo Melchiorre, Maria L. Bolognesi, Alberto Chiarini, Anna Minarini, and Santi Spampinato pp 3734 - 3737; DOI: 10.1021/jm00075a032 |
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(Dipropylphenoxy)phenylacetic acids: a new generation of nonpeptide angiotensin II receptor antagonists 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, Prasun K. Chakravarty, and et al. pp 3738 - 3742; DOI: 10.1021/jm00075a033 |
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A homologous series of permanently charged 1,4-dihydropyridines: novel probes designed to localize drug binding sites on ion channels Nandkishore Baindur, Aleta Rutledge, and David J. Triggle pp 3743 - 3745; DOI: 10.1021/jm00075a034 |
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A mechanism-based inactivation study of neutral endopeptidase 24.11. [Erratum to document cited in CA119(13):134114z] Odile E. Levy, Pascale Taibi, Shahriar Mobashery, and Soumitra Ghosh pp 3746 - 3746; DOI: 10.1021/jm00075a035 |
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Phe3-substituted analogs of deltorphin C. Spatial conformation and topography of the aromatic ring in peptide recognition by .delta. opioid receptors Severo Salvadori, Sharon D. Bryant, Clementina Bianchi, Gianfranco Balboni, Valeria Scaranari, Martti Attila, and Lawrence H. Lazarus pp 3748 - 3756; DOI: 10.1021/jm00076a001 |
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Solvent-dependent conformation and hydrogen-bonding capacity of cyclosporin A: evidence from partition coefficients and molecular dynamics simulations Nabil El Tayar, Alan E. Mark, Philippe Vallat, Roger M. Brunne, Bernard Testa, and Wilfred F. van Gunsteren pp 3757 - 3764; DOI: 10.1021/jm00076a002 |
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Cyclic GMP phosphodiesterase inhibitors. 1. The discovery of a novel potent inhibitor, 4-[[3,4-(methylenedioxy)benzyl]amino]-6,7,8-trimethoxyquinazoline Yasutaka Takase, Takao Saeki, Masatoshi Fujimoto, and Isao Saito pp 3765 - 3770; DOI: 10.1021/jm00076a003 |
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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 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 3771 - 3783; DOI: 10.1021/jm00076a004 |
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Synthesis and anti-HIV-1 activity of a series of imidazo[1,5-b]pyridazines David G. H. Livermore, Richard C. Bethell, Nicholas Cammack, Ashley P. Hancock, Michael M. Hann, Darren V. S. Green, R. Brian Lamont, Stewart A. Noble, David C. Orr, and et al. pp 3784 - 3794; DOI: 10.1021/jm00076a005 |
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Analysis of two cycloplatinated compounds derived from N-(4-methoxyphenyl)-.alpha.-benzoylbenzylidenamine. Comparison of the activity of these compounds with other isostructural cyclopalladated compounds Carmen Navarro-Ranniger, Isabel Lopez-Solera, Jose M. Perez, Jesus Rodriguez, Jose L. Garcia-Ruano, Paul R. Raithby, Jose R. Masaguer, and Carlos Alonso pp 3795 - 3801; DOI: 10.1021/jm00076a006 |
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Neuropeptide Y: Y1 and Y2 affinities of the complete series of analogs with single D-residue substitutions Dean A. Kirby, Jaroslav H. Boublik, and Jean E. Rivier pp 3802 - 3808; DOI: 10.1021/jm00076a007 |
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Analyses of ligand binding in five endothiapepsin crystal complexes and their use in the design and evaluation of novel renin inhibitors Elizabeth A. Lunney, Harriet W. Hamilton, John C. Hodges, James S. Kaltenbronn, Joseph T. Repine, Mohammed Badasso, Jon B. Cooper, Chris Dealwis, Bonnie A. Wallace, and et al. pp 3809 - 3820; DOI: 10.1021/jm00076a008 |
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Design and synthesis of an orally active macrocyclic neutral endopeptidase 24.11 inhibitor Lawrence J. MacPherson, Erol K. Bayburt, Michael P. Capparelli, Regine S. Bohacek, Frank H. Clarke, Rajendra D. Ghai, Yumi Sakane, Carol J. Berry, Jane V. Peppard, and Angelo J. Trapani pp 3821 - 3828; DOI: 10.1021/jm00076a009 |
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Heterocyclic lactam derivatives as dual angiotensin converting enzyme and neutral endopeptidase 24.11 inhibitors James L. Stanton, Donald M. Sperbeck, Angelo J. Trapani, Donald Cote, Yumi Sakane, Carol J. Berry, and Rajendra D. Ghai pp 3829 - 3833; DOI: 10.1021/jm00076a010 |
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Synthesis, antiproliferative, and antiviral activity of 4-amino-1-(.beta.-D-ribofuranosyl)pyrrolo[2,3-d]pyridazin-7(6H)-one and related derivatives Eric A. Meade, Linda L. Wotring, John C. Drach, and Leroy B. Townsend pp 3834 - 3842; DOI: 10.1021/jm00076a011 |
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Synthesis of 2,4-disubstituted thiazoles and selenazoles as potential antitumor and antifilarial agents. 1. Methyl 4-(isothiocyanatomethyl)thiazole-2-carbamates, -selenazole-2-carbamates, and related derivatives Yatendra Kumar, Rachel Green, Katherine Z. Borysko, Dean S. Wise, Linda L. Wotring, and Leroy B. Townsend pp 3843 - 3848; DOI: 10.1021/jm00076a012 |
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Synthesis of 2,4-disubstituted thiazoles and selenazoles as potential antifilarial and antitumor agents. 2. 2-Arylamido and 2-alkylamido derivatives of 2-amino-4-(isothiocyanatomethyl)thiazole and 2-amino-4-(isothiocyanatomethyl)selenazole Yatendra Kumar, Rachel Green, Dean S. Wise, Linda L. Wotring, and Leroy B. Townsend pp 3849 - 3852; DOI: 10.1021/jm00076a013 |
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Novel inhibitors of prolyl 4-hydroxylase. 5. The intriguing structure-activity relationships seen with 2,2'-bipyridine and its 5,5'-dicarboxylic acid derivatives Neil J. Hales and John F. Beattie pp 3853 - 3858; DOI: 10.1021/jm00076a014 |
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R2 C-terminal peptide inhibition of mammalian and yeast ribonucleotide reductase Alison Fisher, Fu De Yang, Harvey Rubin, and Barry S. Cooperman pp 3859 - 3862; DOI: 10.1021/jm00076a015 |
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The NEWLEAD program: a new method for the design of candidate structures from pharmacophoric hypotheses Vincenzo Tschinke and Nissim Claude Cohen pp 3863 - 3870; DOI: 10.1021/jm00076a016 |
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Nonprostanoid prostacyclin mimetics. 4. Derivatives of 2-[3-[2-(4,5-diphenyl-2-oxazolyl)ethyl]phenoxy]acetic acid substituted .alpha. to the oxazole ring Nicholas A. Meanwell, Michael J. Rosenfeld, J. J. Kim Wright, Catherine L. Brassard, John O. Buchanan, Marianne E. Federici, J. Stuart Fleming, Marianne Gamberdella, Karen S. Hartl, and et al. pp 3871 - 3883; DOI: 10.1021/jm00076a017 |
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Nonprostanoid prostacyclin mimetics. 5. Structure-activity relationships associated with [3-[4-(4,5-diphenyl-2-oxazolyl)-5-oxazolyl]phenoxy]acetic acid Nicholas A. Meanwell, Jeffrey L. Romine, Michael J. Rosenfeld, Scott W. Martin, Ashok K. Trehan, J. J. Kim Wright, Mary F. Malley, Jack Z. Gougoutas, Catherine L. Brassard, and et al. pp 3884 - 3903; DOI: 10.1021/jm00076a018 |
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3,4-Dihydroxychalcones as potent 5-lipoxygenase and cyclooxygenase inhibitors Satoshi Sogawa, Yasunori Nihro, Hiroki Ueda, Akihiro Izumi, Tokutaro Miki, Hitoshi Matsumoto, and Toshio Satoh pp 3904 - 3909; DOI: 10.1021/jm00076a019 |
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Molecular structures, conformational analysis, and preferential modes of binding of 3-aroyl-2-arylbenzo[b]thiophene estrogen receptor ligands: LY117018 and aryl azide photoaffinity labeling analogs Philip R. Kym, Gregory M. Anstead, Kevin G. Pinney, Scott R. Wilson, and John A. Katzenellenbogen pp 3910 - 3922; DOI: 10.1021/jm00076a020 |
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N-(1-Arylpropionyl)-4-aryltetrahydropyridines, a new class of high-affinity selective .sigma. receptor ligands David I. Schuster, Yan Ping Pan, Guyanand Singh, George Stoupakis, Bing Cai, George Lem, George K. Ehrlich, William Frietze, and Randall B. Murphy pp 3923 - 3928; DOI: 10.1021/jm00076a021 |
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Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and .sigma. receptors Juan C. Jaen, Bradley W. Caprathe, Thomas A. Pugsley, Lawrence D. Wise, and Hyacinth Akunne pp 3929 - 3936; DOI: 10.1021/jm00076a022 |
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Identification of potent, selective P2Y-purinoceptor agonists: structure-activity relationships for 2-thioether derivatives of adenosine 5'-triphosphate Bilha Fischer, Jose L. Boyer, Charles H. V. Hoyle, Airat U. Ziganshin, Antonia L. Brizzolara, Gillian E. Knight, Jeffrey Zimmet, Geoffrey Burnstock, T. Kendall Harden, and Kenneth A. Jacobson pp 3937 - 3946; DOI: 10.1021/jm00076a023 |
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Syntheses of 2,5- and 2,6-difluoronorepinephrine, 2,5-difluoroepinephrine, and 2,6-difluorophenylephrine: effect of disubstitution with fluorine on adrenergic activity George T. Chen, Michael King, Fabian Gusovsky, Cyrus R. Creveling, John W. Daly, Bang Hua Chen, Jun Ying Nie, and Kenneth L. Kirk pp 3947 - 3955; DOI: 10.1021/jm00076a024 |
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Neurosteroid analogs: structure-activity studies of benz[e]indene modulators of GABAA receptor function. 1. The effect of 6-methyl substitution on the electrophysiological activity of 7-substituted benz[e]indene-3-carbonitriles Yuefei Hu, Charles F. Zorumski, and Douglas F. Covey pp 3956 - 3967; DOI: 10.1021/jm00076a025 |
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New analogs of N-(2-aminoethyl)-4-chlorobenzamide (Ro 16-6491). Some of the most potent monoamine oxidase-B inactivators Nikoi Annan and Richard B. Silverman pp 3968 - 3970; DOI: 10.1021/jm00076a026 |
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Cardioselective anti-ischemic ATP-sensitive potassium channel openers Karnail S. Atwal, Gary J. Grover, Syed Z. Ahmed, Francis N. Ferrara, Timothy W. Harper, Kyoung S. Kim, Paul G. Sleph, Steven Dzwonczyk, Anita D. Russell, and et al. pp 3971 - 3974; DOI: 10.1021/jm00076a027 |
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Methoxylation of cocaine reduces binding affinity and produces compounds of differential binding and dopamine uptake inhibitory activity: discovery of a weak cocaine "antagonist" Daniele Simoni, Johannes Stoelwinder, Alan P. Kozikowski, Kenneth M. Johnson, John S. Bergmann, and Richard G. Ball pp 3975 - 3977; DOI: 10.1021/jm00076a028 |
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o-Phenylphenols: potent and orally active leukotriene B4 receptor antagonists Michael J. Sofia, Paul Floreancig, Nicholas J. Bach, S. Richard Baker, Sandra L. Cockerham, Jerome H. Fleisch, Larry L. Froelich, William T. Jackson, Philip Marder, and et al. pp 3978 - 3981; DOI: 10.1021/jm00076a029 |
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Biphenylyl-substituted xanthones: highly potent leukotriene B4 receptor antagonists J. Scott Sawyer, Ronald F. Baldwin, Michael J. Sofia, Paul Floreancig, Philip Marder, David L. Saussy Jr., Larry L. Froelich, Steven A. Silbaugh, Peter W. Stengel, and et al. pp 3982 - 3984; DOI: 10.1021/jm00076a030 |
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Editorial - Expedited Articles: A New Category for the Rapid Dissemination of Cutting-Edge Research Philip S. Portoghese pp 3747 - 3747; DOI: 10.1021/jm00076a600 |
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A novel series of selective, non-peptide inhibitors of angiotensin II binding to the AT2 site Mary K. VanAtten, Carol L. Ensinger, Andrew T. Chiu, Dale E. McCall, Tam T. Nguyen, Ruth R. Wexler, and Pieter B. M. W. M. Timmermans pp 3985 - 3992; DOI: 10.1021/jm00077a001 |
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Nanomolar-affinity, non-peptide oxytocin receptor antagonists Ben E. Evans, George F. Lundell, Kevin F. Gilbert, Mark G. Bock, Kenneth E. Rittle, Leigh Anne Carroll, Peter D. Williams, Joseph M. Pawluczyk, James L. Leighton, and et al. pp 3993 - 4005; DOI: 10.1021/jm00077a002 |
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Three-dimensional quantitative structure-activity relationships of 5-HT receptor binding data for tetrahydropyridinylindole derivatives: a comparison of the Hansch and CoMFA methods Atul Agarwal, Philip P. Pearson, Ethan Will Taylor, Hong B. Li, Torsten Dahlgren, Margareta Herslof, Youhua Yang, Georgina Lambert, David L. Nelson, and et al. pp 4006 - 4014; DOI: 10.1021/jm00077a003 |
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Xanthines with C8 chiral substituents as potent and selective adenosine A1 antagonists Norton P. Peet, Nelsen L. Lentz, Mark W. Dudley, Ann Marie L. Ogden, Deborah R. McCarty, and Margaret M. Racke pp 4015 - 4020; DOI: 10.1021/jm00077a004 |
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Antioxidant and neutrophil-inhibiting properties of new 2-O-methyl-6-(alkylthio)ascorbic acid derivatives Elmar Schmid, Volker Figala, Dagmar Roth, and Volker Ullrich pp 4021 - 4029; DOI: 10.1021/jm00077a005 |
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Synthesis of novel modified dipeptide inhibitors of human collagenase: .beta.-mercapto carboxylic acid derivatives Belle Beszant, John Bird, Laramie M. Gaster, Gregory P. Harper, Ian Hughes, Eric H. Karran, Roger E. Markwell, Anette J. Miles-Williams, and Stephen A. Smith pp 4030 - 4039; DOI: 10.1021/jm00077a006 |
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6-Substituted benzimidazoles as new nonpeptide angiotensin II receptor antagonists: synthesis, biological activity, and structure-activity relationships Uwe J. Ries, Gerhard Mihm, Berthold Narr, Kai M. Hasselbach, Helmut Wittneben, Michael Entzeroth, Jacobus C. A. van Meel, Wolfgang Wienen, and Norbert H. Hauel pp 4040 - 4051; DOI: 10.1021/jm00077a007 |
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Novel antiasthmatic agents with dual activities of thromboxane A2 synthetase inhibition and bronchodilation. 1. 2-[2-(1-Imidazolyl)alkyl]-1(2H)-phthalazinones Masahisa Yamaguchi, Kenshi Kamei, Takaki Koga, Michitaka Akima, Toshio Kuroki, and Nobuhiro Ohi pp 4052 - 4060; DOI: 10.1021/jm00077a008 |
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Novel antiasthmatic agents with dual activities of thromboxane A2 synthetase inhibition and bronchodilation. 2. 4-(3-Pyridyl)-1(2H)-phthalazinones Masahisa Yamaguchi, Kenshi Kamei, Takaki Koga, Michitaka Akima, Akinori Maruyama, Toshio Kuroki, and Nobuhiro Ohi pp 4061 - 4068; DOI: 10.1021/jm00077a009 |
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2-Substituted 5-methoxy-N-acyltryptamines: synthesis, binding affinity for the melatonin receptor, and evaluation of the biological activity Gilberto Spadoni, Bojidar Stankov, Andrea Duranti, Gabriele Biella, Valeria Lucini, Americo Salvatori, and Franco Fraschini pp 4069 - 4074; DOI: 10.1021/jm00077a010 |
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Further studies of the structure-activity relationships of 1-[1-(2-benzo[b]thienyl)cyclohexyl]piperidine. Synthesis and evaluation of 1-(2-benzo[b]thienyl)-N,N-dialkylcyclohexylamines at dopamine uptake and phencyclidine binding sites Xiaoshu He, Lionel P. Raymon, Mariena V. Mattson, Mohyee E. Eldefrawi, and Brian R. de Costa pp 4075 - 4081; DOI: 10.1021/jm00077a011 |
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Glucosidase inhibitors: structures of deoxynojirimycin and castanospermine Andrew Hempel, Norman Camerman, Donald Mastropaolo, and Arthur Camerman pp 4082 - 4086; DOI: 10.1021/jm00077a012 |
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Endothelin-1 analogues substituted at both position 18 and 19: highly potent endothelin antagonists with no selectivity for either receptor subtype ETA or ETB Takashi Kikuchi, Kazuki Kubo, Tetsuya Ohtaki, Nobuhiro Suzuki, Taiji Asami, Norio Shimamoto, Mitsuhiro Wakimasu, and Masahiko Fujino pp 4087 - 4093; DOI: 10.1021/jm00077a013 |
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Synthesis and structure-activity studies of a series of [(hydroxybenzyl)amino]salicylates as inhibitors of EGF receptor-associated tyrosine kinase activity Huixiong Chen, Janine Boiziau, Fabienne Parker, Rachid Maroun, Bruno Tocque, Bernard P. Roques, and Christiane Garbay-Jaureguiberry pp 4094 - 4098; DOI: 10.1021/jm00077a014 |
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Antipsoriatic anthrones with modulated redox properties. 1. Novel 10-substituted 1,8-dihydroxy-9(10H)-anthracenones as inhibitors of 5-lipoxygenase Klaus Mueller, Dieter Guerster, Susanne Piwek, and Wolfgang Wiegrebe pp 4099 - 4107; DOI: 10.1021/jm00077a015 |
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Design of antineoplastic agents on the basis of the 2-phenylnaphthalene-type structural pattern. 2. Synthesis and biological activity studies of benzo[b]naphtho[2,3-d]furan-6,11-dione derivatives C. C. Cheng, Qing Dong, Dun Fu Liu, Yi Lin Luo, Leroy F. Liu, Allan Y. Chen, Chiang Yu, Niramol Savaraj, and Ting Chao Chou pp 4108 - 4112; DOI: 10.1021/jm00077a016 |
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Synthesis and biological evaluation of N4-substituted imidazo- and v-triazolo[4,5-d]pyridazine nucleosides Jacqueline C. Bussolari, Kakarla Ramesh, Johanna D. Stoeckler, Shih Fong Chen, and Raymond P. Panzica pp 4113 - 4120; DOI: 10.1021/jm00077a017 |
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(1-Butyl-4-piperidinyl)methyl 8-amino-7-chloro-1,4-benzodioxane-5-carboxylate hydrochloride: a highly potent and selective 5-HT4 receptor antagonist derived from metoclopramide Laramie M. Gaster, Andrew J. Jennings, Graham F. Joiner, Frank D. King, Keith R. Mulholland, Shirley K. Rahman, Susannah Starr, Paul A. Wyman, Kay A. Wardle, and et al. pp 4121 - 4123; DOI: 10.1021/jm00077a018 |
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Book Reviews pp 4124 - 4129; DOI: 10.1021/jm00077a600 |
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Additions and Corrections - Structure-Activity Relationship Studies with Symmetric Naphthalenesulfonic Acid Derivatives. Synthesis and Influence of Spacer and Naphthalenesulfonic Acid Moiety on Anti-HIV-1 Activity. Prem Mohan, Man Fai Wong, Sandeep Verma, Peggy P. Huang, Anura Wickramasinghe, and Masamori Baba pp 4130 - 4130; DOI: 10.1021/jm00077a601 |
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Additions and Corrections - (E)-3-[[[[[6-(2-Carboxyethenyl)-5-[[8-(4-methoxyphenyl)octy-1]oxy]-2-pyridinyl]methyl]thio]methyl]benzoic Acid: A Novel High-Affinity Leukotriene B4 Receptor Antagonist. Robert A. Daines, Pamela A. Chambers, Israil Pendrak, Dalia R. Jakas, Henry M. Sarau, James J. Foley, Dulcie B. Schmidt, Don E. Griswold, Lenox D. Martin, Maritsa N. Tzimas, and William D. Kingsbury pp 4130 - 4130; DOI: 10.1021/jm00077a602 |
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The inophyllums, novel inhibitors of HIV-1 reverse transcriptase isolated from the Malaysian tree, Calophyllum inophyllum Linn Ashok D. Patil, Alan J. Freyer, Drake S. Eggleston, R. Curtis Haltiwanger, Mark F. Bean, Paul B. Taylor, Mary Jo Caranfa, Ann L. Breen, Henry R. Bartus, and et al. pp 4131 - 4138; DOI: 10.1021/jm00078a001 |
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Synthesis and antimicrobial evaluation of a series of 7-[3-amino (or aminomethyl)-4-aryl (or cyclopropyl)-1-pyrrolidinyl]-4-quinolone and -1,8-naphthyridone-3-carboxylic acids Ruth A. Bucsh, John M. Domagala, Edgardo Laborde, and Josephine C. Sesnie pp 4139 - 4151; DOI: 10.1021/jm00078a002 |
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Three-dimensional QSAR of human immunodeficiency virus (I) protease inhibitors. 1. A CoMFA study employing experimentally-determined alignment rules Chris L. Waller, Tudor I. Oprea, Alessandro Giolitti, and Garland R. Marshall pp 4152 - 4160; DOI: 10.1021/jm00078a003 |
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Studies on analogs of classical antifolates bearing the naphthoyl group in place of benzoyl in the side chain James R. Piper, Cheryl A. Johnson, Joseph A. Maddry, Neeta D. Malik, John J. McGuire, Glenys M. Otter, and Francis M. Sirotnak pp 4161 - 4171; DOI: 10.1021/jm00078a004 |
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CC-1065 functional analogs possessing different electron-withdrawing substituents and leaving groups: synthesis, kinetics, and sequence specificity of reaction with DNA and biological evaluation Yuqiang Wang, Rajan Gupta, Liren Huang, and J. William Lown pp 4172 - 4182; DOI: 10.1021/jm00078a005 |
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Nucleosides and nucleotides. 122. 2'-C-Cyano-2'-deoxy-1-.beta.-D-arabinofuranosylcytosine and its derivatives. A new class of nucleoside with a broad antitumor spectrum Atsushi Azuma, Yuki Nakajima, Naozumi Nishizono, Noriaki Minakawa, Masako Suzuki, Kenji Hanaoka, Tomowo Kobayashi, Motohiro Tanaka, Takuma Sasaki, and Akira Matsuda pp 4183 - 4189; DOI: 10.1021/jm00078a006 |
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Nucleosides and nucleotides. 123. Synthesis of 1-(2-deoxy-2-isocyano-.beta.-D-arabinofuranosyl)cytosine and related nucleosides as potential antitumor agents Akira Matsuda, Akihito Dan, Noriaki Minakawa, Scott James Tregear, Shinji Okazaki, Yoshikazu Sugimoto, and Takuma Sasaki pp 4190 - 4194; DOI: 10.1021/jm00078a007 |
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Synthesis and cytotoxicity of potential tumor-inhibitory analogs of trimelamol (2,4,6-tris[(hydroxymethyl)methylamino]-1,3,5-triazine) having electron-withdrawing groups in place of methyl Michael Jarman, Helen M. Coley, Ian R. Judson, Timothy J. Thornton, Derry E. V. Wilman, George Abel, and Christine J. Rutty pp 4195 - 4200; DOI: 10.1021/jm00078a008 |
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Brush-border-enzyme-mediated intestine-specific drug delivery. Amino acid prodrugs of 5-aminosalicylic acid Roberto Pellicciari, Aaron Garzon-Aburbeh, Benedetto Natalini, Maura Marinozzi, Carlo Clerici, Giorgio Gentili, and Antonio Morelli pp 4201 - 4207; DOI: 10.1021/jm00078a009 |
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Isocyanines and pseudoisocyanines as a novel class of potent noradrenaline-transport inhibitors: synthesis, detection, and biological activity Hermann Russ, Wolfram Engel, and Edgar Schoemig pp 4208 - 4213; DOI: 10.1021/jm00078a010 |
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Synthesis and pharmacological activity of a series of dihydro-1H-pyrrolo[1,2-a]imidazole-2,5(3H,6H)-diones, a novel class of potent cognition enhancers Mario Pinza, Carlo Farina, Alberto Cerri, Ugo Pfeiffer, Maria T. Riccaboni, Silvano Banfi, Raffaella Biagetti, Ottorino Pozzi, Maurizio Magnani, and Luciano Dorigotti pp 4214 - 4220; DOI: 10.1021/jm00078a011 |
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Derivatives of 2-(dipropylamino)tetralin: effect of the C8-substituent on the interaction with 5-HT1A receptors Ye Liu, Hong Yu, Bjoern E. Svensson, Lourdes Cortizo, Tommy Lewander, and Uli Hacksell pp 4221 - 4229; DOI: 10.1021/jm00078a012 |
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Non-peptide angiotensin II receptor antagonists. 1. Design, synthesis, and biological activity of N-substituted indoles and dihydroindoles 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 4230 - 4238; DOI: 10.1021/jm00078a013 |
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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 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 4239 - 4249; DOI: 10.1021/jm00078a014 |
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Phenylselenenyl- and phenylthio-substituted pyrimidines as inhibitors of dihydrouracil dehydrogenase and uridine phosphorylase Naganna M. Goudgaon, Fardos N. M. Naguib, Mahmoud H. el Kouni, and Raymond F. Schinazi pp 4250 - 4254; DOI: 10.1021/jm00078a015 |
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2- and 4-Fluorinated 16.alpha.-[125I]iodoestradiol derivatives: synthesis and effect on estrogen receptor binding and receptor-mediated target tissue uptake Hasrat Ali, Jacques Rousseau, Tsvetan G. Gantchev, and Johan E. van Lier pp 4255 - 4263; DOI: 10.1021/jm00078a016 |
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Structure-activity relationships of the antimalarial agent artemisinin. 1. Synthesis and comparative molecular field analysis of C-9 analogs of artemisinin and 10-deoxoartemisinin Mitchell A. Avery, Fenglan Gao, Wesley K. M. Chong, Sanjiv Mehrotra, and Wilbur K. Milhous pp 4264 - 4275; DOI: 10.1021/jm00078a017 |
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Development of 1,4-benzodiazepine cholecystokinin type B antagonists Mark G. Bock, Robert M. DiPardo, Ben E. Evans, Kenneth E. Rittle, Willie L. Whitter, Victor M. Garsky, Kevin F. Gilbert, James L. Leighton, Kenneth L. Carson, and et al. pp 4276 - 4292; DOI: 10.1021/jm00078a018 |
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Inhibition of matrix metalloproteinases by N-carboxyalkyl peptides Kevin T. Chapman, Ihor E. Kopka, Philippe L. Durette, Craig K. Esser, Thomas J. Lanza, Maria Izquierdo-Martin, Lisa Niedzwiecki, Benedict Chang, Richard K. Harrison, and et al. pp 4293 - 4301; DOI: 10.1021/jm00078a019 |
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Studies of the synthesis, immunology, and cytotoxicity of a cyclic octapeptide corresponding to TNF-.alpha.-(59-66) Leung Sheh, Hsou Hung Lin, Kee Ching G. Jeng, and Chia Fu Chen pp 4302 - 4307; DOI: 10.1021/jm00078a020 |
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Synthesis and optical resolution of (R)- and (S)-trans-7-hydroxy-2-[N-propyl-N-(3'-iodo-2'-propenyl)amino]tetralin: a new D3 dopamine receptor ligand Sumalee Chumpradit, Mei Ping Kung, and Hank F. Kung pp 4308 - 4312; DOI: 10.1021/jm00078a021 |
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6-Azasteroids: potent dual inhibitors of human type 1 and 2 steroid 5.alpha.-reductase Stephen V. Frye, Curt D. Haffner, Patrick R. Maloney, Robert A. Mook Jr., G. F. Dorsey Jr., Roger N. Hiner, Kenneth W. Batchelor, H. Neal Bramson, J. Darren Stuart, and et al. pp 4313 - 4315; DOI: 10.1021/jm00078a022 |