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Rational design of enzyme inhibitors: multisubstrate analog inhibitors Arthur D. Broom pp 2 - 7; DOI: 10.1021/jm00121a001 |
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N6-Bicycloalkyladenosines with unusually high potency and selectivity for the adenosine A1 receptor B. K. Trivedi, A. J. Bridges, W. C. Patt, S. R. Priebe, and R. F. Bruns pp 8 - 11; DOI: 10.1021/jm00121a002 |
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Perfluoro-N-[4-(1H-tetrazol-5-ylmethyl)phenyl]alkanamides. A new class of oral antidiabetic agents Kenneth L. Kees, Robert S. Cheeseman, Dorothy H. Prozialeck, and Kurt E. Steiner pp 11 - 13; DOI: 10.1021/jm00121a003 |
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Benzodiazepine gastrin and brain cholecystokinin receptor ligands; L-365,260 Mark G. Bock, Robert M. DiPardo, Ben E. Evans, Kenneth E. Rittle, Willie L. Whitter, Daniel F. Veber, Paul S. Anderson, and Roger M. Freidinger pp 13 - 16; DOI: 10.1021/jm00121a004 |
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Rationale for the synthesis and preliminary biological evaluation of highly active new antitumor nitrosoureido sugars Pierre Roger, Claude Monneret, Jean Paul Fournier, Patrick Choay, Roselyne Gagnet, Charles Gosse, Yves Letourneux, Ghanem Atassi, and Alain Gouyette pp 16 - 23; DOI: 10.1021/jm00121a005 |
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Hypoxia-selective antitumor agents. 1. Relationships between structure, redox properties and hypoxia-selective cytotoxicity for 4-substituted derivatives of nitracrine William R. Wilson, Robert F. Anderson, and William A. Denny pp 23 - 30; DOI: 10.1021/jm00121a006 |
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Hypoxia-selective antitumor agents. 2. Electronic effects of 4-substituents on the mechanisms of cytotoxicity and metabolic stability of nitracrine derivatives William R. Wilson, Larry H. Thompson, Robert F. Anderson, and William A. Denny pp 31 - 38; DOI: 10.1021/jm00121a007 |
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Stereoelectronic study of zetidoline, a dopamine D2 receptor antagonist Sonia Collin, Guy Evrard, Daniel P. Vercauteren, Francois Durant, Pierre Alain Carrupt, Han Van de Waterbeemd, and Bernard Testa pp 38 - 42; DOI: 10.1021/jm00121a008 |
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5-Isoquinolinesulfonamide derivatives. 1. Synthesis and vasodilatory activity of N-(2-guanidinoethyl)-5-isoquinolinesulfonamide derivatives Anri Morikawa, Takanori Sone, and Toshio Asano pp 42 - 46; DOI: 10.1021/jm00121a009 |
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5-Isoquinolinesulfonamide derivatives. 2. Synthesis and vasodilatory activity of N-(2-aminoethyl)-5-isoquinoline sulfonamide derivatives Anri Morikawa, Takanori Sone, and Toshio Asano pp 46 - 50; DOI: 10.1021/jm00121a010 |
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Structure-activity relationships in prazosin-related compounds. Effect of replacing a piperazine ring with an alkanediamine moiety on .alpha.1-adrenoreceptor blocking activity Dario Giardina, Livio Brasili, Maurizio Gregori, Maurizio Massi, Maria T. Picchio, Wilma Quaglia, and Carlo Melchiorre pp 50 - 55; DOI: 10.1021/jm00121a011 |
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Platelet activating factor (PAF) antagonists: synthesis and structure-activity studies of novel PAF analogs modified in the phosphorylcholine moiety Muneo Takatani, Yoshio Yoshioka, Akihiro Tasaka, Zenichi Terashita, Yoshimi Imura, Kohei Nishikawa, and Susumu Tsushima pp 56 - 64; DOI: 10.1021/jm00121a012 |
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Amine peroxides as potential antimalarials Jonathan L. Vennerstrom pp 64 - 67; DOI: 10.1021/jm00121a013 |
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Conformationally restricted analogs of atriopeptin(103-125) amide Kerry L. Spear, Emily J. Reinhard, Ellen G. McMahon, Gillian M. Olins, Maria A. Palomo, and Dennis R. Patton pp 67 - 72; DOI: 10.1021/jm00121a014 |
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Acyclic analogs of 3'-azido-3'-deoxythymidine as potential antiviral agents. Nucleoside synthesis by Michael addition Peter Scheiner, Aloma Geer, Ann Marie Bucknor, Jean Louis Imbach, and Raymond F. Schinazi pp 73 - 76; DOI: 10.1021/jm00121a015 |
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1',2'-seco-Dideoxynucleosides as potential anti-HIV agents Elie Abushanab and Mallela S. P. Sarma pp 76 - 79; DOI: 10.1021/jm00121a016 |
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Structure-activity relationships among methoctramine-related polymethylenetetramines. Chain length and substituent effects on M-2 muscarinic receptor blocking activity Carlo Melchiorre, Wilma Quaglia, Maria T. Picchio, Dario Giardina, Livio Brasili, and Piero Angeli pp 79 - 84; DOI: 10.1021/jm00121a017 |
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Inhibition of iodine-125 labeled ristocetin binding to Micrococcus luteus cells by the peptides related to bacterial cell wall mucopeptide precursors: quantitative structure-activity relationships Ki-Hwan Kim, Yvonne Martin, Ellen Otis, and James Mao pp 84 - 93; DOI: 10.1021/jm00121a018 |
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Synthesis and anticonvulsant properties of 2,3,3a,4-tetrahydro-1H-pyrrolo[1,2-a]benzimidazol-1-ones Alba Chimirri, Angelina De Sarro, Giovambattista De Sarro, Silvana Grasso, Giuseppe R. Trimarchi, and Maria Zappala pp 93 - 95; DOI: 10.1021/jm00121a019 |
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Alkylating prazosin analog: irreversible label for .alpha.1-adrenoceptors Josef Pitha, Lajos Szabo, Zoltan Szurmai, Wieslaw Buchowiecki, and John W. Kusiak pp 96 - 100; DOI: 10.1021/jm00121a020 |
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Antiinflammatory 2,6-di-tert-butyl-4-(2-arylethenyl)phenols Edward S. Lazer, Hin Chor Wong, Genus J. Possanza, Anne G. Graham, and Peter R. Farina pp 100 - 104; DOI: 10.1021/jm00121a021 |
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Synthesis and antiallergy activity of 4-(diarylhydroxymethyl)-1-[3-(aryloxy)propyl)piperidines and structurally related compounds David A. Walsh, Stephen K. Franzyshen, and John M. Yanni pp 105 - 118; DOI: 10.1021/jm00121a022 |
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Design, synthesis, antineoplastic activity, and chemical properties of bis(carbamate) derivatives of 4,5-bis(hydroxymethyl)imidazole Wayne K. Anderson, Debkumar Bhattacharjee, and D. Michael Houston pp 119 - 127; DOI: 10.1021/jm00121a023 |
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Chemical and biological properties of a new series of cis-diammineplatinum(II) antitumor agents containing three nitrogen donors: cis-[Pt(NH3)2(N-donor) Cl]+ L. Steven Hollis, Alan R. Amundsen, and Eric W. Stern pp 128 - 136; DOI: 10.1021/jm00121a024 |
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Studies on antitumor agents. 8. Antitumor activities of O-alkyl derivatives of 2'-deoxy-5-(trifluoromethyl)uridine and 2'-deoxy-5-fluorouridine Junichi Yamashita, Mitsugi Yasumoto, Setsuo Takeda, Hiroshi Matsumoto, and Norio Unemi pp 136 - 139; DOI: 10.1021/jm00121a025 |
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Development of phosphonate derivatives of gadolinium chelates for NMR imaging of calcified soft tissues I. Kofi Adzamli, H. Gries, D. Johnson, and M. Blau pp 139 - 144; DOI: 10.1021/jm00121a026 |
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N- and 2-substituted N-(phenylsulfonyl)glycines as inhibitors of rat lens aldose reductase Jack DeRuiter, Ronald F. Borne, and Charles A. Mayfield pp 145 - 151; DOI: 10.1021/jm00121a027 |
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Synthesis and activity of nonhydrolyzable pseudomonic acid analogs Larry L. Klein, Clinton M. Yeung, Paul Kurath, James C. Mao, Prabhavathi B. Fernandes, Paul A. Lartey, and Andre G. Pernet pp 151 - 160; DOI: 10.1021/jm00121a028 |
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Quinazoline antifolates inhibiting thymidylate synthase: synthesis of four oligo(L-.gamma.-glutamyl) conjugates of N10-propargyl-5,8-dideazafolic acid and their enzyme inhibition Krzysztof Pawelczak, Terence R. Jones, Michal Kempny, Ann L. Jackman, David R. Newell, Leszek Krzyzanowski, and Barbara Rzeszotarska pp 160 - 165; DOI: 10.1021/jm00121a029 |
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Synthesis of an analog of tabtoxinine as a potential inhibitor of D-alanine:D-alanine ligase (ADP forming) William J. Greenlee, James P. Springer, and Arthur A. Patchett pp 165 - 170; DOI: 10.1021/jm00121a030 |
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2,2-Difluoro-5-hexyne-1,4-diamine. A potent enzyme-activated inhibitor of ornithine decarboxylase David A. Kendrick, Charles Danzin, and Michael Kolb pp 170 - 173; DOI: 10.1021/jm00121a031 |
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Design of potent linear .alpha.-melanotropin 4-10-analogs modified in positions 5 and 10 Fahad Al-Obeidi, Victor J. Hruby, Ana M. de L. Castrucci, and Mac E. Hadley pp 174 - 179; DOI: 10.1021/jm00121a032 |
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Synthesis and .alpha.2-adrenoceptor antagonist activity of some disulfonamidobenzoquinolizines Terence J. Ward, Graham J. Warrellow, John A. Stirrup, Norman Lattimer, and Keith F. Rhodes pp 179 - 182; DOI: 10.1021/jm00121a033 |
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Flavones. 2. Synthesis and structure-activity relationship of flavodilol and its analogs. A novel class of antihypertensive agents with catecholamine depleting properties E. S. C. Wu, T. E. Cole, T. A. Davidson, M. A. Dailey, K. G. Doring, M. Fedorchuk, J. T. Loch, III, T. L. Thomas, J. C. Blosser, and et al. pp 183 - 192; DOI: 10.1021/jm00121a034 |
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Phenolic metabolites of clomiphene. [(E,Z)-2-[4-(1,2-diphenyl-2-chlorovinyl)phenoxy]ethyl]diethylamine. Preparation, electrophilicity, and effects in MCF 7 breast cancer cells Peter C. Ruenitz, Richard F. Arrendale, Walter F. Schmidt, Carolyn B. Thompson, and Nitin T. Nanavati pp 192 - 197; DOI: 10.1021/jm00121a035 |
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Synthesis and biological evaluation of a monocyclic, fully functional analog of compactin Clayton H. Heathcock, Brian R. Davis, and Cheri R. Hadley pp 197 - 202; DOI: 10.1021/jm00121a036 |
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Interactions of thiol-containing androgens with human placental aromatase Patrick J. Bednarski and Sidney D. Nelson pp 203 - 213; DOI: 10.1021/jm00121a037 |
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Synthesis and P-388 antitumor properties of the four diastereomeric dichloro 1-hydroxy-3,4-diaminocyclohexane-platinum(II) complexes Donald T. Witiak, David P. Rotella, Yong Wei, Joyce A. Filppi, and Judith C. Gallucci pp 214 - 217; DOI: 10.1021/jm00121a038 |
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Synthesis and structure-activity relationships of 2-substituted-6-(dimethylamino)-9-(4-methylbenzyl)-9H-purines with antirhinovirus activity James L. Kelley, James A. Linn, and J. W. T. Selway pp 218 - 224; DOI: 10.1021/jm00121a039 |
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Synthesis and cystostatic and antiviral activities of 1-.beta.-D-ribofuranosyl-5-alkylcytosine (5-alkylcytidine) cyclic 3',5'-monophosphates Jozsef Beres, Wesley G. Bentrude, Laszlo Otvos, Jan Balzarini, and Erik De Clercq pp 224 - 228; DOI: 10.1021/jm00121a040 |
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Synthesis of acylguanidine analogs: inhibitors of ADP-induced platelet aggregation Edward W. Thomas, Edward E. Nishizawa, David C. Zimmermann, and Davey J. Williams pp 228 - 236; DOI: 10.1021/jm00121a041 |
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Synthesis of novel bifunctional chelators and their use in preparing monoclonal antibody conjugates for tumor targeting David A. Westerberg, Patrick L. Carney, Patrick E. Rogers, Steven J. Kline, and David K. Johnson pp 236 - 243; DOI: 10.1021/jm00121a042 |
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2-O-Alkyltyrosine derivatives of 1-deaminoarginine-vasopressin: highly specific and potent antidiuretic agonists Bernard Lammek, Kryzsztof Bankowski, Aleksandra Misicka, Maurice Manning, J. Seto, and W. H. Sawyer pp 244 - 247; DOI: 10.1021/jm00121a043 |
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Mitomycin C analogs with a substituted hydrazine at position 7. Synthesis, spectral properties, and biological activity Kailash N. Sawhney and Harold Kohn pp 248 - 252; DOI: 10.1021/jm00121a044 |
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2-(Alkylamino)tetralin derivatives: interaction with 5-HT1A serotonin binding sites Noreen Naiman, Robert A. Lyon, Amy E. Bullock, Laura T. Rydelek, Milt Titeler, and Richard A. Glennon pp 253 - 256; DOI: 10.1021/jm00121a045 |
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Prostaglandin photoaffinity probes: synthesis and biological activity of azide-substituted 16-phenoxy- and 17-phenyl-PGF2.alpha. prostaglandins Kenji Kawada, E. Kurt Dolence, Hiroyuki Morita, Tadashi Kometani, David S. Watt, Anil Balapure, Tony A. Fitz, David J. Orlicky, and L. E. Gerschenson pp 256 - 264; DOI: 10.1021/jm00121a046 |
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Hypolipidemic 2-[4-(1,1-dimethylethyl)phenyl]-4H-3,1-benzoxazin-4-ones. Structure-activity relationships of a novel series of high-density lipoprotein elevators Garry Fenton, Christopher G. Newton, Barry M. Wyman, Philip Bagge, Donald I. Dron, David Riddell, and Graham D. Jones pp 265 - 272; DOI: 10.1021/jm00121a047 |
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Editorial - Medicinal Chemistry 1969 and Beyond Philip S. Portoghese pp 1 - 1; DOI: 10.1021/jm00121a600 |
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Book Reviews pp 273 - 280; DOI: 10.1021/jm00121a601 |
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Selective and enantiospecific acylation of .kappa.-opioid receptors by (1S,2S)-trans-2-isothiocyanato-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]benzeneacetamide. Demonstration of .kappa. receptor heterogeneity Brian R. De Costa, Richard B. Rothman, Victor Bykov, Arthur E. Jacobson, and Kenner C. Rice pp 281 - 283; DOI: 10.1021/jm00122a001 |
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Synthesis and cytostatic activity of geiparvarin analogs Pier Giovanni Baraldi, M. Guarneri, S. Manfredini, D. Simoni, J. Balzarini, and E. De Clercq pp 284 - 288; DOI: 10.1021/jm00122a002 |
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Studies on angiotensin converting enzyme inhibitors. 4. Synthesis and angiotensin converting enzyme inhibitory activities of 3-acyl-1-alkyl-2-oxoimidazolidine-4-carboxylic acid derivatives Kimiaki Hayashi, Kenichi Nunami, Jyoji Kato, Naoto Yoneda, Masami Kubo, Takashi Ochiai, and Ryuichi Ishida pp 289 - 297; DOI: 10.1021/jm00122a003 |
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Synthesis and radioprotective activity of dipeptide cysteamine and cystamine derivatives Joel Oiry, Jean Y. Pue, Jean L. Imbach, Marc Fatome, and Henry Sentenac-Roumanou pp 297 - 301; DOI: 10.1021/jm00122a004 |
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Cyclic enkephalin analog containing .alpha.-amino-.beta.-mercapto-.beta.,.beta.-pentamethylenepropionic acid at position 2 or 5 William M. Bryan, James F. Callahan, Ellen E. Codd, Carole Lemieux, Michael L. Moore, Peter W. Schiller, Richard F. Walker, and William F. Huffman pp 302 - 304; DOI: 10.1021/jm00122a005 |
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Carbamyl analogs of potent, nicotinic agonists: pharmacology and computer-assisted molecular modeling study Charles E. Spivak, Janardan S. Yadav, Wen Cheung Shang, Mark Hermsmeier, and Tamara M. Gund pp 305 - 309; DOI: 10.1021/jm00122a006 |
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Deaminoteicoplanin and its derivatives. Synthesis, antibacterial activity, and binding strength to Ac-D-Ala-D-Ala Aldo Trani, Pietro Ferrari, Rosa Pallanza, and Giorgio Tarzia pp 310 - 314; DOI: 10.1021/jm00122a007 |
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A new series of tricyclic (aryloximino)propanolamines displaying very high selective .beta.2-blocking properties Brigitte Jamart-Gregoire, Paul Caubere, Marie Blanc, Jean Pierre Gnassounou, and Charles Advenier pp 315 - 320; DOI: 10.1021/jm00122a008 |
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Selective thyromimetics. Cardiac-sparing thyroid hormone analogs containing 3'-arylmethyl substituents Paul D. Leeson, John C. Emmett, Virendra P. Shah, Graham A. Showell, Ricardo Novelli, H. Douglas Prain, Martin G. Benson, David Ellis, Nigel J. Pearce, and Anthony H. Underwood pp 320 - 336; DOI: 10.1021/jm00122a009 |
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Bifunctional antitumor compounds. Interaction of adriamycin with metallocene dichlorides A. Moustatih, M. M. L. Fiallo, and A. Garnier-Suillerot pp 336 - 342; DOI: 10.1021/jm00122a010 |
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Cardiotonic agents. 9. Synthesis and biological evaluation of a series of (E)-4,5-dihydro-6-[2-[4-(1H-imidazol-1-yl)phenyl]ethenyl]-3(2H)-pyridazinones: a novel class of compounds with positive inotropic, antithrombotic, and vasodilatory activities for the treatment of congestive heart failure I. Sircar, R. P. Steffen, G. Bobowski, S. E. Burke, R. S. Newton, R. E. Weishaar, J. A. Bristol, and D. B. Evans pp 342 - 350; DOI: 10.1021/jm00122a011 |
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Cardiotonic agents. 1-Methyl-7-(4-pyridyl)-5,6,7,8-tetrahydro-3(2H)-isoquinolinones and related compounds. Synthesis and activity Tatsuo Kaiho, Kunio Sannohe, Seitaro Kajiya, Tsuneji Suzuki, Kengo Otsuka, Toshihiko Ito, Joji Kamiya, and Masahiko Maruyama pp 351 - 357; DOI: 10.1021/jm00122a012 |
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Spermexatin and spermexatol: new synthetic spermidine-based siderophore analogs Sushil K. Sharma, Marvin J. Miller, and Shelley M. Payne pp 357 - 367; DOI: 10.1021/jm00122a013 |
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Synthesis and antiviral activity of phosphonoacetic and phosphonoformic acid esters of 5-bromo-2'-deoxyuridine and related pyrimidine nucleosides and acyclonucleosides Robert W. Lambert, Joseph A. Martin, Gareth J. Thomas, Ian B. Duncan, Michael J. Hall, and Edgar P. Heimer pp 367 - 374; DOI: 10.1021/jm00122a014 |
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Syntheses and biological activities of 13-substituted avermectin aglycons Helmut Mrozik, Bruce O. Linn, Philip Eskola, Aino Lusi, Alexander Matzuk, Franz A. Preiser, Dan A. Ostlind, James M. Schaeffer, and Michael H. Fisher pp 375 - 381; DOI: 10.1021/jm00122a015 |
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Solid-phase synthesis of 16 potent (selective and nonselective) in vivo antagonists of oxytocin Maurice Manning, Marian Kruszynski, Krzysztof Bankowski, Aleksandra Olma, Bernard Lammek, Ling Ling Cheng, Wieslaw A. Klis, Janny Seto, Jaya Haldar, and Wilbur H. Sawyer pp 382 - 391; DOI: 10.1021/jm00122a016 |
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Structure-activity relationships of novel vasopressin antagonists containing C-terminal diaminoalkanes and (aminoalkyl)guanidines James F. Callahan, Daryl Ashton-Shue, Heidemarie G. Bryan, William M. Bryan, Grace D. Heckman, Lewis B. Kinter, Jeanne E. McDonald, Michael L. Moore, Dulcie B. Schmidt, and et al. pp 391 - 396; DOI: 10.1021/jm00122a017 |
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Potential antitumor agents. 57. 2-Phenylquinoline-8-carboxamides as minimal DNA-intercalating antitumor agents with in vivo solid tumor activity Graham J. Atwell, Bruce C. Baguley, and William A. Denny pp 396 - 401; DOI: 10.1021/jm00122a018 |
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Synthesis, cytotoxicity, and antiviral activity of some acyclic analogs of the pyrrolo[2,3-d]pyrimidine nucleoside antibiotics tubercidin, toyocamycin, and sangivamycin Pranab K. Gupta, Sylvia Daunert, M. Reza Nassiri, Linda L. Wotring, John C. Drach, and Leroy B. Townsend pp 402 - 408; DOI: 10.1021/jm00122a019 |
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Synthesis, tubulin binding, antineoplastic evaluation, and structure-activity relationship of oncodazole analogs Lawrence I. Kruse, David L. Ladd, Peter B. Harrsch, Francis L. McCabe, Shau Ming Mong, Leo Faucette, and Randall Johnson pp 409 - 417; DOI: 10.1021/jm00122a020 |
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Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(Cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective .mu. opioid receptor antagonist Helmut Schmidhammer, Willy P. Burkard, Lislott Eggstein-Aeppli, and Colin F. C. Smith pp 418 - 421; DOI: 10.1021/jm00122a021 |
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Studies on hindered phenols and analogs. 1. Hypolipidemic and hypoglycemic agents with ability to inhibit lipid peroxidation Takao Yoshioka, Takashi Fujita, Tsutomu Kanai, Yuichi Aizawa, Tomoyuki Kurumada, Kazuo Hasegawa, and Hiroyoshi Horikoshi pp 421 - 428; DOI: 10.1021/jm00122a022 |
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Studies on bioactive compounds. 13. Synthesis and lack of growth-inhibitory properties of cyclohexane-1,2,4-triol 1,2-diesters, which resemble ring C of the phorbol ester molecule C. A. Laughton, I. L. Dale, and A. Gescher pp 428 - 433; DOI: 10.1021/jm00122a023 |
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New brain perfusion imaging agents based on technetium-99m bis(aminoethanethiol) complexes: stereoisomers and biodistribution Hank F. Kung, Yu Zhi Guo, Chi Chou Yu, Jeffrey Billings, Vinayakam Subramanyam, and Joseph C. Calabrese pp 433 - 437; DOI: 10.1021/jm00122a024 |
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A novel class of "GABAergic" agents: 1-aryl-3-(aminoalkylidene)oxindoles Reinhard Sarges, Harry R. Howard, B. Kenneth Koe, and Albert Weissman pp 437 - 444; DOI: 10.1021/jm00122a025 |
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Full agonists of CCK8 containing a nonhydrolyzable sulfated tyrosine residue I. Marseigne, P. Roy, A. Dor, C. Durieux, D. Pelaprat, M. Reibaud, J. C. Blanchard, and B. P. Roques pp 445 - 449; DOI: 10.1021/jm00122a026 |
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Synthesis and structure-activity studies of some disubstituted phenylisoxazoles against human picornavirus Guy D. Diana, David Cutcliffe, Richard C. Oglesby, Michael J. Otto, John P. Mallamo, Vahan Akullian, and Mark A. McKinlay pp 450 - 455; DOI: 10.1021/jm00122a027 |
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Synthesis and evaluation of antileukemic activity of 5-thienyl- or 5-(2-furyl)-2,3-dihydro-6,7-bis(hydroxymethyl)-1H-pyrrolizine bis(alkylcarbamates) and derivatives Daniel Laduree, Jean Charles Lancelot, Max Robba, E. Chenu, and G. Mathe pp 456 - 461; DOI: 10.1021/jm00122a028 |
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1-(2,3-Dideoxy-.beta.-D-glycero-pent-2-enofuranosyl)thymine. A highly potent and selective anti-HIV agent Muzammil M. Mansuri, John E. Starrett Jr., Ismail Ghazzouli, Michael J. M. Hitchcock, Roman Z. Sterzycki, Vera Brankovan, Tai Shun Lin, E. Michael August, William H. Prusoff, and et al. pp 461 - 466; DOI: 10.1021/jm00122a029 |
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Potent angiotensin II antagonists with non-.beta.-branched amino acids in position 5 J. Samanen, D. Narindray, T. Cash, E. Brandeis, W. Adams, T. Yellin, D. Eggleston, C. DeBrosse, and D. Regoli pp 466 - 472; DOI: 10.1021/jm00122a030 |
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Studies on semirigid tricyclic analogs of the nigrostriatal toxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine Raymond G. Booth, Anthony Trevor, Thomas P. Singer, and Neal Castagnoli pp 473 - 477; DOI: 10.1021/jm00122a031 |
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Conformationally defined adrenergic agents. 15. Conformationally restricted and conformationally defined tyramine analogs as inhibitors of phenylethanolamine N-methyltransferase Qizhuang Ye and Gary L. Grunewald pp 478 - 486; DOI: 10.1021/jm00122a032 |
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Synthesis and copper-dependent antimycoplasmal activity of 1-amino-3-(2-pyridyl)isoquinoline derivatives. 2. Amidines Marcel A. H. De Zwart, Henk Van der Goot, and Henk Timmerman pp 487 - 493; DOI: 10.1021/jm00122a033 |
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Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 2. Preparation and in vitro and in vivo evaluaton of 1-(alkoxymethyl)-2-[(hydroxyimino)methyl]-3-methylimidazolium halides for reactivation of organophosphorus-inhibited acetylcholinesterases Clifford D. Bedford, Ralph N. Harris, III, Robert A. Howd, Dane A. Goff, Gary A. Koolpe, M. Petesch, Alexi Miller, Harold W. Nolen, III, H. A. Musallam, and et al. pp 493 - 503; DOI: 10.1021/jm00122a034 |
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Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 3. Synthesis and evaluation of (alkenyloxy)-, (alkynyloxy)-, and (aralykyloxy)methyl quaternarized 2-[(hydroxyimino)methyl]-1-alkylimidazolium halides as reactivators and therapy for soman intoxication Clifford D. Bedford, Ralph N. Harris, Robert A. Howd, Dane A. Goff, Gary A. Koolpe, M. Petesch, Irwin Koplovitz, Walter E. Sultan, and H. A. Musallam pp 504 - 516; DOI: 10.1021/jm00122a035 |
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The 2-desamino and 2-desamino-2-methyl analogs of aminopterin do not inhibit dihydrofolate reductase but are potently toxic to tumor cells in culture Andre Rosowsky, Ronald A. Forsch, James H. Freisheim, and Richard G. Moran pp 517 - 520; DOI: 10.1021/jm00123a001 |
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A carboxy-terminus truncated analog of angiotensin II, [Sar1]angiotensin II-(1-7)-amide, provides an entry to a new class of angiotensin II antagonists P. R. Bovy, A. J. Trapani, E. G. McMahon, and M. Palomo pp 520 - 522; DOI: 10.1021/jm00123a002 |
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Synthesis of gastrin antagonists, analogs of the C-terminal tetrapeptide of gastrin, by introduction of a .beta.-homo residue M. Rodriguez, P. Fulcrand, J. Laur, A. Aumelas, J. P. Bali, and Jean Martinez pp 522 - 528; DOI: 10.1021/jm00123a003 |
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3-Aminopyridazine derivatives with atypical antidepressant, serotonergic and dopaminergic activities Camille Georges Wermuth, Gilbert Schlewer, Jean Jacques Bourguignon, Georges Maghioros, Marie Jeanne Bouchet, Claudine Moire, Jean Paul Kan, Paul Worms, and Kathleen Biziere pp 528 - 537; DOI: 10.1021/jm00123a004 |
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Fluoronaphthyridines and quinolones as antibacterial agents. 1. Synthesis and structure-activity relationship of new 1-substituted derivatives D. Bouzard, P. Di Cesare, M. Essiz, J. P. Jacquet, P. Remuzon, A. Weber, T. Oki, and M. Masuyoshi pp 537 - 542; DOI: 10.1021/jm00123a005 |
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Preparation and biodistribution of 1-[2-(3-[125I]iodo-4-aminophenyl)ethyl]-4-[3-(trifluoromethyl)phenyl]piperazine and 1-[2-(3-[125I]iodo-4-azidophenyl)ethyl]-4-[3-(trifluoromethyl)phenyl]piperazine Sumalee Chumpradit, Hank F. Kung, Jeffrey Billings, Yu Zhi Guo, Yang Wu, and Jean Shih pp 543 - 547; DOI: 10.1021/jm00123a006 |
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New antitumor monoclonal antibody-vinca conjugates LY203725 and related compounds: design, preparation, and representative in vivo activity Bennett C. Laguzza, Cynthia L. Nichols, Stephen L. Briggs, George J. Cullinan, David A. Johnson, James J. Starling, A. Leroy Baker, Thomas F. Bumol, and Jose R. F. Corvalan pp 548 - 555; DOI: 10.1021/jm00123a007 |
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Structure-activity studies of trichothecenes: cytotoxicity of analogs and reaction products derived from T-2 toxin and neosolaniol D. W. Anderson, R. M. Black, C. G. Lee, C. Pottage, R. L. Rickard, M. S. Sandford, T. D. Webber, and N. E. Williams pp 555 - 562; DOI: 10.1021/jm00123a008 |
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Long acting dihydropyridine calcium antagonists. 2. 2-[2-aminoheterocycloethoxy]methyl derivatives John E. Arrowsmith, Simon F. Campbell, Peter E. Cross, Roger A. Burges, and Donald G. Gardiner pp 562 - 568; DOI: 10.1021/jm00123a009 |
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Quinazoline antifolate thymidylate synthase inhibitors: nitrogen, oxygen, sulfur, and chlorine substituents in the C2 position Peter R. Marsham, Paula Chambers, Anthony J. Hayter, Leslie R. Hughes, Ann L. Jackman, Breda M. O'Connor, Joel A. M. Bishop, and A. Hilary Calvert pp 569 - 575; DOI: 10.1021/jm00123a010 |
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2(1H)-Quinolinones with cardiac stimulant activity. 2. Synthesis and biological activities of 6-(N-linked, five-membered heteroaryl) derivatives Colin T. Alabaster, Andrew S. Bell, Simon F. Campbell, Peter Ellis, Christopher G. Henderson, David S. Morris, David A. Roberts, Keith S. Ruddock, Gillian M. R. Samuels, and Mark H. Stefaniak pp 575 - 583; DOI: 10.1021/jm00123a011 |
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Acrylamide derivatives as antiallergic agents. 2. Synthesis and structure activity relationships of N-[4-[4-(diphenylmethyl)-1-piperazinyl]butyl]-3-(3-pyridyl)acrylamides Yoshinori Nishikawa, Tokuhiko Shindo, Katsumi Ishii, Hideo Nakamura, Tatsuya Kon, and Hitoshi Uno pp 583 - 593; DOI: 10.1021/jm00123a012 |
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5-(1-Piperazinyl)-1H-1,2,4-triazol-3-amines as antihypertensive agents Walter E. Meyer, Andrew S. Tomcufcik, Peter S. Chan, and Margie Haug pp 593 - 597; DOI: 10.1021/jm00123a013 |
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Synthesis and hypertensive activity of neuropeptide Y fragments and analogs with modified N- or C-termini or D-substitutions J. H. Boublik, N. A. Scott, M. R. Brown, and J. E. Rivier pp 597 - 601; DOI: 10.1021/jm00123a014 |
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Synthesis and in vitro activity of 1.beta.-methyl C-2 quaternary heterocyclic alkylthio carbapenems Choung Un Kim, Bing Y. Luh, Peter F. Misco, and Michael J. M. Hitchcock pp 601 - 604; DOI: 10.1021/jm00123a015 |
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Antitumor agents. 100. Inhibition of human DNA topoisomerase II by cytotoxic ether and ester derivatives of podophyllotoxin and .alpha.-peltatin Lee S. Thurston, Yasuhiro Imakura, Mitsumasa Haruna, De Hua Li, Zong Chao Liu, Su Ying Liu, Yung Chi Cheng, and Kuo Hsiung Lee pp 604 - 608; DOI: 10.1021/jm00123a016 |
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Potential tumor- or organ-imaging agents. 29. Radioiodinated esters and amides of 20-hydroxy- and 20-aminopregn-5-en-3.beta.-ols T. Haradahira, S. W. Schwendner, M. Kojima, and Raymond E. Counsell pp 609 - 612; DOI: 10.1021/jm00123a017 |
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Structure-activity relationships of pyrimidine nucleosides as antiviral agents for human immunodeficiency virus type 1 in peripheral blood mononuclear cells Chung K. Chu, Raymond F. Schinazi, Moon K. Ahn, Giliyar V. Ullas, and Zi P. Gu pp 612 - 617; DOI: 10.1021/jm00123a018 |
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1-(3-Cyano-2,3-dideoxy-.beta.-D-erythro-pentofuranosyl)thymine (cyanothymidine): synthesis and antiviral evaluation against human immunodeficiency virus Colin W. Greengrass, David W. T. Hoople, Stephen D. A. Street, Fiona Hamilton, Michael S. Marriott, Jon Bordner, Angus G. Dalgleish, Hiroaki Mitsuya, and Samuel Broder pp 618 - 622; DOI: 10.1021/jm00123a019 |
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A dihydropyridine carrier system for sustained delivery of 2',3'-dideoxynucleosides to the brain Eduardo Palomino, David Kessel, and Jerome P. Horwitz pp 622 - 625; DOI: 10.1021/jm00123a020 |
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A novel prodrug of an impermeant inhibitor of 3-deoxy-D-manno-2-octulosonate cytidylyltransferase has antibacterial activity Daniel W. Norbeck, William Rosenbrook, James B. Kramer, David J. Grampovnik, and Paul A. Lartey pp 625 - 629; DOI: 10.1021/jm00123a021 |
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Antitumor and antiviral activity of synthetic .alpha.- and .beta.-ribonucleosides of certain substituted pyrimido[5,4-d]pyrimidines: a new synthetic strategy for exocyclic aminonucleosides Yogesh S. Sanghvi, Steven B. Larson, Steven S. Matsumoto, L. Dee Nord, Donald F. Smee, Randall C. Willis, Thomas L. Avery, Roland K. Robins, and Ganapathi R. Revankar pp 629 - 637; DOI: 10.1021/jm00123a022 |
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Synthesis of highly .mu. and .delta. opioid receptor-selective peptides containing a photoaffinity group Geoffrey Landis, George Lui, Jennifer E. Shook, Henry I. Yamamura, Thomas F. Burks, and Victor J. Hruby pp 638 - 643; DOI: 10.1021/jm00123a023 |
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Synthesis and evaluation of iodinated analogs of diacylglycerols as potential probes for protein kinase C Laurie M. Strawn, Robert E. Martell, Robert U. Simpson, Karen L. Leach, and Raymond E. Counsell pp 643 - 648; DOI: 10.1021/jm00123a024 |
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Crystallographic resolution and crystal and molecular structures of stereoisomers of 1,3,5-triglycidyl-s-triazinetrione Andrew Hempel, Norman Camerman, and Arthur Camerman pp 648 - 651; DOI: 10.1021/jm00123a025 |
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Effects of steroid D-ring modification on suicide inactivation and competitive inhibition of aromatase by analogs of androsta-1,4-diene-3,17-dione Paul F. Sherwin, Patrick C. McMullan, and Douglas F. Covey pp 651 - 658; DOI: 10.1021/jm00123a026 |
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Alkylating partial muscarinic agonists related to oxotremorine. N-[4-[(2-Haloethyl)methylamino]-2-butynyl]-5-methyl-2-pyrrolidones Bjorn Ringdahl, Margareth Roch, Esther D. Katz, and Maria C. Frankland pp 659 - 663; DOI: 10.1021/jm00123a027 |
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New 4-(heteroanilido)piperidines, structurally related to the pure opioidagonist fentanyl, with agonist and/or antagonist properties Jerome R. Bagley, Richard L. Wynn, Frieda G. Rudo, Brian M. Doorley, H. Kenneth Spencer, and Theodore Spaulding pp 663 - 671; DOI: 10.1021/jm00123a028 |
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Studies on prodrugs. 11. Synthesis and antimicrobial activity of N-[(4-methyl-5-methylene-2-oxo-1,3-dioxolan-4-yl)oxy]norfloxacin Hirosato Kondo, Fumio Sakamoto, Toshio Uno, Yoshihiro Kawahata, and Goro Tsukamoto pp 671 - 674; DOI: 10.1021/jm00123a029 |
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In vitro metabolic transformations of vinblastine: oxidations catalyzed by peroxidase Sayed A. Elmarakby, Michael W. Duffel, Animesh Goswami, F. Sima Sariaslani, and John P. N. Rosazza pp 674 - 679; DOI: 10.1021/jm00123a030 |
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Studies on prodrugs. 10. Possible mechanism of N-dealkylation of N-masked norfloxacins having several active methylene groups Hirosato Kondo, Fumio Sakamoto, Yoshimasa Inoue, and Goro Tsukamoto pp 679 - 682; DOI: 10.1021/jm00123a031 |
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3-(Aminoalkyl)-1,2,3,4-tetrahydro-5H-[1]benzopyrano[3,4-c]pyridin-5-ones as potential anticholinergic bronchodilators David T. Connor, Paul C. Unangst, Charles F. Schwender, Roderick J. Sorenson, Mary E. Carethers, Chester Puchalski, Richard E. Brown, and Martin P. Finkel pp 683 - 688; DOI: 10.1021/jm00123a032 |
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Heterocyclic analogs of benzamide antiarrhythmic agents Reda Hanna, John W. Lampe, William C. Lumma, Paul W. Erhardt, Samuel S. Wong, and Mark E. Sullivan pp 688 - 693; DOI: 10.1021/jm00123a033 |
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Portage transport of sulfanilamide and sulfanilic acid Se Young Hwang, David A. Berges, John J. Taggart, and Charles Gilvarg pp 694 - 698; DOI: 10.1021/jm00123a034 |
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Dermorphin analogs carrying an increased positive net charge in their "message" domain display extremely high .mu.-opioid receptor selectivity Peter W. Schiller, Nguyen Thi Mai Dung, Nga N. Chung, and Carole Lemieux pp 698 - 703; DOI: 10.1021/jm00123a035 |
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Preparation and antitumor activity of additional mitomycin A analogs Salah M. Sami, William A. Remers, and William T. Bradner pp 703 - 708; DOI: 10.1021/jm00123a036 |
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(6R,6S)-5,8,10-Trideaza-5,6,7,8-tetrahydrofolate and (6R,6S)-5,8,10-trideaza-5,6,7,8-tetrahydropteroyl-L-ornithine as potential antifolates and antitumor agents. 35 Andre Rosowsky, Ronald A. Forsch, and Richard G. Moran pp 709 - 715; DOI: 10.1021/jm00123a037 |
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Modification of the hydroxylactone ring of camptothecin: inhibition of mammalian topoisomerase I and biological activity Robert P. Hertzberg, Mary Jo Caranfa, Kenneth G. Holden, Dalia R. Jakas, Gregory Gallagher, Michael R. Mattern, Shau Ming Mong, Joan O'Leary Bartus, Randall K. Johnson, and William D. Kingsbury pp 715 - 720; DOI: 10.1021/jm00123a038 |
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2H-[1]Benzopyrano[3,4-b]pyridines. Synthesis and activity at central monoamine receptors Alan Hutchison, Michael Williams, Reynalda De Jesus, George A. Stone, L. Sylvester, Frank H. Clarke, and Matthew A. Sills pp 720 - 727; DOI: 10.1021/jm00123a039 |
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Evaluation of glycolamide esters and various other esters of aspirin as true aspirin prodrugs Niels Moerk Nielsen and Hans Bundgaard pp 727 - 734; DOI: 10.1021/jm00123a040 |
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Benzofurans as mechanism-based inhibitors of dopamine .beta.-hydroxylase G. King Farrington, Alok Kumar, and Joseph J. Villafranca pp 735 - 737; DOI: 10.1021/jm00124a001 |
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Carboxyalkyl dipeptides with atrial natriuretic factor potentiating and antihypertensive activity Martin F. Haslanger, Edmund J. Sybertz, Bernard R. Neustadt, Elizabeth M. Smith, Terry L. Nechuta, and Joel Berger pp 737 - 739; DOI: 10.1021/jm00124a002 |
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Hybrid cholecystokinin (CCK) antagonists: new implications in the design and modification of CCK antagonists James F. Kerwin, Alex M. Nadzan, Hana Kopecka, Chun Wel Lin, Thomas Miller, David Witte, and Stanley Burt pp 739 - 742; DOI: 10.1021/jm00124a003 |
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Analogs of cisplatin derived from diaminodideoxytetritols. Synthesis and activity against the ADJ/PC6 plasmacytoma in mice Alan H. Haines, Christopher Morley, and Barry A. Murrer pp 742 - 745; DOI: 10.1021/jm00124a004 |
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Analysis of the in vitro antiviral activity of certain ribonucleosides against parainfluenza virus using a novel computer aided receptor modeling procedure Arup K. Ghose, Gordon M. Crippen, Ganapathi R. Revankar, Patricia A. McKernan, Donald F. Smee, and Roland K. Robins pp 746 - 756; DOI: 10.1021/jm00124a005 |
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Computer assisted design and synthesis of novel aldose reductase inhibitors John Butera, Jehan Bagli, Wendel Doubleday, Leslie Humber, Adi Treasurywala, Deborah Loughney, Kazimir Sestanj, Jane Millen, and Janet Sredy pp 757 - 765; DOI: 10.1021/jm00124a006 |
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Topography and conformational preferences of 6,7,8,9-tetrahydro-1-hydroxy-N,N-dipropyl-5H-benzocyclohepten-6-ylamine. A rationale for the dopaminergic inactivity Anders Karlen, Anne Helander, Lennart Kenne, and Uli Hacksell pp 765 - 774; DOI: 10.1021/jm00124a007 |
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Synthesis, DNA-binding properties, and antitumor activity of novel distamycin derivatives Federico Maria Arcamone, Fabio Animati, Brunella Barbieri, Emanuela Configliacchi, Roberto D'Alessio, Cristina Geroni, Fernando Carlo Giuliani, Ettore Lazzari, Milena Menozzi, and et al. pp 774 - 778; DOI: 10.1021/jm00124a008 |
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Resolved N,N-dialkylated 2-amino-8-hydroxytetralins: stereoselective interactions with 5-HT1A receptors in the brain Lena Bjoerk, Berit Backlund Hoeoek, David L. Nelson, Nils Erik Anden, and Uli Hacksell pp 779 - 783; DOI: 10.1021/jm00124a009 |
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Synthesis and biological evaluation of de(acetylglucosaminyl)didehydrodeoxy derivatives of teicoplanin antibiotics Adriano Malabarba, Aldo Trani, Giorgio Tarzia, Pietro Ferrari, Rosa Pallanza, and Marisa Berti pp 783 - 788; DOI: 10.1021/jm00124a010 |
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Synthesis of congeners and prodrugs. 3. Water-soluble prodrugs of taxol with potent antitumor activity H. M. Deutsch, J. A. Glinski, M. Hernandez, R. D. Haugwitz, V. L. Narayanan, M. Suffness, and Leon H. Zalkow pp 788 - 792; DOI: 10.1021/jm00124a011 |
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Potential antitumor agents. 58. Synthesis and structure-activity relationships of substituted xanthenone-4-acetic acids active against the colon 38 tumor in vivo Gordon W. Rewcastle, Graham J. Atwell, Bruce C. Baguley, Stephen B. Calveley, and William A. Denny pp 793 - 799; DOI: 10.1021/jm00124a012 |
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2'-Fluorinated isonucleosides. 1. Synthesis and biological activity of some methyl 2'-deoxy-2'-fluoro-2'-pyrimidinyl-D-arabinopyranosides M. Bobek, S. H. An, D. Skrincosky, E. De Clercq, and R. J. Bernacki pp 799 - 807; DOI: 10.1021/jm00124a013 |
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Hydroxyacetophenone-derived antagonists of the peptidoleukotrienes Frederick J. Brown, Peter R. Bernstein, Laura A. Cronk, David L. Dosset, Kevin C. Hebbel, Thomas P. Maduskuie Jr., Howard S. Shapiro, Edward P. Vacek, Ying K. Yee, and et al. pp 807 - 826; DOI: 10.1021/jm00124a014 |
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Synthesis and pharmacology of a series of 3- and 4-(phosphonoalkyl)pyridine- and -piperidine-2-carboxylic acids. Potent N-methyl-D-aspartate receptor antagonists Paul L. Ornstein, John M. Schaus, John W. Chambers, Diane L. Huser, J. David Leander, David T. Wong, Jonathan W. Paschal, Noel D. Jones, and Jack B. Deeter pp 827 - 833; DOI: 10.1021/jm00124a015 |
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Retinobenzoic acids. 2. Structure-activity relationships of chalcone-4-carboxylic acids and flavone-4'-carboxylic acids Hiroyuki Kagechika, Emiko Kawachi, Yuichi Hashimoto, and Koichi Shudo pp 834 - 840; DOI: 10.1021/jm00124a016 |
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Synthesis of some novel potent and selective catechol O-methyltransferase inhibitors Reijo Backstrom, Erkki Honkanen, Aino Pippuri, Pekka Kairisalo, Jarmo Pystynen, Kalevi Heinola, Erkki Nissinen, Inge Britt Linden, Pekka T. Mannisto, and et al. pp 841 - 846; DOI: 10.1021/jm00124a017 |
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Quinazoline antifolates inhibiting thymidylate synthase: 2-desamino derivatives with enhanced solubility and potency Terence R. Jones, Timothy J. Thornton, Anthony Flinn, Ann L. Jackman, D. R. Newell, and A. Hilary Calvert pp 847 - 852; DOI: 10.1021/jm00124a018 |
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Comparison of the biological effects of selected 5,8-dideazafolate analogs with their 2-desamino counterparts John B. Hynes, Shirish A. Patil, Robert L. Hagan, Aimee Cole, William Kohler, and James H. Freisheim pp 852 - 856; DOI: 10.1021/jm00124a019 |
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Synthesis and evaluation of the pharmacological activity of rigid analogs of sympathomimetic catecholamines derived from bicyclo[2.2.1]heptane A. Balsamo, M. C. Breschi, A. Lapucci, B. Macchia, F. Macchia, E. Martinotti, S. Nencetti, P. Nieri, and E. Orlandini pp 856 - 859; DOI: 10.1021/jm00124a020 |
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Design and synthesis of propranolol analogs as serotonergic agents M. Edward Pierson, Robert A. Lyon, Milt Titeler, Paul Kowalski, and Richard A. Glennon pp 859 - 863; DOI: 10.1021/jm00124a021 |
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Conformationally restricted analogs of the muscarinic agent N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide J. R. Michael Lundkvist, Bjorn Ringdahl, and Uli Hacksell pp 863 - 869; DOI: 10.1021/jm00124a022 |
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Identification of structural requirements for analogs of atrial natriuretic peptide (ANP) to discriminate between ANP receptor subtypes Philippe R. Bovy, Joan M. O'Neal, Gillian M. Olins, and Dennis R. Patton pp 869 - 874; DOI: 10.1021/jm00124a023 |
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Synthesis and D2 dopaminergic activity of pyrrolidinium, tetrahydrothiophenium, and tetrahydrothiophene analogs of sulpiride Marc W. Harrold, Raye Ann Wallace, Tahira Farooqui, Lane J. Wallace, Norman Uretsky, and Duane D. Miller pp 874 - 880; DOI: 10.1021/jm00124a024 |
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A minor modification of residue 1 in potent vasopressin antagonists dramatically reduces agonist activity William F. Huffman, Christine Albrightson-Winslow, Bridget Brickson, Heidemarie G. Bryan, Nancy Caldwell, George Dytko, Drake S. Eggleston, Lewis B. Kinter, Michael L. Moore, and et al. pp 880 - 884; DOI: 10.1021/jm00124a025 |
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Approaches to isozyme-specific inhibitors. 16. A novel methyl-C5' covalent adduct of L-ethionine and .beta.,.gamma.-imido-ATP as a potent multisubstrate inhibitor of rat methionine adenosyltransferases Vivekananda M. Vrudhula, Francis Kappler, Carol Afshar, Stephan L. Ginell, Leslie Lessinger, and Alexander Hampton pp 885 - 890; DOI: 10.1021/jm00124a026 |
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[(1H-Imidazol-1-yl)methyl]- and [(3-pyridinyl)methyl]pyrroles as thromboxane synthetase inhibitors Gregory R. Martinez, Donald R. Hirschfeld, Patrick J. Maloney, Diana S. Yang, Roberto P. Rosenkranz, and K. A. M. Walker pp 890 - 897; DOI: 10.1021/jm00124a027 |
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Topographic probes of angiotensin and receptor: potent angiotensin II agonist containing diphenylalanine and long-acting antagonists containing biphenylalanine and 2-indan amino acid in position 8 Kun Hwa Hsieh, Thomas R. LaHann, and Robert C. Speth pp 898 - 903; DOI: 10.1021/jm00124a028 |
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New sensitizers for photodynamic therapy. Controlled synthesis of purpurins and their effect on normal tissue Alan R. Morgan, Ashraff Rampersaud, Greta M. Garbo, Rick W. Keck, and Steven H. Selman pp 904 - 908; DOI: 10.1021/jm00124a029 |
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Book Reviews pp 909 - 928; DOI: 10.1021/jm00124a600 |
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A perspective on drug discovery and development through the genetic engineering of antibiotic-producing microorganisms C. Richard Hutchinson, Christopher W. Borell, Sharee L. Otten, Kim J. Stutzman-Engwall, and Yi Guang Wang pp 929 - 937; DOI: 10.1021/jm00125a001 |
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A multisubstrate adduct inhibitor of a purine biosynthetic enzyme with a picomolar dissociation constant James Inglese, Richard A. Blatchly, and Stephen J. Benkovic pp 937 - 940; DOI: 10.1021/jm00125a002 |
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Synthesis of 5-[1-hydroxy(or methoxy)-2-bromo(or chloro)ethyl]-2'-deoxyuridines and related halohydrin analogs with antiviral and cytotoxic activity Rakesh Kumar, Leonard I. Wiebe, Tse W. Hall, Edward E. Knaus, Dorothy R. Tovell, D. Lorne Tyrrell, Theresa M. Allen, and R. Fathi-Afshar pp 941 - 944; DOI: 10.1021/jm00125a003 |
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Synthesis and biological evaluation of certain C-4 substituted pyrazolo[3,4-b]pyridine nucleosides Yogesh S. Sanghvi, Steven B. Larson, Randall C. Willis, Roland K. Robins, and Ganapathi R. Revankar pp 945 - 951; DOI: 10.1021/jm00125a004 |
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The binding of benzenesulfonamides to carbonic anhydrase enzyme. A molecular mechanics study and quantitative structure-activity relationships Maria Cristina Menziani, Pier G. De Benedetti, Federico Gago, and W. Graham Richards pp 951 - 956; DOI: 10.1021/jm00125a005 |
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N-(Fluoroethyl)(imidazolylphenyl)formamidines. The issue of the active species of mifentidine Arturo Donetti, Enzo Cereda, Antoine Ezhaya, and Rosella Micheletti pp 957 - 961; DOI: 10.1021/jm00125a006 |
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Synthesis and dopaminergic activity of 2-substituted octahydrobenzo[f]quinolines J. Cymerman Craig, Steven M. Torkelson, Paul R. Findell, and Richard I. Weiner pp 961 - 968; DOI: 10.1021/jm00125a007 |
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Synthesis and pharmacological evaluation of 4,4-disubstituted piperidines John A. Colapret, George Diamantidis, H. Kenneth Spencer, Ted C. Spaulding, and Frieda G. Rudo pp 968 - 974; DOI: 10.1021/jm00125a008 |
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9,11-Epoxy-9-homo-14-thiaprost-5-enoic acid derivatives: potent thromboxane A2 antagonists Steven E. Hall, Wen Ching Han, Don N. Harris, Anders Hedberg, and Martin L. Ogletree pp 974 - 984; DOI: 10.1021/jm00125a009 |
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Design and synthesis of inhibitors of N8-acetylspermidine deacetylase Sasi A. Dredar, James W. Blankenship, Pamela E. Marchant, Victor Manneh, and David S. Fries pp 984 - 989; DOI: 10.1021/jm00125a010 |
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Renal vasodilators. The role of the 4-substituent in isoquinolin-3-ol cardiovascular agents. 4-Ureido derivatives of isoquinolin-3-ol with selective renal vasodilator properties Ramesh M. Kanojia, O. William Lever, Jeffery B. Press, Louella Williams, Harvey M. Werblood, Edward C. Giardino, Robert Falotico, and Alfonso J. Tobia pp 990 - 997; DOI: 10.1021/jm00125a011 |
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Synthesis and antiproliferative effects of novel 5'-fluorinated analogs of 5'-deoxy-5'-(methylthio)adenosine Janice R. Sufrin, Arthur J. Spiess, Debora L. Kramer, Paul R. Libby, and Carl W. Porter pp 997 - 1001; DOI: 10.1021/jm00125a012 |
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18-Cycloalkyl analogs of enisoprost Paul W. Collins, Alan F. Gasiecki, William E. Perkins, Gary W. Gullikson, Peter H. Jones, and Raymond F. Bauer pp 1001 - 1006; DOI: 10.1021/jm00125a013 |
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2,3-Dihydro-5-benzofuranols as antioxidant-based inhibitors of leukotriene biosynthesis Milton L. Hammond, Ihor E. Kopka, Robert A. Zambias, Charles G. Caldwell, Joshua Boger, Florence Baker, Tom Bach, Silvi Luell, and D. Euan MacIntyre pp 1006 - 1020; DOI: 10.1021/jm00125a014 |
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Benzodiazepine receptor binding activity of 6,9-disubstituted purines James L. Kelley, Ed W. McLean, Robert M. Ferris, and James L. Howard pp 1020 - 1024; DOI: 10.1021/jm00125a015 |
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Synthesis and structure-activity relationship of substituted tetrahydro- and hexahydro-1,2-benzisothiazol-3-one 1,1-dioxides and thiadiazinones: potential anxiolytic agents Magid Abou-Gharbia, John A. Moyer, Usha Patel, Michael Webb, Guy Schiehser, Terrance Andree, and J. Thomas Haskins pp 1024 - 1033; DOI: 10.1021/jm00125a016 |
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Synthesis and in vitro aldose reductase inhibitory activity of compounds containing an N-acylglycine moiety Jack DeRuiter, Blake E. Swearingen, Vinay Wandrekar, and Charles A. Mayfield pp 1033 - 1038; DOI: 10.1021/jm00125a017 |
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In-vitro antiproliferative activity of 4-substituted 2-(2-hydroxyphenyl)thiazolines on murine leukemia cells Gary T. Elliott, William A. Nagle, Ken F. Kelly, David McCollough, Robert L. Bona, and E. Robert Burns pp 1039 - 1043; DOI: 10.1021/jm00125a018 |
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Electrophilic derivatives of purines as irreversible inhibitors of A1 adenosine receptors Kenneth A. Jacobson, Suzanne Barone, Udai Kammula, and Gary L. Stiles pp 1043 - 1051; DOI: 10.1021/jm00125a019 |
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Activity of aromatic substituted phenylpiperazines lacking affinity for dopamine binding sites in a preclinical test of antipsychotic efficacy Gregory E. Martin, Robert J. Elgin, Joanne R. Mathiasen, Coralie B. Davis, James M. Kesslick, William J. Baldy, Richard P. Shank, Deena L. DiStefano, Cynthia L. Fedde, and Malcom K. Scott pp 1052 - 1056; DOI: 10.1021/jm00125a020 |
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Synthesis and biological evaluation of iodine-125- and iodine-123-4-iododexetimide, a potent muscarinic cholinergic receptor antagonist Alan A. Wilson, Robert F. Dannals, Hayden T. Ravert, J. James Frost, and Henry N. Wagner pp 1057 - 1062; DOI: 10.1021/jm00125a021 |
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Aromatic dienoyl tetramic acids. Novel antibacterial agents with activity against anaerobes and staphylococci Terry Rosen, Prabhavathi B. Fernandes, Mary A. Marovich, Linus Shen, James Mao, and Andre G. Pernet pp 1062 - 1069; DOI: 10.1021/jm00125a022 |
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Synthesis of 8-substituted derivatives of the 2-deoxy analog of 3-deoxy-.beta.-D-manno-2-octulopyranosonic acid (2-deoxy-.beta.-KDO) as inhibitors of 3-deoxy-D-manno-octulosonate cytidylyltransferase Brian G. Pring, Anita M. Jansson, Kerstin Persson, Inger Andersson, Ingalill Gagner-Milchert, Kent Gustafsson, and Alf Claesson pp 1069 - 1074; DOI: 10.1021/jm00125a023 |
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Synthesis, DNA binding and biological evaluation of synthetic precursors and novel analogs of netropsin Francoise Debart, Christian Perigaud, Gilles Gosselin, Driss Mrani, Bernard Rayner, Pierre Le Ber, Christian Auclair, Jan Balzarini, Erik De Clercq, and et al. pp 1074 - 1083; DOI: 10.1021/jm00125a024 |
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New hydrogen-bond potentials for use in determining energetically favorable binding sites on molecules of known structure David N. A. Boobbyer, Peter J. Goodford, Peter M. McWhinnie, and Rebecca C. Wade pp 1083 - 1094; DOI: 10.1021/jm00125a025 |
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Analogs of atriopeptin(103-125)amide having high binding selectivity Kerry L. Spear, Monica S. Brown, Gillian M. Olins, and Dennis R. Patton pp 1094 - 1098; DOI: 10.1021/jm00125a026 |
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Retinobenzoic acids. 3. Structure-activity relationships of retinoidal azobenzene-4-carboxylic acids and stilbene-4-carboxylic acids Hiroyuki Kagechika, Toshiyuki Himi, Koushi Namikawa, Emiko Kawachi, Yuichi Hashimoto, and Koichi Shudo pp 1098 - 1108; DOI: 10.1021/jm00125a027 |
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Peripherally acting enkephalin analogs. 2. Polar tri- and tetrapeptides George W. Hardy, Lawrence A. Lowe, Gail Mills, Pang Yih Sang, Dean S. A. Simpkin, Rhonda L. Follenfant, Clare Shankley, and Terence W. Smith pp 1108 - 1118; DOI: 10.1021/jm00125a028 |
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Antiinflammatory activity of a series of substituted 2,3-dihydro-6-hydroxypyrimido[2,1-f]purine-4,8(1H,9H)-diones James J. Kaminski, Daniel M. Solomon, David J. Conn, Shing Chun Wong, P. J. S. Chiu, Tobias Massa, Marvin I. Siegel, and Arthur S. Watnick pp 1118 - 1127; DOI: 10.1021/jm00125a029 |
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Dynamics and thermodynamics of the counterion effect in 7H-pyridocarbazole dimer (ditercalinium). Hypothesis of a nonbisintercalative binding mode to calf thymus DNA at high drug base ratio G. Dodin pp 1127 - 1134; DOI: 10.1021/jm00125a030 |
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Synthesis of the 2-chloro analogs of 3'-deoxyadenosine, 2',3'-dideoxyadenosine, and 2',3'-didehydro-2',3'-dideoxyadenosine as potential antiviral agents Andre Rosowsky, Vishnu C. Solan, Joseph G. Sodroski, and Ruth M. Ruprecht pp 1135 - 1140; DOI: 10.1021/jm00125a031 |
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Book Reviews pp 1140 - 1144; DOI: 10.1021/jm00125a600 |
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7-[3-(4-Acetyl-3-methoxy-2-propylphenoxy)propoxy]-3,4-dihydro-8-propyl-2H-1-benzopyran-2-carboxylic acid: an orally active selective leukotriene B4 receptor antagonist Stevan W. Djuric, Paul W. Collins, Peter H. Jones, Robert L. Shone, Bie Shung Tsai, Donald J. Fretland, Gregory M. Butchko, Doreen Villani-Price, Robert H. Keith, and et al. pp 1145 - 1147; DOI: 10.1021/jm00126a001 |
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The thieno[3,2-c]pyridine and furo[3,2-c]pyridine rings: new pharmacophores with potential antipsychotic activity James S. New, William L. Christopher, Joseph P. Yevich, Rhett Butler, R. Francis Schlemmer, Cam P. VanderMaelen, and Joseph A. Cipollina pp 1147 - 1156; DOI: 10.1021/jm00126a002 |
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1-(2-Aminoethyl)-6-aryl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepines with diuretic and natriuretic activity Jackson B. Hester, James H. Ludens, D. Edward Emmert, and Bruce E. West pp 1157 - 1163; DOI: 10.1021/jm00126a003 |
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Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations William S. Messer, Brenda R. Ellerbrock, Douglas A. Smith, and Wayne Hoss pp 1164 - 1172; DOI: 10.1021/jm00126a004 |
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Cardiotonic agents. 5. Fragments from the heterocycle-phenyl-imidazole pharmacophore Paul W. Erhardt, Alfred A. Hagedorn, III, David Davey, Cynthia A. Pease, Bhaskar R. Venepalli, Carl W. Griffin, Robert P. Gomez, Jay R. Wiggins, William R. Ingebretsen, and et al. pp 1173 - 1176; DOI: 10.1021/jm00126a005 |
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N-[(Arylmethoxy)phenyl] and N-[(arylmethoxy)naphthyl] sulfonamides: potent orally active leukotriene d4 antagonists of novel structure John H. Musser, Anthony F. Kreft, Reinhold H. W. Bender, Dennis M. Kubrak, Richard P. Carlson, Joseph Chang, and James M. Hand pp 1176 - 1183; DOI: 10.1021/jm00126a006 |
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Synthesis and binding affinities of cyclic and related linear analogs of CCK8 selective for central receptors Bruno Charpentier, Adeline Dor, Pierre Roy, Patrick England, Hung Pham, Christiane Durieux, and Bernard P. Roques pp 1184 - 1190; DOI: 10.1021/jm00126a007 |
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Synthesis and structure-activity relationships of a novel class of 5-lipoxygenase inhibitors. 2-(Phenylmethyl)-4-hydroxy-3,5-dialkylbenzofurans: the development of L-656,224 Cheuk K. Lau, Patrice C. Belanger, John Scheigetz, Claude Dufresne, Haydn W. R. Williams, Alan L. Maycock, Yvan Guindon, Thomas Bach, Aimee L. Dallob, and et al. pp 1190 - 1197; DOI: 10.1021/jm00126a008 |
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2-Haloaporphines as potent dopamine agonists Sten Ramsby, John L. Neumeyer, Dimitri Grigoriadis, and Philip Seeman pp 1198 - 1201; DOI: 10.1021/jm00126a009 |
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Synthesis and antiinflammatory and analgesic activity of 5-aroyl-6-(methylthio)-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids and 1-methyl-4-(methylthio)-5-aroylpyrrole-2-acetic acids Joseph M. Muchowski, Edvige Galeazzi, Robert Greenhouse, Angel Guzman, Virginia Perez, Neil Ackerman, Silveria A. Ballaron, Joseph R. Rovito, Albert J. Tomolonis, and et al. pp 1202 - 1207; DOI: 10.1021/jm00126a010 |
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Rotationally restricted mimics of rigid molecules: nonspirocyclic hydantoin aldose reductase inhibitors James P. Rizzi, Rodney C. Schnur, Nancy J. Hutson, Kenneth G. Kraus, and Paul R. Kelbaugh pp 1208 - 1213; DOI: 10.1021/jm00126a011 |
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Thienylpyrazoloquinolines with high affinity to benzodiazepine receptors: continuous shift from inverse agonist to agonist properties depending on the size of the alkyl substituent Hirohisa Shindo, Susumu Takada, Shunji Murata, Masami Eigyo, and Akira Matsushita pp 1213 - 1217; DOI: 10.1021/jm00126a012 |
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Synthesis, in vitro acetylcholine-storage-blocking activities, and biological properties of derivatives and analogs of trans-2-(4-phenylpiperidino)cyclohexanol (vesamicol) Gary A. Rogers, Stanley M. Parsons, D. C. Anderson, Lena M. Nilsson, Ben A. Bahr, Wayne D. Kornreich, Rose Kaufman, Robert S. Jacobs, and Bernard Kirtman pp 1217 - 1230; DOI: 10.1021/jm00126a013 |
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Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions Mah T. Shamim, Dieter Ukena, William L. Padgett, and John W. Daly pp 1231 - 1237; DOI: 10.1021/jm00126a014 |
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6-Alkyl-N,N-disubstituted-2-pyridinamines as anticonvulsant agents Michael R. Pavia, Charles P. Taylor, and Sandra J. Lobbestael pp 1237 - 1242; DOI: 10.1021/jm00126a015 |
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Phencyclidine-like effects of tetrahydroisoquinolines and related compounds Nancy M. Gray, Brian K. Cheng, Stephen J. Mick, Cecelia M. Lair, and Patricia C. Contreras pp 1242 - 1248; DOI: 10.1021/jm00126a016 |
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Antimalarial activity of new water-soluble dihydroartemisinin derivatives. 2. Stereospecificity of the ether side chain Ai Jeng Lin, Margaret Lee, and Daniel L. Klayman pp 1249 - 1252; DOI: 10.1021/jm00126a017 |
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Acid-sensitive latent inhibitors for proteolytic enzymes: synthesis and characterization Marc S. Silver and John H. Haskell pp 1253 - 1259; DOI: 10.1021/jm00126a018 |
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Synthesis, opioid receptor binding profile, and antinociceptive activity of 1-azaspiro[4.5]decan-10-yl amides Roger A. Fujimoto, Jerome Boxer, Robert H. Jackson, John P. Simke, Robert F. Neale, Elaine W. Snowhill, Beverly J. Barbaz, Michael Williams, and Matthew A. Sills pp 1259 - 1265; DOI: 10.1021/jm00126a019 |
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Synthesis and thromboxane synthetase inhibitory activity of di- or tetrahydrobenzo[b]thiophenecarboxylic acid derivatives Yoshiya Amemiya, Atsusuke Terada, Kazuyuki Wachi, Hachio Miyazawa, Naoko Hatakeyama, Keiichi Matsuda, and Takeshi Oshima pp 1265 - 1272; DOI: 10.1021/jm00126a020 |
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Hybrid molecules: growth inhibition of Leishmania donovani promastigotes by thiosemicarbazones of 3-carboxy-.beta.-carbolines Robert H. Dodd, Catherine Ouannes, Malka Robert-Gero, and Pierre Potier pp 1272 - 1276; DOI: 10.1021/jm00126a021 |
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Folate analogs. 31. Synthesis of the reduced derivatives of 11-deazahomofolic acid, 10-methyl-11-deazahomofolic acid, and their evaluation as inhibitors of glycinamide ribonucleotide formyltransferase M. G. Nair, B. R. Murthy, Sharadbala D. Patil, R. L. Kisliuk, J. Thorndike, Y. Gaumont, R. Ferone, D. S. Duch, and M. P. Edelstein pp 1277 - 1283; DOI: 10.1021/jm00126a022 |
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Folate analogs. 32. Synthesis and biological evaluation of 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid and related compounds Sharadbala D. Patil, Cecil Jones, M. G. Nair, J. Galivan, F. Maley, R. L. Kisliuk, Y Gaumont, David Duch, and Robert Ferone pp 1284 - 1289; DOI: 10.1021/jm00126a023 |
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Synthesis and tumor uptake of 5-bromine-82- and 5-iodine-131-labeled 5-halo-1-(2-fluoro-2-deoxy-.beta.-D-ribofuranosyl)uracils John R. Mercer, Li Hua Xu, Edward E. Knaus, and Leonard I. Wiebe pp 1289 - 1294; DOI: 10.1021/jm00126a024 |
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Synthesis and antitumor activity of fused tetracyclic quinoline derivatives. 1 Masatoshi Yamato, Yasuo Takeuchi, Kuniko Hashigaki, Yuji Ikeda, Ming Rong Chang, Kyoko Takeuchi, Mayumi Matsushima, Takashi Tsuruo, Tazuko Tashiro, and et al. pp 1295 - 1300; DOI: 10.1021/jm00126a025 |
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Synthesis and biological evaluation of S-adenosyl-1,12-diamino-3-thio-9-azadodecane, a multisubstrate adduct inhibitor of spermine synthase Patrick M. Woster, Alison Y. Black, Keith J. Duff, James K. Coward, and Anthony E. Pegg pp 1300 - 1307; DOI: 10.1021/jm00126a026 |
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Synthesis and biological properties of purine and pyrimidine 5'-deoxy-5'-(dihydroxyphosphinyl)-.beta.-D-ribofuranosyl analogs of AMP, GMP, IMP, and CMP Natarajan Raju, Donald F. Smee, Roland K. Robins, and Morteza M. Vaghefi pp 1307 - 1313; DOI: 10.1021/jm00126a027 |
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Synthesis of novel 5-fluoro analogs of norfloxacin and ciprofloxacin Daniel B. Moran, Carl B. Ziegler, Theresa S. Dunne, Nydia A. Kuck, and Yang I Lin pp 1313 - 1318; DOI: 10.1021/jm00126a028 |
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Darmstoff analogs. 3. Actions of choline esters of acetal phosphatidic acids on visceral smooth muscle Michael H. Marx, Robert A. Wiley, D. G. Satchell, and M. Helen Maguire pp 1319 - 1322; DOI: 10.1021/jm00126a029 |
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Cyclic carbamate analogs of pilocarpine Per Sauerberg, June Chen, Elizabeth WoldeMussie, and Henry Rapoport pp 1322 - 1326; DOI: 10.1021/jm00126a030 |
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Thromboxane A2 synthetase inhibitors. 2. Syntheses and activities of tetrahydronaphthalene and indane derivatives Munefumi Kanao, Yoshifumi Watanabe, Youichi Kimura, Junji Saegusa, Kenjiro Yamamoto, Hideyuki Kanno, Naoaki Kanaya, Hideo Kubo, Shinichiro Ashida, and Fumiyoshi Ishikawa pp 1326 - 1334; DOI: 10.1021/jm00126a031 |
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N1-alkyl-substituted derivatives of chlorpropamide as inhibitors of aldehyde dehydrogenase Herbert T. Nagasawa, James A. Elberling, Eugene G. DeMaster, and Frances N. Shirota pp 1335 - 1340; DOI: 10.1021/jm00126a032 |
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Metabolism of 3-(p-chlorophenyl)pyrrolidine. Structural effects in conversion of a prototype .gamma.-aminobutyric acid prodrug to lactam and .gamma.-aminobutyric acid type metabolites G. Michael Wall and John K. Baker pp 1340 - 1348; DOI: 10.1021/jm00126a033 |
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New cyclic peptides with cytotoxic activity from the ascidian Lissoclinum patella Bernard M. Degnan, Clifford J. Hawkins, Martin F. Lavin, Elizabeth J. McCaffrey, David L. Parry, Anna L. Van den Brenk, and Diane J. Watters pp 1349 - 1354; DOI: 10.1021/jm00126a034 |
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Novel cytotoxic compounds from the ascidian Lissoclinum bistratum Bernard M. Degnan, Clifford J. Hawkins, Martin F. Lavin, Elizabeth J. McCaffrey, David L. Parry, and Diane J. Watters pp 1354 - 1359; DOI: 10.1021/jm00126a035 |
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Novel indolecarboxamidotetrazoles as potential antiallergy agents Paul C. Unangst, David T. Connor, S. Russell Stabler, Robert J. Weikert, Mary E. Carethers, John A. Kennedy, David O. Thueson, James C. Chestnut, Richard L. Adolphson, and M. C. Conroy pp 1360 - 1366; DOI: 10.1021/jm00126a036 |
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The role of position four in angiotensin II antagonism: a structure-activity study James Samanen, T. Cash, D. Narindray, E. Brandeis, T. Yellin, and D. Regoli pp 1366 - 1370; DOI: 10.1021/jm00126a037 |
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Azido glycols: potent, low molecular weight renin inhibitors containing an unusual post scissile site residue Saul H. Rosenberg, Keith W. Woods, Hollis D. Kleinert, Herman Stein, Hugh N. Nellans, Daniel J. Hoffman, Stephen G. Spanton, Richard A. Pyter, Jerome Cohen, and et al. pp 1371 - 1378; DOI: 10.1021/jm00126a038 |
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Inhibition of aminopeptidases by peptides containing ketomethylene and hydroxyethylene amide bond replacements Scott L. Harbeson and Daniel H. Rich pp 1378 - 1392; DOI: 10.1021/jm00126a039 |
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Probes for narcotic receptor mediated phenomena. 15. (3S,4S)-(+)-trans-3-Methylfentanyl isothiocyanate, a potent site-directed acylating agent for the .delta.-opioid receptors in vitro Chong Ho Kim, Richard B. Rothman, Arthur E. Jacobson, Mariena V. Mattson, Victor Bykov, Richard A. Streaty, Werner A. Klee, Clifford George, Joseph B. Long, and Kenner C. Rice pp 1392 - 1398; DOI: 10.1021/jm00126a040 |
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Synthesis and antimicrobial properties of substituted .beta.-aminoxypropionyl penicillins and cephalosporins A. Balsamo, G. Broccali, A. Lapucci, B. Macchia, F. Macchia, E. Orlandini, and A. Rossello pp 1398 - 1401; DOI: 10.1021/jm00126a041 |
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New 1,4-dihydropyridine derivatives combining calcium antagonism and .alpha.-adrenolytic properties Gilbert Marciniak, Antonio Delgado, Gerard Leclerc, Jeanne Velly, Nicole Decker, and Jean Schwartz pp 1402 - 1407; DOI: 10.1021/jm00126a042 |
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Book Reviews pp 1407 - 1414; DOI: 10.1021/jm00126a600 |
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Oxidation of neplanocin A to the corresponding 3'-keto derivative by S-adenosylhomocysteine hydrolase Steven D. Paisley, Michael S. Wolfe, and Ronald T. Borchardt pp 1415 - 1418; DOI: 10.1021/jm00127a001 |
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E-ring desoxy analogs of etoposide Mark G. Saulnier, Dolatrai M. Vyas, David R. Langley, Terrence W. Doyle, William C. Rose, Alfred R. Crosswell, and Byron H. Long pp 1418 - 1420; DOI: 10.1021/jm00127a002 |
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Synthesis, cytotoxicity, and antiviral activity of certain 7-[(2-hydroxyethoxy)methyl]pyrrolo[2,3-d]pyrimidine nucleosides related to toyocamycin and sangivamycin Pranab K. Gupta, M. Reza Nassiri, Lisa A. Coleman, Linda L. Wotring, John C. Drach, and Leroy B. Townsend pp 1420 - 1425; DOI: 10.1021/jm00127a003 |
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Bifunctional antitumor compounds: synthesis and characterization of a gold(III)-streptonigrin complex with thiol-modulating properties A. Moustatih and A. Garnier-Suillerot pp 1426 - 1431; DOI: 10.1021/jm00127a004 |
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(.+-.)-7-Chloro-8-hydroxy-1-(4'-[125I]iodophenyl)-3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine: a potential CNS D-1 dopamine receptor imaging agent Sumalee Chumpradit, Hank F. Kung, Jeffrey Billings, Mei Ping Kung, and Sangren Pan pp 1431 - 1435; DOI: 10.1021/jm00127a005 |
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N-(Cyclohexylcarbonyl)-D-phenylalanines and related compounds. A new class of oral hypoglycemic agents. 2 Hisashi Shinkai, Masahiko Nishikawa, Yusuke Sato, Koji Toi, Izumi Kumashiro, Yoshiko Seto, Mariko Fukuma, Katsuaki Dan, and Shigeshi Toyoshima pp 1436 - 1441; DOI: 10.1021/jm00127a006 |
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Synthesis of 3-deazaneplanocin A, a powerful inhibitor of S-adenosylhomocysteine hydrolase with potent and selective in vitro and in vivo antiviral activities Christopher K. H. Tseng, Victor E. Marquez, Richard W. Fuller, Barry M. Goldstein, David R. Haines, Howard McPherson, Jack L. Parsons, William M. Shannon, Gussie Arnett, and et al. pp 1442 - 1446; DOI: 10.1021/jm00127a007 |
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Synthesis and antitumor activity of ribavirin imidates. New facile synthesis of ribavirin amidine (1-.beta.-D-ribofuranosyl-1,2,4-triazole-3-carboxamidine hydrochloride) Ganesh D. Kini, Roland K. Robins, and Thomas L. Avery pp 1447 - 1449; DOI: 10.1021/jm00127a008 |
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Inhibition of cyclic adenosine-3',5'-monophosphate phosphodiesterase from vascular smooth muscle by rolipram analogs Michel C. Marivet, Jean Jacques Bourguignon, Claire Lugnier, Andre Mann, Jean Claude Stoclet, and Camille Georges Wermuth pp 1450 - 1457; DOI: 10.1021/jm00127a009 |
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Synthesis and antiviral activity of the nucleotide analog (S)-1-[3-hydroxy-2-(phosphonylmethoxy)propyl]cystosine Joanne J. Bronson, Ismail Ghazzouli, Michael J. M. Hitchcock, Robert R. Webb, and John C. Martin pp 1457 - 1463; DOI: 10.1021/jm00127a010 |
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3,7-Dideazapurine nucleosides. Synthesis and antitumor activity of 1-deazatubercidin and 2-chloro-2'-deoxy-3,7-dideazaadenosine Gloria Cristalli, Palmarisa Franchetti, M. Grifantini, Giuseppe Nocentini, and Sauro Vittori pp 1463 - 1466; DOI: 10.1021/jm00127a011 |
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Synthesis of 2,3-diaziridinyl-1,4-naphthoquinonyl sulfonate derivatives as potential antineoplastic agents Tai Shun Lin, Shiping Xu, Liya Zhu, Lucille A. Cosby, and Alan C. Sartorelli pp 1467 - 1471; DOI: 10.1021/jm00127a012 |
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Nucleosides of azathioprine and thiamiprine as antiarthritics Thomas A. Krenitsky, Willard W. Hall, Jeffrey L. Selph, James F. Truax, and Ralph Vinegar pp 1471 - 1475; DOI: 10.1021/jm00127a013 |
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Synthesis of a tritium-labeled indolidan analog and its use as a radioligand for phosphodiesterase-inhibitor cardiotonic binding sites David W. Robertson, Joseph H. Krushinski, Barbara G. Utterback, and Raymond F. Kauffman pp 1476 - 1480; DOI: 10.1021/jm00127a014 |
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Nonsteroidal cardiotonics. 2. The inotropic activity of linear, tricyclic 5-6-5 fused heterocycles Wolfgang Von der Saal, Jens Peter Hoelck, Wolfgang Kampe, Alfred Mertens, and Bernd Mueller-Beckmann pp 1481 - 1491; DOI: 10.1021/jm00127a015 |
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Effects of N-substitution on the activation mechanisms of 4-hydroxycyclophosphamide analogs Chul Hoon Kwon and Richard F. Borch pp 1491 - 1496; DOI: 10.1021/jm00127a016 |
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New kelatorphan-related inhibitors of enkephalin metabolism: improved antinociceptive properties Juan Xie, Jean Marc Soleilhac, Catherine Schmidt, Jacques Peyroux, Bernard P. Roques, and Marie Claude Fournie-Zaluski pp 1497 - 1503; DOI: 10.1021/jm00127a017 |
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Effect of structural modifications in the C7-C11 region of the retinoid skeleton on biological activity in a series of aromatic retinoids Marcia I. Dawson, Peter D. Hobbs, Krzysztof A. Derdzinski, Wan Ru Chao, Gernot Frenking, Gilda H. Loew, Anton M. Jetten, Joseph L. Napoli, John B. Williams, and et al. pp 1504 - 1517; DOI: 10.1021/jm00127a018 |
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Synthesis and antitumor activity of 5-deaza-5,6,7,8-tetrahydrofolic acid and its N10-substituted analogs Edward C. Taylor, James M. Hamby, Chuan Shih, Gerald B. Grindey, Sharon M. Rinzel, G. Peter Beardsley, and Richard G. Moran pp 1517 - 1522; DOI: 10.1021/jm00127a019 |
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Binary antidotes for organophosphate poisoning: aprophen analogs that are both antimuscarinics and carbamates Haim Leader, Ruthann M. Smejkal, Charlotte S. Payne, Felipe N. Padilla, B. P. Doctor, Richard K. Gordon, and Peter K. Chiang pp 1522 - 1528; DOI: 10.1021/jm00127a020 |
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Organic phosphorus compounds. 2. Synthesis and coronary vasodilator activity of (benzothiazolylbenzyl)phosphonate derivatives Kohichiro Yoshino, Toshihiko Kohno, Tominori Morita, and Goro Tsukamoto pp 1528 - 1532; DOI: 10.1021/jm00127a021 |
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Diethylstilbestrol-linked cytotoxic agents. Synthesis and binding affinity for estrogen receptors Karsten Krohn, Konrad Kulikowski, and Guy Leclercq pp 1532 - 1538; DOI: 10.1021/jm00127a022 |
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Hexestrol-linked cytotoxic agents: synthesis and binding affinity for estrogen receptors Hannelore Koehle, Karsten Krohn, and Guy Leclercq pp 1538 - 1547; DOI: 10.1021/jm00127a023 |
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Synthesis and biological evaluation of certain 3-.beta.-D-ribofuranosyl-1,2,4-triazolo[4,3-b]pyridazines related to formycin prepared via ring closure of pyridazine precursors Yonghan Kang, Steven B. Larson, Roland K. Robins, and Ganapathi R. Revankar pp 1547 - 1551; DOI: 10.1021/jm00127a024 |
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2(1H)-Quinolinones with cardiac stimulant activity. 3. Synthesis and biological properties of 6-imidazol-1-yl derivatives Andrew S. Bell, Simon F. Campbell, David S. Morris, David A. Roberts, and Mark H. Stefaniak pp 1552 - 1558; DOI: 10.1021/jm00127a025 |
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Inhibition of mammalian folylpolyglutamate synthetase and human dihydrofolate reductase by 5,8-dideaza analogs of folic acid and aminopterin bearing a terminal L-ornithine Shirish A. Patil, Barry Shane, James H. Freisheim, Shyam K. Singh, and John B. Hynes pp 1559 - 1565; DOI: 10.1021/jm00127a026 |
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Tetrahydro thiadiazolo isoquinolines: synthesis and inhibition of phenylethanolamine-N-methyltransferase Gerald R. Girard, William E. Bondinell, Leonard M. Hillegass, Kenneth G. Holden, Robert G. Pendleton, and Irene Uzinskas pp 1566 - 1571; DOI: 10.1021/jm00127a027 |
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Synthesis of the novel .pi.-(benzyloxymethyl)-protected histidine analog of statine. Inhibition of penicillopepsin by pepstatin-derived peptides containing different statine side-chain derivatives Juergen Maibaum and Daniel H. Rich pp 1571 - 1576; DOI: 10.1021/jm00127a028 |
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Sodium channel binding and anticonvulsant activities for the enantiomers of a bicyclic 2,4-oxazolidinedione and monocyclic models Wayne J. Brouillette, Gary L. Grunewald, George B. Brown, Timothy M. DeLorey, M. Shamim Akhtar, and Gang Liang pp 1577 - 1580; DOI: 10.1021/jm00127a029 |
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Exploration of phenyl-spaced 2-amino-(5-9)-phosphonoalkanoic acids as competitive N-methyl-D-aspartic acid antagonists Christopher F. Bigge, James T. Drummond, Graham Johnson, Thomas Malone, Albert W. Probert, Frank W. Marcoux, Linda L. Coughenour, and Laura J. Brahce pp 1580 - 1590; DOI: 10.1021/jm00127a030 |
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Dimethylsulfonium analogs of the muscarinic agent McN-A-343: [4-[[N-(3- or 4-halophenyl)carbamoyl]oxy]-2-butynyl]dimethylsulfonium perchlorates Charlotta Mellin, Hugo M. Vargas, and Bjorn Ringdahl pp 1590 - 1593; DOI: 10.1021/jm00127a031 |
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Intercalating agents with covalent bond forming capability. A novel type of potential anticancer agents. 2. Derivatives of chrysophanol and emodin Masao Koyama, Kiyobumi Takahashi, Ting Chao Chou, Zbigniew Darzynkiewicz, Jan Kapuscinski, T. Ross Kelly, and Kyoichi A. Watanabe pp 1594 - 1599; DOI: 10.1021/jm00127a032 |
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Angiotensin converting enzyme inhibitors: spirapril and related compounds Elizabeth M. Smith, Gerald F. Swiss, Bernard R. Neustadt, Paul McNamara, Elijah H. Gold, Edmund J. Sybertz, and Thomas Baum pp 1600 - 1606; DOI: 10.1021/jm00127a033 |
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Inhibition of human leukocyte elastase by derivatives of N-hydroxysuccinimide. A structure-activity-relationship study W. C. Groutas, M. J. Brubaker, M. A. Stanga, J. C. Castrisos, J. P. Crowley, and E. J. Schatz pp 1607 - 1611; DOI: 10.1021/jm00127a034 |
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Synthesis, mechanism of action, and biological evaluation of mitosenes E. O. M. Orlemans, W. Verboom, M. W. Scheltinga, D. N. Reinhoudt, P. Lelieveld, H. H. Fiebig, B. R. Winterhalter, J. A. Double, and M. C. Bibby pp 1612 - 1620; DOI: 10.1021/jm00127a035 |
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Highly selective .kappa.-opioid analgesics. 2. Synthesis and structure activity relationships of novel N-(2-aminocyclohexyl)arylacetamide derivatives Paul R. Halfpenny, Raymond G. Hill, David C. Horwell, John Hughes, John C. Hunter, Stephen Johnson, and David C. Rees pp 1620 - 1626; DOI: 10.1021/jm00127a036 |
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Heteroaromatic analogs of the .alpha.2-adrenoreceptor partial agonist clonidine Christopher B. Chapleo, Richard C. M. Butler, David C. England, Peter L. Myers, Alan G. Roach, Colin F. C. Smith, Michael R. Stillings, and Ian F. Tulloch pp 1627 - 1630; DOI: 10.1021/jm00127a037 |
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The importance of the orientation of the C9 substituent to cannabinoid activity Patricia H. Reggio, Kaylar V. Greer, and Stephanie M. Cox pp 1630 - 1635; DOI: 10.1021/jm00127a038 |
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Mono and bis(bioreductive) alkylating agents: synthesis and antitumor activities in a B16 melanoma model Donald T. Witiak, John T. Loper, Subramaniam Ananthan, Anna Maria Almerico, Vernon L. Verhoef, and Joyce A. Filppi pp 1636 - 1642; DOI: 10.1021/jm00127a039 |
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17-Desoxy estrogen analogs Richard H. Peters, David F. Crowe, Mitchell A. Avery, Wesley K. M. Chong, and Masato Tanabe pp 1642 - 1652; DOI: 10.1021/jm00127a040 |
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Renin inhibitors. Synthesis of transition-state analog inhibitors containing phosphorus acid derivatives at the scissile bond Mark C. Allen, Walter Fuhrer, Brian Tuck, Roy Wade, and Jeanette M. Wood pp 1652 - 1661; DOI: 10.1021/jm00127a041 |
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Book Reviews pp 1661 - 1664; DOI: 10.1021/jm00127a600 |
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S-(2-oxopentadecyl)-CoA, a nonhydrolyzable analog of myristoyl-CoA, is a potent inhibitor of myristoyl-CoA: protein N-myristoyltransferase Lisa A. Paige, Guo Qiang Zheng, Shawn A. DeFrees, John M. Cassady, and Robert L. Geahlen pp 1665 - 1667; DOI: 10.1021/jm00128a001 |
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C2,N6-Disubstituted adenosines: synthesis and structure-activity relationships Bharat K. Trivedi and Robert F. Bruns pp 1667 - 1673; DOI: 10.1021/jm00128a002 |
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Antibacterials. Synthesis and structure-activity studies of 3-aryl-2-oxooxazolidines. 1. The B group Walter A. Gregory, David R. Brittelli, C. L. J. Wang, Mark A. Wuonola, Ronald J. McRipley, David C. Eustice, Virginia S. Eberly, Andrew M. Slee, Martin Forbes, and P. T. Bartholomew pp 1673 - 1681; DOI: 10.1021/jm00128a003 |
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Cholecystokinin antagonists. Synthesis and biological evaluation of 3-substituted benzolactams W. H. Parsons, A. A. Patchett, M. K. Holloway, G. M. Smith, J. L. Davidson, V. J. Lotti, and R. S. L. Chang pp 1681 - 1685; DOI: 10.1021/jm00128a004 |
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Antiulcer agents. 4. Conformational considerations and the antiulcer activity of substituted imidazo[1,2-a]pyridines and related analogs James J. Kaminski, Chester Puchalski, Daniel M. Solomon, Razia K. Rizvi, David J. Conn, Arthur J. Elliott, Raymond G. Lovey, Henry Guzik, P. J. S. Chiu, and et al. pp 1686 - 1700; DOI: 10.1021/jm00128a005 |
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Structure-activity relationship of antiestrogens. A study using triarylbutenone, benzofuran, and triarylfuran analogs as models for triarylethylenes and triarylpropenones Neelam Durani, Raka Jain, Ashraf Saeed, Dinesh K. Dikshit, Susheel Durani, and Randhir S. Kapil pp 1700 - 1707; DOI: 10.1021/jm00128a006 |
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Minimum-structure enkephalin analogs incorporating L-tyrosine, D (or L)-phenylalanine, and a diamine spacer Alan R. Jacobson, Alan R. Gintzler, and Lawrence M. Sayre pp 1708 - 1717; DOI: 10.1021/jm00128a007 |
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Tricyclic compounds as selective muscarinic receptor antagonists. 3. Structure-selectivity relationships in a series of cardioselective (M2) antimuscarinics Wolfhard W. Engel, Wolfgang G. Eberlein, Gerhard Mihm, Rudolf Hammer, and Guenter Trummlitz pp 1718 - 1724; DOI: 10.1021/jm00128a008 |
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Synthesis of unsymmetrically substituted 1,4-bis[(aminoalkyl)amino]anthracene-9,10-diones as potential antileukemic agents Barbara Stefanska, Maria Dzieduszycka, Sante Martelli, and Edward Borowski pp 1724 - 1728; DOI: 10.1021/jm00128a009 |
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Antimalarials. 16. Synthesis of 2-substituted analogs of 8-[(4-amino-1-methylbutyl)amino]-6-methoxy-4-methyl-5-[3-(trifluoromethyl)phenoxy]quinoline as candidate antimalarials Maurice P. LaMontagne, Peter Blumbergs, and David C. Smith pp 1728 - 1732; DOI: 10.1021/jm00128a010 |
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Synthesis and antiviral activity of 3'-C-cyano-3'-deoxynucleosides Maria Jose Camarasa, Angel Diaz-Ortiz, Ana Calvo-Mateo, Federico G. De las Heras, Jan Balzarini, and Erik De Clercq pp 1732 - 1738; DOI: 10.1021/jm00128a011 |
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Prodrugs of the selective antiherpesvirus agent 9-[4-hydroxy-3-(hydroxymethyl)but-1-yl]guanine (BRL 39123) with improved gastrointestinal absorption properties Michael R. Harnden, Richard L. Jarvest, Malcolm R. Boyd, David Sutton, and R. Anthony Vere Hodge pp 1738 - 1743; DOI: 10.1021/jm00128a012 |
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3'-Fluoro-2',3'-dideoxy-5-chlorouridine: most selective anti-HIV-1 agent among a series of new 2'- and 3'-fluorinated 2',3'-dideoxynucleoside analogs Arthur Van Aerschot, Piet Herdewijn, Jan Balzarini, Rudi Pauwels, and Erik De Clercq pp 1743 - 1749; DOI: 10.1021/jm00128a013 |
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N-Azamonobactams. 2. Synthesis of some N-iminoacetic acid and N-glycyl analogs William V. Curran and Robert H. Lenhard pp 1749 - 1753; DOI: 10.1021/jm00128a014 |
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Replacement of 3'-CH group by nitrogen in the carbocyclic analog of thymidine Kam Mui Eva Ng and Leslie E. Orgel pp 1754 - 1757; DOI: 10.1021/jm00128a015 |
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Synthesis and antirhinovirus activity of 6-(dimethylamino)-2-(trifluoromethyl)-9-(substituted benzyl)-9H-purines James L. Kelley, James A. Linn, and J. W. T. Selway pp 1757 - 1763; DOI: 10.1021/jm00128a016 |
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Nucleic acid related compounds. 57. Synthesis, x-ray crystal structure, lipophilic partition properties, and antiretroviral activities of anomeric 3'-azido-2',3'-dideoxy-2,6-diaminopurine ribosides Morris J. Robins, Steven G. Wood, N. Kent Dalley, Piet Herdewijn, Jan Balzarini, and Erik De Clercq pp 1763 - 1768; DOI: 10.1021/jm00128a017 |
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Phosphorus-31 NMR studies of the kinetics of bisalkylation by isophosphoramide mustard: comparisons with phosphoramide mustard Jila H. Boal, Margaret Williamson, Victoria L. Boyd, Susan M. Ludeman, and William Egan pp 1768 - 1773; DOI: 10.1021/jm00128a018 |
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Improved delivery through biological membranes. 38. Brain-specific chemical delivery systems for .beta.-lactam antibiotics. Synthesis and properties of some dihydropyridine and dihydroisoquinoline derivatives of benzylpenicillin Emil Pop, Whei Mei Wu, Efraim Shek, and Nicholas Bodor pp 1774 - 1781; DOI: 10.1021/jm00128a019 |
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Improved delivery through biological membranes. 39. Brain-specific chemical delivery systems for .beta.-lactam antibiotics. In vitro and in vivo studies of some dihydropyridine and dihydroisoquinoline derivatives of benzylpenicillin in rats Whei Mei Wu, Emil Pop, Efraim Shek, and Nicholas Bodor pp 1782 - 1788; DOI: 10.1021/jm00128a020 |
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Chemical delivery systems for some penicillinase-resistant semisynthetic penicillins Emil Pop, Whei Mei Wu, and Nicholas Bodor pp 1789 - 1795; DOI: 10.1021/jm00128a021 |
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A probe for octopamine receptors. Synthesis of 2-[(4-azido-2,6-diethylphenyl)imino]imidazolidine and its tritiated derivative, a potent reversible irreversible activator of octopamine-sensitive adenylate cyclase James A. Nathanson and Girts Kaugars pp 1795 - 1799; DOI: 10.1021/jm00128a022 |
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Synthesis and benzodiazepine receptor affinities of rigid analogs of 3-carboxy-.beta.-carbolines: demonstration that the benzodiazepine receptor recognizes preferentially the s-cis conformation of the 3-carboxy group Gilbert Dorey, Guillaume Poissonnet, Marie Claude Potier, Lia Prado De Carvalho, Patrice Venault, Georges Chapouthier, Jean Rossier, Pierre Potier, and Robert H. Dodd pp 1799 - 1804; DOI: 10.1021/jm00128a023 |
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9-Amino-1,2,3,4-tetrahydroacridin-1-ols. Synthesis and evaluation as potential Alzheimer's disease therapeutics Gregory M. Shutske, Frank A. Pierrat, Kevin J. Kapples, Michael L. Cornfeldt, Mark R. Szewczak, Francis P. Huger, Gina M. Bores, Vahram Haroutunian, and Kenneth L. Davis pp 1805 - 1813; DOI: 10.1021/jm00128a024 |
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Biphenylcarboxamide derivatives as antagonists of platelet-activating factor Jefferson W. Tilley, John W. Clader, Sonja Zawoiski, Maria Wirkus, Ronald A. LeMahieu, Margaret O'Donnell, Herman Crowley, and Ann F. Welton pp 1814 - 1820; DOI: 10.1021/jm00128a025 |
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Pentadienyl carboxamide derivatives as antagonists of platelet activating factor Robert W. Guthrie, Gerald L. Kaplan, Francis A. Mennona, Jefferson W. Tilley, Richard W. Kierstead, John G. Mullin, Ronald A. LeMahieu, Sonja Zawoiski, Margaret O'Donnell, and et al. pp 1820 - 1835; DOI: 10.1021/jm00128a026 |
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Differential effects of a series of hydroxamic acid derivatives on 5-lipoxygenase and cyclooxygenase from neutrophils and 12-lipoxygenase from platelets and their in vivo effects on inflammation and anaphylaxis Fu Chih Huang, T. Scott Shoupe, Clara J. Lin, Thomas D. Y. Lee, Wan Kit Chan, Jenny Tan, Melvin Schnapper, John T. Suh, Robert J. Gordon, and et al. pp 1836 - 1842; DOI: 10.1021/jm00128a027 |
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3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists Noal Cohen, Giuseppe Weber, Bruce L. Banner, Rocco J. Lopresti, Beatrice Schaer, Antonino Focella, Gladys B. Zenchoff, Anne Marie Chiu, Louis Todaro, and et al. pp 1842 - 1860; DOI: 10.1021/jm00128a028 |
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Synthesis and antiviral activity of the enantiomeric forms of carba-5-iodo-2'-deoxyuridine and carba-(E)-5-(2-bromovinyl)-2'-deoxyuridine Jan Balzarini, Harald Baumgartner, Michael Bodenteich, Erik De Clercq, and Herfried Griengl pp 1861 - 1865; DOI: 10.1021/jm00128a029 |
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New 2-substituted indoloquinone mitomycin analogs Bhashyam S. Iyengar, William A. Remers, and Joseph J. Catino pp 1866 - 1872; DOI: 10.1021/jm00128a030 |
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Sulfur-containing 1,3-dialkylxanthine derivatives as selective antagonists at A1-adenosine receptors Kenneth A. Jacobson, Leonidas Kiriasis, Suzanne Barone, Barton J. Bradbury, Udai Kammula, Jean Michel Campagne, John W. Daly, John L. Neumeyer, Wolfgang Pfleiderer, and Sherrie Secunda pp 1873 - 1879; DOI: 10.1021/jm00128a031 |
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The synthesis of acyclonucleoside hydroxamic acids as inhibitors of ribonucleotide reductase Robert A. Farr, Philippe Bey, Prasad S. Sunkara, and Bruce J. Lippert pp 1879 - 1885; DOI: 10.1021/jm00128a032 |
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(3-Amino-2-oxoalkyl)phosphonic acids and their analogs as novel inhibitors of D-alanine:D-alanine ligase Prasun K. Chakravarty, William J. Greenlee, William H. Parsons, Arthur A. Patchett, Patricia Combs, Alan Roth, Robert D. Busch, and Theodore N. Mellin pp 1886 - 1890; DOI: 10.1021/jm00128a033 |
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Synthesis and antiviral activity of several 2,5'-anhydro analogs of 3'-azido-3'-deoxythymidine (AZT), 3'-azido-2',3'-dideoxyuridine (AZU), 3'-azido-2',3'-dideoxy-5-halouridines, and 3'-deoxythymidine against human immunodeficiency virus (HIV-1) and Rauscher-Murine leukemia virus (R-MuLV) Tai Shun Lin, Zhi Yi Shen, E. Michael August, Vera Brankovan, Hyekyung Yang, Ismail Ghazzouli, and William H. Prusoff pp 1891 - 1895; DOI: 10.1021/jm00128a034 |
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On the structure selectivity problem in drug design. A comparative study of benzylpyrimidine inhibition of vertebrate and bacterial dihydrofolate reductase via molecular graphics and quantitative structure-activity relationships Cynthia Dias Selassie, Zhaoxia Fang, Renli Li, Corwin Hansch, Gargi Debnath, Teri Klein, Robert Langridge, and Bernard T. Kaufman pp 1895 - 1905; DOI: 10.1021/jm00128a035 |
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Nucleoside peptides. 10. Synthesis and T-cell immunostimulatory properties of certain peptide derivatives of 6-azacadeguomycin Kandasamy Ramasamy, Brahma S. Sharma, Weldon B. Jolley, Roland K. Robins, and Ganapathi R. Revankar pp 1905 - 1909; DOI: 10.1021/jm00128a036 |
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Ester derivatives of 2,6-bis(1-pyrrolidinylmethyl)-4-benzamidophenol as short-acting antiarrhythmic agents. 1 David M. Stout, Lawrence A. Black, Cynthia Barcelon-Yang, W. L. Matier, Barry S. Brown, Check Y. Quon, and Herman F. Stampfli pp 1910 - 1913; DOI: 10.1021/jm00128a037 |
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Synthesis and receptor affinities of some conformationally restricted analogs of the dopamine D1 selective ligand (5R)-8-chloro-2,3,4,5-tetrahydro-3-methyl-5-phenyl-1H-3-benzazepin-7-ol Joel G. Berger, Wei K. Chang, John W. Clader, Donald Hou, Richard E. Chipkin, and Andrew T. McPhail pp 1913 - 1921; DOI: 10.1021/jm00128a038 |
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N-(phthalimidoalkyl) derivatives of serotonergic agents: a common interaction at 5-HT1A serotonin binding sites? Richard A. Glennon, Noreen A. Naiman, M. Edward Pierson, J. Doyle Smith, Abd M. Ismaiel, Milt Titeler, and Robert A. Lyon pp 1921 - 1926; DOI: 10.1021/jm00128a039 |
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2,4-Diamino-5-benzylpyrimidines and analogs as antibacterial agents. 10. 2,4-Diamino-5-(6-quinolylmethyl)- and -[(tetrahydro-6-quinolyl)methyl]pyrimidine derivatives. Further specificity studies Barbara S. Rauckman, Mary Y. Tidwell, Jay V. Johnson, and Barbara Roth pp 1927 - 1935; DOI: 10.1021/jm00128a040 |
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2,4-Diamino-5-benzylpyrimidines and analogs as antibacterial agents. 11. Quinolylmethyl analogs with basic substituents conveying specificity Steven E. Davis, Barbara S. Rauckman, Joseph H. Chan, and Barbara Roth pp 1936 - 1942; DOI: 10.1021/jm00128a041 |
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2,4-Diamino-5-benzylpyrimidines and analogs as antibacterial agents. 12. 1,2-Dihydroquinolylmethyl analogs with high activity and specificity for bacterial dihydrofolate reductase Jay V. Johnson, Barbara S. Rauckman, David P. Baccanari, and Barbara Roth pp 1942 - 1949; DOI: 10.1021/jm00128a042 |
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2,4-Diamino-5-benzylpyrimidines as antibacterial agents. 13. Some alkenyl derivatives with high in vitro activity against anaerobic organisms Barbara Roth, Mary Y. Tidwell, Robert Ferone, David P. Baccanari, Carl W. Sigel, Diane DeAngelis, and Lynn P. Elwell pp 1949 - 1958; DOI: 10.1021/jm00128a043 |
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5-HT1A-Receptor antagonism: N-alkyl derivatives of (R)-(-)-8,11-dimethoxynoraporphine Joseph G. Cannon, Henry Jackson, John Paul Long, Paul Leonard, and Ranbir K. Bhatnagar pp 1959 - 1962; DOI: 10.1021/jm00128a044 |
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Synthesis and in vitro pharmacology of arpromidine and related phenyl(pyridylalkyl)guanidines, a potential new class of positive inotropic drugs Armin Buschauer pp 1963 - 1970; DOI: 10.1021/jm00128a045 |
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2-[[(4-Amino-2-pyridyl)methyl]sulfinyl]benzimidazole H+/K+-ATPase inhibitors. The relationship between pyridine basicity, stability, and activity Robert J. Ife, Catherine A. Dyke, David J. Keeling, Eugene Meenan, Malcolm L. Meeson, Michael E. Parsons, Carolyn A. Price, Colin J. Theobald, and Anthony H. Underwood pp 1970 - 1977; DOI: 10.1021/jm00128a046 |
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Cardiac glycoside-like structure and function of 5.beta.,14.beta.-pregnanes J. F. Templeton, V. P. Sashi Kumar, D. Bose, and Frank S. LaBella pp 1977 - 1981; DOI: 10.1021/jm00128a047 |
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Synthesis, biological activity, and conformational analysis of (2S,3R,4S)-MeBmt-cyclosporin, a novel 1-position epimer of cyclosporin A Daniel H. Rich, Chong Qing Sun, Dominique Guillaume, Brian Dunlap, David A. Evans, and Ann E. Weber pp 1982 - 1987; DOI: 10.1021/jm00128a048 |
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Synthesis and biological activity of novel carbacyclins having bicyclic substituents on the .omega.-chain Tsuyoshi Tomiyama, Shuichi Wakabayashi, and Masayuki Yokota pp 1988 - 1996; DOI: 10.1021/jm00128a049 |
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Alterations in the stereochemistry of the .kappa.-selective opioid agonist U50,488 result in high-affinity .sigma. ligands Brian R. De Costa, Wayne D. Bowen, Susan B. Hellewell, Clifford George, Richard B. Rothman, Audrey A. Reid, J. Michael Walker, Arthur E. Jacobson, and Kenner C. Rice pp 1996 - 2002; DOI: 10.1021/jm00128a050 |
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Lipophilic analogs of sparsomycin as strong inhibitors of protein synthesis and tumor growth: a structure-activity relationship study Leon A. G. M. Van den Broek, Ester Lazaro, Zbigniew Zylicz, Paul J. Fennis, Frank A. N. Missler, Peter Lelieveld, Marina Garzotto, D. J. Theo Wagener, Juan P. G. Ballesta, and Harry C. J. Ottenheijm pp 2002 - 2015; DOI: 10.1021/jm00128a051 |
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Water-soluble third generation antitumor platinum complexes, [2,2-bis(aminomethyl)-1,3-propanediol-N,N']-[1,1-cyclobutanedicarboxylato(2-)-O,O']platinum(II) and [1,1-cyclobutanedicarboxylato(2-)-O,O'][tetrahydro-4H-pyran-4,4-dimethanamine-N,N']platinum(II) Panayota Bitha, Suzanne G. Carvajal, Ronald V. Citarella, Ralph G. Child, Eugenia F. Delos Santos, Theresa S. Dunne, Fredrick E. Durr, Joseph J. Hlavka, S. A. Lang Jr., and et al. pp 2015 - 2020; DOI: 10.1021/jm00128a052 |
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Book Reviews pp 2021 - 2026; DOI: 10.1021/jm00128a600 |
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DNA and associated targets for drug design Laurence H. Hurley pp 2027 - 2033; DOI: 10.1021/jm00129a001 |
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(8a.alpha.,12a.alpha.,13a.alpha.)-5,8,8a,9,10,11,12,12a,13,13a,-Decahydro-3-methoxy-12-(methylsulfonyl)-6H-isoquino[2,1-g][1,6]naphthyridine, a potent and highly selective .alpha.2-adrenoceptor antagonist Robin D. Clark, David B. Repke, Andrew T. Kilpatrick, Christine M. Brown, Alison C. MacKinnon, Ruth U. Clague, and Michael Spedding pp 2034 - 2036; DOI: 10.1021/jm00129a002 |
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LH-RH antagonists: design and synthesis of a novel series of peptidomimetics Biswanath De, Jacob J. Plattner, Eugene N. Bush, Hwan Soo Jae, Gilbert Diaz, Edwin S. Johnson, and Thomas J. Perun pp 2036 - 2038; DOI: 10.1021/jm00129a003 |
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A potent, tissue-selective, synthetic inhibitor of HMG-CoA reductase N. Balasubramanian, P. J. Brown, J. D. Catt, W. T. Han, R. A. Parker, S. Y. Sit, and J. J. Wright pp 2038 - 2041; DOI: 10.1021/jm00129a004 |
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7-Heteroaryl-1,2,3,5-tetrahydroimidazol[2,1-b]quinazolin-2(1H)-one derivatives with cardiac stimulant activity Andrew S. Bell, Simon F. Campbell, David A. Roberts, and Keith S. Ruddock pp 2042 - 2049; DOI: 10.1021/jm00129a005 |
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Conformational analysis and molecular modeling of 1-phenyl-, 4-phenyl-, and 1-benzyl-1,2,3,4-tetrahydroisoquinolines as D1 dopamine receptor ligands Paul S. Charifson, J. Phillip Bowen, Steven D. Wyrick, Andrew J. Hoffman, Michael Cory, Andrew T. McPhail, and Richard B. Mailman pp 2050 - 2058; DOI: 10.1021/jm00129a006 |
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Synthesis and anthelmintic activity of a series of of pyrazino[2,1-a][2]benzazepine derivatives Malcolm D. Brewer, Malcolm N. Burgess, Roderick J. J. Dorgan, Richard L. Elliott, Patrick Mamalis, Brian R. Manger, and Richard A. B. Webster pp 2058 - 2062; DOI: 10.1021/jm00129a007 |
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A new family of water-soluble, third-generation antitumor platinum complexes Panayota Bitha, Suzanne G. Carvajal, Ronald V. Citarella, Eugenia F. Delos Santos, Fredrick E. Durr, Joseph J. Hlavka, S. A. Lang Jr., Harry L. Lindsay, John P. Thomas, and et al. pp 2063 - 2067; DOI: 10.1021/jm00129a008 |
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Opioid agonist and antagonist activities of peripherally selective derivatives of naltrexamine and oxymorphamine S. Botros, A. W. Lipkowski, D. L. Larson, P. A. Stark, A. E. Takemori, and Phillip S. Portoghese pp 2068 - 2071; DOI: 10.1021/jm00129a009 |
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Synthesis and hypolipidemic and antidiabetogenic activities of .beta.,.beta.,.beta.',.beta.'-tetrasubstituted, long-chain dioic acids Jacob Bar-Tana, Shoshana Ben-Shoshan, Jochanan Blum, Yoelit Migron, Rachel Hertz, Johannes Pill, Gene Rose-Kahn, and Ernst Christian Witte pp 2072 - 2084; DOI: 10.1021/jm00129a010 |
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Design of potential anti-HIV agents. 1. Mannosidase inhibitors David A. Winkler and George Holan pp 2084 - 2089; DOI: 10.1021/jm00129a011 |
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New anticancer agents: chiral isomers of ethyl 5-amino-1,2-dihydro-2-methyl-3-phenylpyrido[3,4-b]pyrazine-7-carbamate Carroll Temple and Gregory A. Rener pp 2089 - 2092; DOI: 10.1021/jm00129a012 |
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Effect of triphenylacrylonitrile derivatives on estradiol-receptor binding and on human breast cancer cell growth Eric Bignon, Michel Pons, Andre Crastes de Paulet, Jean Christophe Dore, Jacques Gilbert, Josephine Abecassis, Jean Francois Miquel, Tiiu Ojasoo, and Jean Pierre Raynaud pp 2092 - 2103; DOI: 10.1021/jm00129a013 |
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Iodoaryl analogs of dioctanoylglycerol and 1-oleoyl-2-acetylglycerol as probes for protein kinase C Laurie M. Strawn, Robert E. Martell, Robert U. Simpson, Karen L. Leach, and Raymond E. Counsell pp 2104 - 2110; DOI: 10.1021/jm00129a014 |
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Carbohydrate biguanides as potential hypoglycemic agents. Allen B. Reitz, Robert W. Tuman, Carol S. Marchione, Alfonzo D. Jordan, Charles R. Bowden, and Bruce E. Maryanoff pp 2110 - 2116; DOI: 10.1021/jm00129a015 |
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Evaluation and synthesis of amino-hydroxy isoxazoles and pyrazoles as potential glycine agonists J. Drummond, G. Johnson, D. G. Nickell, D. F. Ortwine, R. F. Bruns, and B. Welbaum pp 2116 - 2128; DOI: 10.1021/jm00129a016 |
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Synthesis and evaluation of N,N-di-n-propyltetrahydrobenz[f]indol-7-amine and related congeners as dopaminergic agonists David E. Nichols, John M. Cassady, Paul E. Persons, Ming C. Yeung, James A. Clemens, and E. Barry Smalstig pp 2128 - 2134; DOI: 10.1021/jm00129a017 |
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Synthesis and biological evaluation of 4,6-diethyl-1,3,4,5-tetrahydropyrano[4,3-b]indole-4-acetic acid, an isomer of etodolac Philip Hughes, John DeVirgilio, Leslie G. Humber, Chau Thuy, Barry Weichman, and Glen Neuman pp 2134 - 2137; DOI: 10.1021/jm00129a018 |
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2-(Fluoromethyl)-3-phytyl-1,4-naphthoquinone and its 2,3-epoxide. Inhibition of vitamin K epoxide reductase Richard B. Silverman and John S. Oliver pp 2138 - 2141; DOI: 10.1021/jm00129a019 |
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Potential tumor or organ-imaging agents. 30. Radioiodinated phospholipid ethers Karen L. Meyer, Susan W. Schwendner, and Raymond E. Counsell pp 2142 - 2147; DOI: 10.1021/jm00129a020 |
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Polyfluoro 1,3-diketones as systemic insecticides G. D. Crouse, M. J. McGowan, and R. J. Boisvenue pp 2148 - 2151; DOI: 10.1021/jm00129a021 |
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Squalene analogs containing isopropylidene mimics as potential inhibitors of pig liver squalene epoxidase and oxidosqualene cyclase Stephanie E. Sen and Glenn D. Prestwich pp 2152 - 2158; DOI: 10.1021/jm00129a022 |
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In vitro metabolic transformations of vinblastine: oxidations catalyzed by human ceruloplasmin Sayed A. Elmarakby, Michael W. Duffel, and John P. N. Rosazza pp 2158 - 2162; DOI: 10.1021/jm00129a023 |
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2-Arylindenes and 2-arylindenones: molecular structures and considerations in the binding orientation of unsymmetrical nonsteroidal ligands to the estrogen receptor Gregory M. Anstead, Scott R. Wilson, and John A. Katzenellenbogen pp 2163 - 2171; DOI: 10.1021/jm00129a024 |
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4-(Phosphonoalkyl)- and 4-(phosphonoalkenyl)-2-piperidinecarboxylic acids: synthesis, activity at N-methyl-D-aspartic acid receptors and anticonvulsant activity Alan J. Hutchison, Michael Williams, Christoff Angst, Reynalda De Jesus, Louis Blanchard, Robert H. Jackson, E. Jay Wilusz, Deborah E. Murphy, Patrick S. Bernard, and et al. pp 2171 - 2178; DOI: 10.1021/jm00129a025 |
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Benzo- and pyrido-1,4-oxazepin-5-ones and -thiones: synthesis and structure-activity relationships of a new series of H1-antihistamines Albert D. Cale, Thomas W. Gero, Kathleen R. Walker, Young S. Lo, William J. Welstead, Larry W. Jaques, Ashby F. Johnson, Charles A. Leonard, Joseph C. Nolan, and David N. Johnson pp 2178 - 2199; DOI: 10.1021/jm00129a026 |
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Synthesis and biological activity of photoactive derivatives of erythromycin M. Angeles Arevalo, Francisco Tejedor, Florentino Polo, and J. P. G. Ballesta pp 2200 - 2204; DOI: 10.1021/jm00129a027 |
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Synthesis and biological activity of 3-substituted imidazo[1,2-a]pyridines as antiulcer agents John E. Starrett, Thomas A. Montzka, Alfred R. Crosswell, and Robert L. Cavanagh pp 2204 - 2210; DOI: 10.1021/jm00129a028 |
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Introduction of a putative dopaminergic prodrug moiety into a 6,7-substitution pattern characteristic of certain 2-aminotetralin dopaminergic agonists Joseph G. Cannon, Claire Diane True, John Paul Long, Ranbir K. Bhatnagar, Paul Leonard, and Jan R. Flynn pp 2210 - 2214; DOI: 10.1021/jm00129a029 |
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Quinones. 4. Novel eicosanoid antagonists: synthesis and pharmacological evaluation Mitsuru Shiraishi, Kaneyoshi Kato, Shinji Terao, Yasuko Ashida, Zenichi Terashita, and Go Kito pp 2214 - 2221; DOI: 10.1021/jm00129a030 |
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Benzofuro[2,3-c]pyridin-6-ols: synthesis, affinity for opioid-receptor subtypes, and antinociceptive activity Alan J. Hutchison, Reynalda De Jesus, Michael Williams, John P. Simke, Robert F. Neale, Robert H. Jackson, Francis Ambrose, Beverly J. Barbaz, and Matthew A. Sills pp 2221 - 2226; DOI: 10.1021/jm00129a031 |
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Book Reviews pp 2227 - 2230; DOI: 10.1021/jm00129a600 |
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Is there a case for P-450 inhibitors in cancer treatment? Jean P. Van Wauwe and Paul A. J. Janssen pp 2231 - 2239; DOI: 10.1021/jm00130a001 |
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Cytostatic trans-platinum(II) complexes Nicholas Farrell, Tam T. B. Ha, Jean Pierre Souchard, Franz L. Wimmer, Suzy Cros, and Neil P. Johnson pp 2240 - 2241; DOI: 10.1021/jm00130a002 |
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5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity Giuseppe Cascio, Elso Manghisi, and Giancarlo Fregnan pp 2241 - 2247; DOI: 10.1021/jm00130a003 |
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Linear and proximal benzo-separated alkylated xanthines as adenosine-receptor antagonists Stewart W. Schneller, Augusto C. Ibay, William J. Christ, and Robert F. Bruns pp 2247 - 2254; DOI: 10.1021/jm00130a004 |
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Excitatory amino acid agonists. Enzymic resolution, x-ray structure, and enantioselective activities of (R)- and (S)-bromohomoibotenic acid Jan J. Hansen, Birgitte Nielsen, Povl Krogsgaard-Larsen, Lotte Brehm, Elsebet O. Nielsen, and David R. Curtis pp 2254 - 2260; DOI: 10.1021/jm00130a005 |
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Sterically hindered 5,11-dicarbo analogs of clozapine as potential chiral antipsychotic agents J. Howard Rupard, Tomas De Paulis, Aaron Janowsky, and Howard E. Smith pp 2261 - 2268; DOI: 10.1021/jm00130a006 |
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Enantioselectivity of muscarinic antagonists. Isomeric 2-cyclohexyl-2-phenyl-5-[(dimethylamino)methyl]-1,3-oxathiolane 3-oxide methiodides M. Novella Romanelli, F. Gualtieri, P. Angeli, and M. Teresa Picchio pp 2269 - 2273; DOI: 10.1021/jm00130a007 |
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Resolved 6,7,8,9-tetrahydro-N,N-dimethyl-3H-benz[e]indol-8-amine: central dopamine and serotonin receptor stimulating properties Haakan Wikstroem, Bengt Andersson, Arne Svensson, Leslie G. Humber, Andre A. Asselin, Kjell Svensson, Agneta Ekman, Arvid Carlsson, Ingemar Nilsson, and Connie Chidester pp 2273 - 2276; DOI: 10.1021/jm00130a008 |
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Synthesis and biological evaluation of substituted benzo[h]cinnolinones and 3H-benzo[6,7]cyclohepta[1,2-c]pyridazinones: higher homologs of the antihypertensive and antithrombotic 5H-indeno[1,2-c]pyridazinones Giorgio Cignarella, Daniela Barlocco, Gerard A. Pinna, Mario Loriga, Maria M. Curzu, Odoardo Tofanetti, Mauro Germini, Pietro Cazzulani, and Ennio Cavalletti pp 2277 - 2282; DOI: 10.1021/jm00130a009 |
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Novel benzodiazepine receptor partial agonists: oxadiazolylimidazobenzodiazepines Frank Watjen, Raymond Baker, Mogens Engelstoff, Richard Herbert, Angus MacLeod, Anthony Knight, Kevin Merchant, Jonathan Moseley, John Saunders, and et al. pp 2282 - 2291; DOI: 10.1021/jm00130a010 |
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Retinobenzoic acids. 4. Conformation of aromatic amides with retinoidal activity. Importance of trans-amide structure for the activity Hiroyuki Kagechika, Toshiyuki Himi, Emiko Kawachi, and Koichi Shudo pp 2292 - 2296; DOI: 10.1021/jm00130a011 |
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Syntheses and bioevaluation of substituted dihydropyridines for pregnancy-interceptive activity in hamsters Anita Mukherjee, Mohammad S. Akhtar, Vishnu L. Sharma, Manju Seth, Amiya P. Bhaduri, Anila Agnihotri, Purshottam K. Mehrotra, and Ved Prakash Kamboj pp 2297 - 2300; DOI: 10.1021/jm00130a012 |
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Oral hypoglycemic agents. Discovery and structure-activity relationships of phenacylimidazolium halides Samuel J. Dominianni and Terence T. Yen pp 2301 - 2306; DOI: 10.1021/jm00130a013 |
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11.beta.-Nitrate estrane analogs: potent estrogens Richard H. Peters, David F. Crowe, Mitchell A. Avery, Wesley K. M. Chong, and Masato Tanabe pp 2306 - 2310; DOI: 10.1021/jm00130a014 |
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(R)- and (S)-5,6,7,8-Tetrahydro-1-hydroxy-N,N-dipropyl-9H-benzocyclohepten-8-ylamine. Stereoselective interactions with 5-HT1A-receptors in the brain Ye Liu, Charlotta Mellin, Lena Bjoerk, Bjoern Svensson, Ingeborg Csoeregh, Anne Helander, Lennart Kenne, Nils Erik Anden, and Uli Hacksell pp 2311 - 2318; DOI: 10.1021/jm00130a015 |
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Potential antiatherosclerotic agents. 6. Hypocholesterolemic trisubstituted urea analogs Vern G. DeVries, Jonathan D. Bloom, Minu D. Dutia, Andrew S. Katocs, and Elwood E. Largis pp 2318 - 2325; DOI: 10.1021/jm00130a016 |
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Boron neutron capture therapy: linkage of a boronated macromolecule to monoclonal antibodies directed against tumor-associated antigens Fazlul Alam, Albert H. Soloway, Rolf F. Barth, Naoki Mafune, Dianne M. Adams, and Walter H. Knoth pp 2326 - 2330; DOI: 10.1021/jm00130a017 |
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Synthesis and biological activity of some partially modified retro-inverso analogs of cholecystokinin Marc Rodriguez, Marie Christine Galas, Marie Francoise Lignon, Christiane Mendre, Jeanine Laur, Andre Aumelas, and Jean Martinez pp 2331 - 2339; DOI: 10.1021/jm00130a018 |
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Active reduced-size hexapeptide analogs of luteinizing hormone-releasing hormone Fortuna Haviv, Christopher A. Palabrica, Eugene N. Bush, Gilbert Diaz, Edwin S. Johnson, Stephen Love, and Jonathan Greer pp 2340 - 2344; DOI: 10.1021/jm00130a019 |
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Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors Aviv Gazit, Pnina Yaish, Chaim Gilon, and Alexander Levitzki pp 2344 - 2352; DOI: 10.1021/jm00130a020 |
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Synthesis and investigation of effects of 2-[4-[[(arylamino)carbonyl]amino]phenoxy]-2-methylpropionic acids on the affinity of hemoglobin for oxygen: structure-activity relationships Iraj Lalezari and Parviz Lalezari pp 2352 - 2357; DOI: 10.1021/jm00130a021 |
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The xanthene-9-spiro-4'-piperidine nucleus as a probe for opiate activity Ronald H. B. Galt, John Horbury, Zbigniew S. Matusiak, Robert J. Pearce, and John S. Shaw pp 2357 - 2362; DOI: 10.1021/jm00130a022 |
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New anticancer agents: alterations of the carbamate group of ethyl (5-amino-1,2-dihydro-3-phenylpyrido[3,4-b]pyrazin-7-yl)carbamates Carroll Temple, Gregory A. Rener, and Robert N. Comber pp 2363 - 2367; DOI: 10.1021/jm00130a023 |
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Novel linked antiviral and antitumor agents related to netropsin and distamycin: synthesis and biological evaluation J. William Lown, Krzysztof Krowicki, Jan Balzarini, Robert A. Newman, and Erik De Clercq pp 2368 - 2375; DOI: 10.1021/jm00130a024 |
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Heteroarenobenzodiazepines. 6. Synthesis and pharmacological evaluation of CNS activities of [1,2,3]triazolo[4,5-b][1,5]-, imidazolo[4,5,-b][1,5]-, and pyrido[2,3-b][1,5]benzodiazepines. 10-Piperazinyl-4H-1,2,3-triazolo[4,5-b][1,5]benzodiazepines with neuroleptic activity Jiban K. Chakrabarti, Terrence M. Hotten, Ian A. Pullar, and David J. Steggles pp 2375 - 2381; DOI: 10.1021/jm00130a025 |
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Long-acting dihydropyridine calcium antagonists. 3. Synthesis and structure-activity relationships for a series of 2-[(heterocyclylmethoxy)methyl] derivatives David Alker, Simon F. Campbell, Peter E. Cross, Roger A. Burges, Anthony J. Carter, and Donald G. Gardiner pp 2381 - 2388; DOI: 10.1021/jm00130a026 |
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Substituted 5-amino-4,5,6,7-tetrahydroindazoles as partial ergoline structures with dopaminergic activity Loretta A. McQuaid, Jane E. Latz, James A. Clemens, Ray W. Fuller, David T. Wong, and Norman R. Mason pp 2388 - 2396; DOI: 10.1021/jm00130a027 |
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Quantitative structure-activity relationships in dihydropteroate synthase inhibition by multisubstituted sulfones. Design and synthesis of some new derivatives with improved potency Pier G. De Benedetti, Dario Iarossi, Ugo Folli, Chiara Frassineti, Maria Cristina Menziani, and Carlo Cennamo pp 2396 - 2399; DOI: 10.1021/jm00130a028 |
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Dihydropyrimidines: novel calcium antagonists with potent and long-lasting vasodilative and anti-hypertensive activity Hidetsura Cho, Masaru Ueda, Keiyuu Shima, Akira Mizuno, Mariko Hayashimatsu, Yoshiko Ohnaka, Yumi Takeuchi, Mikiko Hamaguchi, Kazuo Aisaka, and et al. pp 2399 - 2406; DOI: 10.1021/jm00130a029 |
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Tetrapeptide inhibitors of the IgA1 proteinases from type I Neisseria gonorrhoeae Stephen G. Wood, Mary Lynch, Andrew G. Plaut, and James Burton pp 2407 - 2411; DOI: 10.1021/jm00130a030 |
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Book Reviews pp 2411 - 2412; DOI: 10.1021/jm00130a600 |
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Design of potential anticonvulsant agents: mechanistic classification of GABA aminotransferase inactivators Shrenik M. Nanavati and Richard B. Silverman pp 2413 - 2421; DOI: 10.1021/jm00131a001 |
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Synthesis and antitubercular activity of N-(2-naphthyl)glycine hydrazide analogs B. Ramamurthy and M. V. Bhatt pp 2421 - 2426; DOI: 10.1021/jm00131a002 |
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Synthesis of methotrexate-antibody conjugates by regiospecific coupling and assessment of drug and antitumor activities J. Kralovec, G. Spencer, A. H. Blair, M. Mammen, M. Singh, and T. Ghose pp 2426 - 2431; DOI: 10.1021/jm00131a003 |
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Photoaffinity, biotinyl, and iodo analogs as probes for vasotocin receptors Angeliki Buku, Diana Gazis, and Patrick Eggena pp 2432 - 2435; DOI: 10.1021/jm00131a004 |
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3-Sulfonyl-1-carba-1-dethiacephems Thomas A. Crowell, Basil D. Halliday, John H. McDonald, Joseph M. Indelicato, Carol E. Pasini, and Ernie C. Y. Wu pp 2436 - 2442; DOI: 10.1021/jm00131a005 |
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3-Quaternary ammonium 1-carba-1-dethiacephems Gwendolyn K. Cook, John H. McDonald, III, William Alborn Jr., Donald B. Boyd, Judy A. Eudaly, Joseph M. Indelicato, Rod Johnson, Jeffrey S. Kasher, Carol E. Pasini, and et al. pp 2442 - 2450; DOI: 10.1021/jm00131a006 |
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Synthesis and biological properties of N63-carboxamides of teicoplanin antibiotics. Structure-activity relationships Adriano Malabarba, Aldo Trani, Paolo Strazzolini, Giuseppe Cietto, Pietro Ferrari, Giorgio Tarzia, Rosa Pallanza, and Marisa Berti pp 2450 - 2460; DOI: 10.1021/jm00131a007 |
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Design, synthesis, and testing of potential antisickling agents. 7. Ethacrynic acid analogs D. J. Abraham, A. S. Mehanna, F. S. Williams, E. J. Cragoe, and O. W. Woltersdorf pp 2460 - 2467; DOI: 10.1021/jm00131a008 |
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Structural studies on bioactive compounds. 8. Synthesis, crystal structure and biological properties of a new series of 2,4-diamino-5-aryl-6-ethylpyrimidine dihydrofolate reductase inhibitors with in vivo activity against a methotrexate-resistant tumor cell line Roger J. Griffin, Michelle A. Meek, Carl H. Schwalbe, and Malcolm F. G. Stevens pp 2468 - 2474; DOI: 10.1021/jm00131a009 |
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Pyrido[3,4-e]-1,2,4-triazines and related heterocycles as potential antifungal agents Marvin F. Reich, Paul F. Fabio, Ving J. Lee, Nydia A. Kuck, and Ray T. Testa pp 2474 - 2485; DOI: 10.1021/jm00131a010 |
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Topically active carbonic anhydrase inhibitors. 1. O-Acyl derivatives of 6-hydroxybenzothiazole-2-sulfonamide O. W. Woltersdorf Jr., H. Schwam, J. B. Bicking, S. L. Brown, S. J. DeSolms, D. R. Fishman, S. L. Graham, P. D. Gautheron, J. M. Hoffman, and et al. pp 2486 - 2492; DOI: 10.1021/jm00131a011 |
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Orally active aldose reductase inhibitors derived from bioisosteric substitutions on tolrestat Jay Wrobel, Jane Millen, Janet Sredy, Arlene Dietrich, Joseph M. Kelly, Beverly J. Gorham, and Kazimir Sestanj pp 2493 - 2500; DOI: 10.1021/jm00131a012 |
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Book Reviews pp 2500 - 2502; DOI: 10.1021/jm00131a600 |
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A novel solution-stable, water-soluble prodrug type for drugs containing a hydroxyl or an NH-acidic group Hans Bundgaard, Erik Falch, and Ejvind Jensen pp 2503 - 2507; DOI: 10.1021/jm00132a001 |
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A novel lead for specific anti-HIV-1 agents: 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine Tadashi Miyasaka, Hiromichi Tanaka, Masanori Baba, Hiroyuki Hayakawa, Richard T. Walker, Jan Balzarini, and Erik De Clercq pp 2507 - 2509; DOI: 10.1021/jm00132a002 |
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Thienothiopyran-2-sulfonamides: novel topically active carbonic anhydrase inhibitors for the treatment of glaucoma John J. Baldwin, Gerald S. Ponticello, Paul S. Anderson, Marcia E. Christy, Mark A. Murcko, William C. Randall, Harvey Schwam, Michael F. Sugrue, Pierre Gautheron, and et al. pp 2510 - 2513; DOI: 10.1021/jm00132a003 |
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Specific inhibition of benzodiazepine receptor binding by some N-(indol-3-ylglyoxylyl) amino acid derivatives: stereoselective interactions Giampaolo Primofiore, Anna M. Marini, Federico Da Settimo, Claudia Martini, Anna Bardellini, Gino Giannaccini, and Antonio Lucacchini pp 2514 - 2518; DOI: 10.1021/jm00132a004 |
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Enkephalinase inhibitors. 1. 2,4-Dibenzylglutaric acid derivatives Gary M. Ksander, Clive G. Diefenbacher, Andrew M. Yuan, F. Clark, Yumi Sakane, and R. D. Ghai pp 2519 - 2526; DOI: 10.1021/jm00132a005 |
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Derivatives of tamoxifen. Dependence of antiestrogenicity on the 4-substituent Raymond McCague, Guy Leclercq, Nicole Legros, Joyce Goodman, G. Michael Blackburn, Michael Jarman, and Allan B. Foster pp 2527 - 2533; DOI: 10.1021/jm00132a006 |
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4-Phenyl- and 4-heteroaryl-4-anilidopiperidines. A novel class of analgesic and anesthetic agents Linas V. Kudzma, Sherry A. Severnak, Mark J. Benvenga, Edward F. Ezell, Michael H. Ossipov, Valerie V. Knight, Frieda G. Rudo, H. Kenneth Spencer, and Theodore C. Spaulding pp 2534 - 2542; DOI: 10.1021/jm00132a007 |
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Selective elimination of interactions: a method for assessing thermodynamic contributions to ligand binding with application to rhinovirus antivirals Wan F. Lau and B. Montgomery Pettitt pp 2542 - 2547; DOI: 10.1021/jm00132a008 |
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Topically active carbonic anhydrase inhibitors. 2. Benzo[b]thiophenesulfonamide derivatives with ocular hypotensive activity Samuel L. Graham, Kenneth L. Shepard, Paul S. Anderson, John J. Baldwin, Darryl B. Best, Marcia E. Christy, Mark B. Freedman, Pierre Gautheron, Charles N. Habecker, and et al. pp 2548 - 2554; DOI: 10.1021/jm00132a009 |
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Potent and prolonged-acting cyclic lactam analogs of .alpha.-melanotropin: design based on molecular dynamics Fahad Al-Obeidi, Ana M. de L. Castrucci, Mac E. Hadley, and Victor J. Hruby pp 2555 - 2561; DOI: 10.1021/jm00132a010 |
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Synthesis and structure-activity relationships of a series of anxioselective pyrazolopyridine ester and amide anxiolytic agents Thomas M. Bare, Charles D. McLaren, James B. Campbell, Judy W. Firor, James F. Resch, Claudia P. Walters, Andre I. Salama, Brad A. Meiners, and Jitendra B. Patel pp 2561 - 2573; DOI: 10.1021/jm00132a011 |
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Heteroarenobenzodiazepines. Part 7. Synthesis and pharmacological evaluation of a series of 4-piperazinylpyrazolo[3,4-b] and [4,3-b][1,5]benzodiazepines as potential anxiolytics Jiban K. Chakrabarti, Terrence M. Hotten, Ian A. Pullar, and Nicholas C. Tye pp 2573 - 2582; DOI: 10.1021/jm00132a012 |
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Bis(4-hydroxyphenyl) [2-(phenoxysulfonyl)phenyl]methane: isolation and structure elucidation of a novel estrogen from commercial preparations of phenol red (phenolsulfonphthalein) [Erratum to document cited in CA109(15):128488b] Rajeshwar D. Bindal and John A. Katzenellenbogen pp 2582 - 2582; DOI: 10.1021/jm00132a013 |
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Etodolac, a novel antiinflammatory agent. The syntheses and biological evaluation of its metabolites [Erratum to document cited in CA109(11):92846a] Leslie G. Humber, Eckhardt Ferdinandi, Christopher A. Demerson, Syed Ahmed, Uresh Shah, Dominick Mobilio, Joseph Sabatucci, Barbara De Lange, Francesco Labbadia, and et al. pp 2582 - 2582; DOI: 10.1021/jm00132a014 |
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Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 3. Guanidines [Erratum to document cited in CA106(19):156365r] Christopher B. Chapleo, Peter L. Myers, Alan C. B. Smith, Ian F. Tulloch, Stephen Turner, and Donald S. Walter pp 2582 - 2582; DOI: 10.1021/jm00132a015 |
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Methotrexate analogs. 31. Meta and ortho isomers of aminopterin, compounds with a double bond in the side chain, and a novel analog modified at the .alpha.-carbon: chemical and in vitro biological studies [Erratum to document cited in CA109(1):6923u] Andre Rosowsky, Henry Bader, Ronald A. Forsch, Richard G. Moran, and James H. Freisheim pp 2582 - 2582; DOI: 10.1021/jm00132a016 |
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Thromboxane A2 synthetase inhibitors. 2. Syntheses and activities of tetrahydronaphthalene and indane derivatives [Erratum to document cited in CA110(25):231524e] Munefumi Kanao, Yoshifumi Watanabe, Youichi Kimura, Junji Saegusa, Kenjiro Yamamoto, Hideyuki Kanno, Naoaki Kanaya, Hideo Kubo, Shinichiro Ashida, and Fumiyoshi Ishikawa pp 2583 - 2583; DOI: 10.1021/jm00132a017 |
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Hybrid cholecystokinin (CCK) antagonists: new implications in the design and modification of CCK antagonists [Erratum to document cited in CA110(19):165531b] James F. Kerwin, Alex M. Nadzan, Hana Kopecka, Chun Wel Lin, Thomas Miller, David Witte, and Stanley Burt pp 2583 - 2583; DOI: 10.1021/jm00132a018 |
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A multisubstrate adduct inhibitor of a purine biosynthetic enzyme with a picomolar dissociation constant [Erratum to document cited in CA110(21):193361q] James Inglese, Richard A. Blatchly, and Stephen J. Benkovic pp 2583 - 2583; DOI: 10.1021/jm00132a019 |
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Exploration of phenyl-spaced 2-amino-(5-9)-phosphonoalkanoic acids as competitive N-methyl-D-aspartic acid antagonists [Erratum to document cited in CA111(3):23931d] Christopher F. Bigge, James T. Drummond, Graham Johnson, Thomas Malone, Albert W. Probert, Frank W. Marcoux, Linda L. Coughenour, and Laura J. Brahce pp 2583 - 2583; DOI: 10.1021/jm00132a020 |
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A new series of tricyclic (aryloximino)propanolamines displaying very high selective .beta.2-blocking properties [Erratum to document cited in CA110(7):57277q] Brigitte Jamart-Gregoire, Paul Caubere, Marie Blanc, Jean Pierre Gnassounou, and Charles Advenier pp 2583 - 2583; DOI: 10.1021/jm00132a021 |
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Synthesis, DNA-binding properties, and antitumor activity of novel distamycin derivatives [Erratum to document cited in CA110(19):173740j] Federico Maria Arcamone, Fabio Animati, Brunella Barbieri, Emanuela Configliacchi, Roberto D'Alessio, Cristina Geroni, Fernando Carlo Giuliani, Ettore Lazzari, Milena Menozzi, and et al. pp 2583 - 2583; DOI: 10.1021/jm00132a022 |
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Retinobenzoic acids. 1. Structure-activity relationships of aromatic amides with retinoidal activity [Erratum to document cited in CA110(3):23483p] Hiroyuki Kagechika, Emiko Kawachi, Yuichi Hashimoto, Koichi Shudo, and Toshiyuki Himi pp 2583 - 2583; DOI: 10.1021/jm00132a023 |
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Book Reviews pp 2584 - 2588; DOI: 10.1021/jm00132a600 |