Aldose reductase inhibitors: a potential new class of agents for the pharmacological control of certain diabetic complications Peter F. Kador, Jin H. Kinoshita, and Norman E. Sharpless pp 841 - 849; DOI: 10.1021/jm00145a001 |
A computational procedure for determining energetically favorable binding sites on biologically important macromolecules P. J. Goodford pp 849 - 857; DOI: 10.1021/jm00145a002 |
Comparative computer graphics and solution studies of the DNA interaction of substituted anthraquinones based on doxorubicin and mitoxantrone Suhail A. Islam, Stephen Neidle, Bijukumar M. Gandecha, Malcolm Partridge, Laurence H. Patterson, and Jeffrey R. Brown pp 857 - 864; DOI: 10.1021/jm00145a003 |
Solubility properties in polymers and biological media. 2. The correlation and prediction of the solubilities of nonelectrolytes in biological tissues and fluids Michael H. Abraham, Mortimer J. Kamlet, R. W. Taft, Ruth M. Doherty, and Paul K. Weathersby pp 865 - 870; DOI: 10.1021/jm00145a004 |
Tetracyclic pyridazines as potential psychopharmacological agents Bruce S. Ross and Robert A. Wiley pp 870 - 875; DOI: 10.1021/jm00145a005 |
Antiulcer agents. 1. Gastric antisecretory and cytoprotective properties of substituted imidazo[1,2-a]pyridines James J. Kaminski, James A. Bristol, Chester Puchalski, Raymond G. Lovey, Arthur J. Elliott, Henry Guzik, Daniel M. Solomon, David J. Conn, Martin S. Domalski, and et al. pp 876 - 892; DOI: 10.1021/jm00145a006 |
Psychotomimetic N-methyl-N-isopropyltryptamines. Effects of variation of aromatic oxygen substituents David B. Repke, Douglas B. Grotjahn, and Alexander T. Shulgin pp 892 - 896; DOI: 10.1021/jm00145a007 |
New chiral and isomeric cyclopropyl ketoxime propanolamine derivatives with potent .beta.-adrenergic blocking properties Mohamed Bouzoubaa, Gerard Leclerc, Suman Rakhit, and Guy Andermann pp 896 - 900; DOI: 10.1021/jm00145a008 |
Effects of alkyl and aryl substitution on the myocardial specificity of radioiodinated phosphonium, arsonium, and ammonium cations P. C. Srivastava, H. G. Hay, and F. F. Knapp pp 901 - 904; DOI: 10.1021/jm00145a009 |
Synthesis and biological activities of 2-pyrimidinone nucleosides. 2. 5-Halo-2-pyrimidinone 2'-deoxyribosides Simon M. N. Efange, Elaine M. Alessi, H. C. Shih, Yung Chi Cheng, and Thomas J. Bardos pp 904 - 910; DOI: 10.1021/jm00145a010 |
N-[[(Mercaptoacetyl)amino]benzoyl]glycines mucolytic agents Tellis A. Martin and William T. Comer pp 910 - 914; DOI: 10.1021/jm00145a011 |
Synthesis of the antileukemic agents 5,10-dideazaaminopterin and 5,10-dideaza-5,6,7,8-tetrahydroaminopterin Edward C. Taylor, Peter J. Harrington, Stephen R. Fletcher, G. Peter Beardsley, and Richard G. Moran pp 914 - 921; DOI: 10.1021/jm00145a012 |
Synthesis and biological activity of 6-substituted mitosene analogs of the mitomycins Michael L. Casner, William A. Remers, and William T. Bradner pp 921 - 926; DOI: 10.1021/jm00145a013 |
Synthesis and antiherpetic activity of (S)-, (R)-, and (.+-.)-9-[(2,3-dihydroxy-1-propoxy)methyl]guanine, linear isomers of 2'-nor-2'-deoxyguanosine Wallace T. Ashton, Laura F. Canning, Glenn F. Reynolds, Richard L. Tolman, John D. Karkas, Richard Liou, Mary Ellen M. Davies, Corrille M. DeWitt, Helen C. Perry, and A. Kirk Field pp 926 - 933; DOI: 10.1021/jm00145a014 |
Synthesis, in vitro [3H]prazosin displacement, and in vivo activity of 3-aryl-4,5,6,7-tetrahydropyrazolo[4,3-c]pyridines, a new class of antihypertensive agents Giorgio Winters, Alberto Sala, Domenico Barone, and Emiliana Baldoli pp 934 - 940; DOI: 10.1021/jm00145a015 |
The intercalation of 6-chloro-2-substituted-9-[[3-(dimethylamino)propyl]amino]acridines with DNA S. E. Kitchen, Yuehhwa Wang, A. L. Baumstark, W. D. Wilson, and David W. Boykin pp 940 - 944; DOI: 10.1021/jm00145a016 |
Bioactive conformation of 1-arylpiperazines at central serotonin receptors Joel R. Huff, Stella W. King, Walfred S. Saari, J. P. Springer, Gregory E. Martin, and Michael Williams pp 945 - 948; DOI: 10.1021/jm00145a017 |
Opioid agonists and antagonists. 6-Desoxy-6-substituted lactone, epoxide, and glycidate ester derivatives of naltrexone and oxymorphone Gary A. Koolpe, Wendel L. Nelson, T. L. Gioannini, Lloyd Angel, Nicholas Appelmans, and Eric J. Simon pp 949 - 957; DOI: 10.1021/jm00145a018 |
Reductive amination of C-3-ketoanguidin and antitumor activity of the products T. Kaneko, H. Wong, H. G. Howell, W. C. Rose, W. T. Bradner, and T. W. Doyle pp 958 - 960; DOI: 10.1021/jm00145a019 |
4-Deoxypyrido[1',2':1,2]imidazo[5,4-c]rifamycin SV derivatives. A new series of semisynthetic rifamycins with high antibacterial activity and low gastroenteric absorption Egidio Marchi, Giuseppe Mascellani, Laura Montecchi, Anna Paolo Venturini, Mario Brufani, and Luciano Cellai pp 960 - 963; DOI: 10.1021/jm00145a020 |
A comparison of mechanisms proposed for the conversion of mitomycins into mitosenes Bhashyam S. Iyengar and William A. Remers pp 963 - 967; DOI: 10.1021/jm00145a021 |
Improved antagonists of luteinizing hormone-releasing hormone modified in position 7 Simon J. Hocart, Mary V. Nekola, and David H. Coy pp 967 - 970; DOI: 10.1021/jm00145a022 |
Synthesis of 1-[[2-hydroxy-1-(hydroxymethyl)ethoxy]methyl]-5-benzyluracil and its amino analog new potent uridine phosphorylase inhibitors with high water solubility Tai Shun Lin and Mao Chin Liu pp 971 - 973; DOI: 10.1021/jm00145a023 |
10-Ketonaltrexone and 10-ketooxymorphone Sydney Archer, Ahmad Seyed-Mozaffari, Susan Ward, Hans W. Kosterlitz, Stewart J. Paterson, Alexander T. McKnight, and Alistair D. Corbett pp 974 - 976; DOI: 10.1021/jm00145a024 |
Book Reviews pp 976 - 978; DOI: 10.1021/jm00145a600 |
Pilocarpic acid esters as novel sequentially labile pilocarpine prodrugs for improved ocular delivery Hans Bundgaard, Erik Falch, Claus Larsen, Gerold L. Mosher, and Thomas J. Mikkelson pp 979 - 981; DOI: 10.1021/jm00146a001 |
Modifications on the heterocyclic base of acyclovir: syntheses and antiviral properties Lilia M. Beauchamp, Bart L. Dolmatch, Howard J. Schaeffer, Peter Collins, D. J. Bauer, Paul M. Keller, and James A. Fyfe pp 982 - 987; DOI: 10.1021/jm00146a002 |
Potential radiosensitizing agents. 7. 4(5)-Iodo-5(4)-nitroimidazole derivatives Rajender P. Gupta, Cynthia A. Larroquette, Krishna C. Agrawal, J. Grodkowski, and P. Neta pp 987 - 991; DOI: 10.1021/jm00146a003 |
Substrate probes for the mechanism of aromatic hydroxylation catalyzed by cytochrome P-450: selectively deuterated analogs of warfarin Ernie D. Bush and William F. Trager pp 992 - 996; DOI: 10.1021/jm00146a004 |
Metabolism of the nigrostriatal toxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine by liver homogenate fractions Jeff Weissman, Anthony Trevor, Kan Chiba, Lisa A. Peterson, Patricia Caldera, Neal Castagnoli, and Thomas Baillie pp 997 - 1001; DOI: 10.1021/jm00146a005 |
Psoralenamines. 3. Synthesis, pharmacological behavior, and DNA binding of 5-(aminomethyl)-8-methoxy-, 5-[[(3-aminopropyl)oxy]methyl]- and 8-[(3-aminopropyl)oxy]psoralen derivatives John B. Hansen, Peter Bjerring, Ole Buchardt, Peter Ebbesen, Anders Kanstrup, Gunnar Karup, Peter H. Knudsen, Peter E. Nielsen, Bengt Norden, and Birgitta Ygge pp 1001 - 1010; DOI: 10.1021/jm00146a006 |
Synthesis and biological activity of 6-azacadeguomycin and certain 3,4,6-trisubstituted pyrazolo[3,4-d]pyrimidine ribonucleosides Charles R. Petrie, Howard B. Cottam, Patricia A. McKernan, Roland K. Robins, and Ganapathi R. Revankar pp 1010 - 1016; DOI: 10.1021/jm00146a007 |
Syntheses and evaluation as antifolates of MTX analogs derived from 2,.omega.-diaminoalkanoic acids J. R. Piper, G. S. McCaleb, J. A. Montgomery, F. A. Schmid, and F. M. Sirotnak pp 1016 - 1025; DOI: 10.1021/jm00146a008 |
Synthesis and antitumor activity of tropolone derivatives. 2 Masatoshi Yamato, Kuniko Hashigaki, Shigetaka Ishikawa, Nobuhiko Kokubu, Yuka Inoue, Takashi Tsuruo, and Tazuko Tashiro pp 1026 - 1031; DOI: 10.1021/jm00146a009 |
Synthesis and antitumor activity of structural analogs of the anticancer benzophenanthridine alkaloid fagaronine chloride Mark Cushman and Prem Mohan pp 1031 - 1036; DOI: 10.1021/jm00146a010 |
Synthesis, antiinflammatory and analgesic activity of 5-aroyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids and related compounds Joseph M. Muchowski, Stefan H. Unger, Jack Ackrell, Paul Cheung, James Cook, Pascuale Gallegra, Otto Halpern, Richard Koehler, Arthur F. Kluge, and et al. pp 1037 - 1049; DOI: 10.1021/jm00146a011 |
Novel dopamine receptor agonists and antagonists with preferential action on autoreceptors Anette M. Johansson, Lars Erik Arvidsson, Uli Hacksell, J. Lars G. Nilsson, Kjell Svensson, Stephan Hjorth, David Clark, Arvid Carlsson, Domingo Sanchez, and et al. pp 1049 - 1053; DOI: 10.1021/jm00146a012 |
.alpha.-Adrenoreceptor reagents. 3. Synthesis of some 2-substituted 1,4-benzodioxans as selective presynaptic .alpha.2-adrenoreceptor antagonists Michael R. Stillings, Christopher B. Chapleo, Richard C. M. Butler, J. Alfred Davis, C. David England, Malcolm Myers, Peter L. Myers, Neil Tweddle, Anthony P. Welbourn, and et al. pp 1054 - 1062; DOI: 10.1021/jm00146a013 |
Synthesis and biological activity of pentapeptide analogs of the potent angiotensin converting enzyme inhibitor 5(S)-benzamido-4-oxo-6-phenylhexanoyl-L-proline Ronald G. Almquist, Clive Jennings-White, Wan Ru Chao, Thomas Steeger, Kevin Wheeler, James Rogers, and Chozo Mitoma pp 1062 - 1066; DOI: 10.1021/jm00146a014 |
Synthesis and biological activity of carboxylic acid replacement analogs of the potent angiotensin converting enzyme inhibitor 5(S)-benzamido-4-oxo-6-phenylhexanoyl-L-proline Ronald G. Almquist, Wan Ru Chao, and Clive Jennings-White pp 1067 - 1071; DOI: 10.1021/jm00146a015 |
Synthesis of xanthines as adenosine antagonists, a practical quantitative structure-activity relationship application Harriet W. Hamilton, Daniel F. Ortwine, Donald F. Worth, Edward W. Badger, James A. Bristol, Robert F. Bruns, Stephen J. Haleen, and Robert P. Steffen pp 1071 - 1079; DOI: 10.1021/jm00146a016 |
Vinblastin-23-oyl amino acid derivatives: chemistry, physicochemical data, toxicity, and antitumor activities against P388 and L1210 leukemias Kandukuri S. P. Bhushana Rao, Marie Paule M. Collard, Jean Paul C. Dejonghe, Ghanem Atassi, Jean A. Hannart, and Andre Trouet pp 1079 - 1088; DOI: 10.1021/jm00146a017 |
Decomposition reactions of (hydroxyalkyl)nitrosoureas and related compounds: possible relationship to carcinogenicity Sandra S. Singer pp 1088 - 1093; DOI: 10.1021/jm00146a018 |
Structure-activity relationship in PAF-acether. 2. RAC-1-O-octadecyl-2-O-acetyl-3-O-[.gamma.-(dimethylamino)propyl]glycerol Francoise Heymans, Marie Claude Borrel, Colette Broquet, Jean Lefort, and Jean Jacques Godfroid pp 1094 - 1096; DOI: 10.1021/jm00146a019 |
Improved synthesis of 2'-deoxyformycin A and studies of its in vitro activity against mouse lymphoma of T-cell origin Andre Rosowsky, Vishnu C. Solan, and Lorraine J. Gudas pp 1096 - 1099; DOI: 10.1021/jm00146a020 |
Correlation of structure and activity in ansamycins: structure, conformation, and interactions of antibiotic rifamycin S Satish K. Arora pp 1099 - 1102; DOI: 10.1021/jm00146a021 |
Optimization of the Schiff bases of N-hydroxy-N'-aminoguanidine as anticancer and antiviral agents Anne T'ang, Eric J. Lien, and Michael M. C. Lai pp 1103 - 1106; DOI: 10.1021/jm00146a022 |
Substituted 2-pyrones, 2-pyridones, and other congeners of elasnin as potential agents for the treatment of chronic obstructive lung diseases William C. Groutas, Michael A. Stanga, Michael J. Brubaker, Tien L. Huang, Min K. Moi, and Robert T. Carroll pp 1106 - 1109; DOI: 10.1021/jm00146a023 |
Synthesis and pharmacological evaluation of cis-2,3,3a,4,5,6,7,7a-octahydro-3-oxoisoxazolo[5,4-c]pyridine: a structural analog of the GABA agonist THIP Rene Nordmann, Patrick Graff, Richard Maurer, and Beat H. Gaehwiler pp 1109 - 1111; DOI: 10.1021/jm00146a024 |
Stereoselective antitumor properties in the Lewis Lung carcinoma model using bis(morpholinomethyl) derivatives of tricyclic bis(dioxopiperazines) Donald T. Witiak, Bharat K. Trivedi, and Franz A. Schmid pp 1111 - 1113; DOI: 10.1021/jm00146a025 |
Activity of platinum(II) intercalating agents against murine leukemia L1210 W. David McFadyen, Laurence P. G. Wakelin, Ian A. G. Roos, and Virginia A. Leopold pp 1113 - 1116; DOI: 10.1021/jm00146a026 |
Inhibition of muscarinic receptor binding and acetylcholine-induced contraction of guinea pig ileum by analogs of 5'-(isobutylthio)adenosine Marvin C. Pankaskie, James F. Kachur, Tokuo Itoh, Richard K. Gordon, and Peter K. Chiang pp 1117 - 1119; DOI: 10.1021/jm00146a027 |
Structure features of imidazole derivatives that enhance styrene oxide hydrolase activity in rat hepatic microsomes Margaret O. James and Kenneth B. Sloan pp 1120 - 1124; DOI: 10.1021/jm00146a028 |
Synthesis and antineoplastic evaluations of 5,8-bis[(aminoalkyl)amino]-1-azaanthracene-9,10-diones A. Paul Krapcho, John J. Landi, Miles P. Hacker, and John J. McCormack pp 1124 - 1126; DOI: 10.1021/jm00146a029 |
Book Reviews pp 1126 - 1132; DOI: 10.1021/jm00146a600 |
Computer-assisted drug design A. J. Hopfinger pp 1133 - 1139; DOI: 10.1021/jm00147a001 |
Stereostructure-activity relationship of opioid agonist and antagonist bivalent ligands. Evidence for bridging between vicinal opioid receptors P. S. Portoghese, D. L. Larson, C. B. Yim, L. M. Sayre, G. Ronsisvalle, A. W. Lipkowski, A. E. Takemori, K. C. Rice, and S. W. Tam pp 1140 - 1141; DOI: 10.1021/jm00147a002 |
6,7-Dihydro-5-[[(cis-2-hydroxy-trans-3-Phenoxycylopentyl)amino]methyl]-2-methylbenzo[b]thiophen-4(5H)-one: a novel .alpha.1-adrenergic receptor antagonist and renal vasodilator James R. McCarthy, Mark B. Zimmerman, Donald L. Trepanier, Michael E. LeTourneau, Paul E. Wiedman, Jeffrey P. Whitten, Robert J. Broersma, Philip J. Shea, Norbert L. Wiech, and John C. Huffman pp 1142 - 1145; DOI: 10.1021/jm00147a003 |
Synthesis and pharmacological characterization of 5-(2-dodecylphenyl)-4,6-dithianonanedioic acid and 5-[2-(8-phenyloctyl)phenyl]-4,6-dithianonanedioic acid: prototypes of a novel class of leukotriene antagonists Carl D. Perchonock, Mary E. McCarthy, Karl F. Erhard, John G. Gleason, Martin A. Wasserman, Roseanna M. Muccitelli, Jeris F. DeVan, Stephanie S. Tucker, Lynne M. Vickery, and et al. pp 1145 - 1147; DOI: 10.1021/jm00147a004 |
Syntheses and differentiating action of vitamin D endoperoxides. Singlet oxygen adducts of vitamin D derivatives in human myeloid leukemia cells (HL-60) Sachiko Yamada, Keiko Yamamoto, Hiroyuki Naito, Takayoshi Suzuki, Masayuki Ohmori, Hiroaki Takayama, Yoshiko Shiina, Chisato Miyaura, Hirofumi Tanaka, and et al. pp 1148 - 1153; DOI: 10.1021/jm00147a005 |
Mechanism of the differentiating action of 25-hydroxyvitamin D3 endoperoxides in human myeloid leukemia cells (HL-60) Yoshiko Shiina, Chisato Miyaura, Hirofumi Tanaka, Etsuko Abe, Sachiko Yamada, Keiko Yamamoto, Eiichi Ino, Hiroaki Takayama, Isao Matsunaga, and et al. pp 1153 - 1158; DOI: 10.1021/jm00147a006 |
New bidentates as full inhibitors of enkephalin-degrading enzymes: synthesis and analgesic properties Marie Claude Fournie-Zaluski, Annie Coulaud, Romaine Bouboutou, Pierre Chaillet, Jocelyne Devin, Gilles Waksman, Jean Costentin, and Bernard P. Roques pp 1158 - 1169; DOI: 10.1021/jm00147a007 |
5,6-Diaryl-2,3-dihydroimidazo[2,1-b]thiazoles: a new class of immunoregulatory antiinflammatory agents Paul E. Bender, David Hill, Priscilla H. Offen, Kazys Razgaitis, Patricia Lavanchy, Orum D. Stringer, Blaine M. Sutton, Don E. Griswold, Michael DiMartino, and et al. pp 1169 - 1177; DOI: 10.1021/jm00147a008 |
Acylmorphinans. A novel class of potent analgesic agents Erno Mohacsi, Jay O'Brien, John Blount, and Jerry Sepinwall pp 1177 - 1180; DOI: 10.1021/jm00147a009 |
Analogs of platelet activating factor (PAF). 2. Some modifications of the glycerine backbone A. Wissner, R. E. Schaub, P. E. Sum, C. A. Kohler, and B. M. Goldstein pp 1181 - 1187; DOI: 10.1021/jm00147a010 |
Preparation, antiarthritic and analgesic activity of 4,5-diaryl-2-(substituted thio)-1H-imidazoles and their sulfoxides and sulfones Thomas R. Sharpe, Saul C. Cherkofsky, Walter E. Hewes, Dewey H. Smith, Walter A. Gregory, Stephen B. Haber, Michael R. Leadbetter, and Joel G. Whitney pp 1188 - 1194; DOI: 10.1021/jm00147a011 |
8-Substituted guanosine and 2'-deoxyguanosine derivatives as potential inducers of the differentiation of Friend erythroleukemia cells Tai Shun Lin, Jia Chong Cheng, Kimiko Ishiguro, and Alan C. Sartorelli pp 1194 - 1198; DOI: 10.1021/jm00147a012 |
Synthesis and biological activity of 5-thiobredinin and certain related 5-substituted imidazole-4-carboxamide ribonucleosides Steven G. Wood, Krishna G. Upadhya, N. Kent Dalley, Patricia A. McKernan, Peter G. Canonico, Roland K. Robins, and Ganapathi R. Revankar pp 1198 - 1203; DOI: 10.1021/jm00147a013 |
Synthesis and biological effects of novel thiocolchicines. 3. evaluation of N-acyldeacetylthiocolchicines, N-(alkoxycarbonyl)deacetylthiocolchicines, and O-ethyldemethylthiocolchicines. New synthesis of thiodemecolcine and antileukemic effects of 2-demethyl- and 3-demethylthiocolchicine Peter Kerkes, Padam N. Sharma, Arnold Brossi, Colin F. Chignell, and Frank R. Quinn pp 1204 - 1208; DOI: 10.1021/jm00147a014 |
Synthesis and biological evaluation of phosphonamidate peptide inhibitors of enkephalinase and angiotensin-converting enzyme R. L. Elliott, N. Marks, M. J. Berg, and P. S. Portoghese pp 1208 - 1216; DOI: 10.1021/jm00147a015 |
N-(Aminoalkyl)imide antineoplastic agents. Synthesis and biological activity Robert K. Y. Zee-Cheng and C. C. Cheng pp 1216 - 1222; DOI: 10.1021/jm00147a016 |
Adriamycin analogs. Rationale, synthesis, and preliminary antitumor evaluation of highly active DNA-nonbinding N-(trifluoroacetyl)adriamycin 14-O-hemiester derivatives Mervyn Israel, P. Gopalakrishnan Potti, and Ramakrishnan Seshadri pp 1223 - 1228; DOI: 10.1021/jm00147a017 |
Synthesis and antimetastatic properties of stereoisomeric tricyclic bis(dioxopiperazines) in the Lewis lung carcinoma model Donald T. Witiak, Raghunathan V. Nair, and Franz A. Schmid pp 1228 - 1234; DOI: 10.1021/jm00147a018 |
Antiparasitic agents. 6. Synthesis and anthelmintic activities of novel isothiocyanatophenyl-1,2,4-oxadiazoles R. D. Haugwitz, A. J. Martinez, J. Venslavsky, R. G. Angel, B. V. Maurer, G. A. Jacobs, V. L. Narayanan, L. R. Cruthers, and J. Szanto pp 1234 - 1241; DOI: 10.1021/jm00147a019 |
Synthesis and antiherpes simplex virus activity of 9-[(1,3-dihydroxy-2-propylthio)methyl]guanine Danny P. C. McGee, John C. Martin, Donald F. Smee, Thomas R. Matthews, and Julien P. H. Verheyden pp 1242 - 1245; DOI: 10.1021/jm00147a020 |
Structure-activity relationships of some pyridine, piperidine, and pyrrolidine analogs for enhancing and inhibiting the binding of (.+-.)-[3H]nicotine to the rat brain P2 preparation Jewell W. Sloan, William R. Martin, Robert Hook, and Jorge Hernandez pp 1245 - 1251; DOI: 10.1021/jm00147a021 |
Synthesis and LSD-like discriminative stimulus properties in a series of N(6)-alkyl norlysergic acid N,N-diethylamide derivatives Andrew J. Hoffman and David E. Nichols pp 1252 - 1255; DOI: 10.1021/jm00147a022 |
Synthesis and antiallergic activities of 1,3-oxazolo[4,5-h]quinolines John H. Musser, Howard Jones, Stanley Sciortino, Kevin Bailey, Stephen M. Coutts, Atul Khandwala, Paula Sonnino-Goldman, Mitchell Leibowitz, Peter Wolf, and Edward S. Neiss pp 1255 - 1259; DOI: 10.1021/jm00147a023 |
Anticonvulsant activity of some 4-aminobenzanilides C. Randall Clark, Ricky T. Sansom, Ching Ming Lin, and George N. Norris pp 1259 - 1262; DOI: 10.1021/jm00147a024 |
Potential neuroleptic agents. 3. Chemistry and antidopaminergic properties of substituted 6-methoxysalicylamides Tomas De Paulis, Yatendra Kumar, Lars Johansson, Sten Raemsby, Lennart Florvall, Haakan Hall, Kristina Aengeby-Moeller, and Sven Ove Oegren pp 1263 - 1269; DOI: 10.1021/jm00147a025 |
N-Substituted imidazolines and ethylenediamines and their action on .alpha.- and .beta.-adrenergic receptors Akihiko Hamada, Emily L. Yaden, J. S. Horng, Robert R. Ruffolo, Popat N. Patil, and Duane D. Miller pp 1269 - 1273; DOI: 10.1021/jm00147a026 |
Molecular mechanism of action of 5,6-dihydroxytryptamine. Synthesis and biological evaluation of 4-methyl-, 7-methyl- and 4,7-dimethyl-5,6-dihydroxytryptamines Achintya K. Sinhababu, Anil K. Ghosh, and Ronald T. Borchardt pp 1273 - 1279; DOI: 10.1021/jm00147a027 |
Synthesis of new bis(aminoethanethiol) (BAT) derivatives: possible ligands for 99mTc brain imaging agents H. F. Kung, C. C. Yu, J. Billings, M. Molnan, and M. Blau pp 1280 - 1284; DOI: 10.1021/jm00147a028 |
Synthesis and structure-activity relationships of a new series of antiarrhythmic agents: 4,4-disubstituted hexahydro-3H-pyrido[1,2-c]pyrimidin-3-ones and related compounds Robert J. Chorvat, Kathleen A. Prodan, Gilbert W. Adelstein, Robert M. Rydzewski, Kathleen T. McLaughlin, Margarete H. Stamm, Leo G. Frederick, Henry C. Schniepp, and Janice L. Stickney pp 1285 - 1291; DOI: 10.1021/jm00147a029 |
Synthesis and biological activity of modified peptide inhibitors of angiotensin-converting enzyme W. Howard Roark, Francis J. Tinney, David Cohen, Arnold D. Essenburg, and Harvey R. Kaplan pp 1291 - 1295; DOI: 10.1021/jm00147a030 |
Ring-substituted 1,1,2,2-tetraalkylated 1,2-bis(hydroxyphenyl)ethanes. 4. Synthesis, estrogen receptor binding affinity, and evaluation of antiestrogenic and mammary tumor inhibiting activity of symmetrically disubstituted 1,1,2,2-tetramethyl-1,2-bis(hydroxyphenyl)ethanes Rolf W. Hartmann, Walter Schwarz, Alexander Heindl, and Helmut Schoenenberger pp 1295 - 1301; DOI: 10.1021/jm00147a031 |
Synthetic and conformational studies on anatoxin-a: a potent acetylcholine agonist Ari M. P. Koskinen and Henry Rapoport pp 1301 - 1309; DOI: 10.1021/jm00147a032 |
Effects of charge, volume, and surface on binding of inhibitor and substrate moieties to acetylcholinesterase Saul G. Cohen, S. Bano Chishti, Jerome L. Elkind, and Heide Reese pp 1309 - 1313; DOI: 10.1021/jm00147a033 |
Benzodiazepine receptor binding and anticonflict activity in a series of 3,6-disubstituted pyridazino[4,3-c]isoquinolines devoid of anticonvulsant properties Emilio Toja, Giorgio Tarzia, Domenico Barone, Franco Luzzani, and Licia Gallico pp 1314 - 1319; DOI: 10.1021/jm00147a034 |
Synthesis of high specific activity [75Br]- and [77Br]bromperidol and tissue distribution studies in the rat Stephen M. Moerlein and Gerhard L. Stoecklin pp 1319 - 1324; DOI: 10.1021/jm00147a035 |
Carbon-11-labeled 4-isopropylantipyrine: preparation and biological evaluation as a blood flow tracer in positron emission tomography (PET) Sharon Stone-Elander, Martin Ingvar, Peter Johnstroem, Erling Ehrin, Birgit Garmelius, Torgny Greitz, J. Lars G. Nilsson, Bahram Resul, Maj Lis Smith, and Lennart Widen pp 1325 - 1328; DOI: 10.1021/jm00147a036 |
Quantitative evaluation of the .beta.2-adrenoceptor affinity of phenoxypropanolamines and phenylethanolamines Adriaan P. Ijzerman, George H. J. Aue, Teake Bultsma, Marcel R. Linschoten, and Hendrik Timmerman pp 1328 - 1334; DOI: 10.1021/jm00147a037 |
Functionalized congeners of 1,3-dialkylxanthines: preparation of analogs with high affinity for adenosine receptors Kenneth A. Jacobson, Kenneth L. Kirk, William L. Padgett, and John W. Daly pp 1334 - 1340; DOI: 10.1021/jm00147a038 |
Functionalized congeners of adenosine: preparation of analogs with high affinity for A1-adenosine receptors Kenneth A. Jacobson, Kenneth L. Kirk, William L. Padgett, and John W. Daly pp 1341 - 1346; DOI: 10.1021/jm00147a039 |
New cysteamine (2-chloroethyl)nitrosoureas. Synthesis and preliminary antitumor results J. C. Madelmont, D. Godeneche, D. Parry, J. Duprat, J. L. Chabard, R. Plagne, G. Mathe, and G. Meyniel pp 1346 - 1350; DOI: 10.1021/jm00147a040 |
In search of new anticancer drugs. 13. Phosphonic and phosphinic analogs of ornithine George Sosnovsky, Jan Lukszo, Enrico Gravela, and Maria Franca Zuretti pp 1350 - 1354; DOI: 10.1021/jm00147a041 |
Structure-activity relationships for prazosin and WB 4101 analogs as .alpha.1-adrenoreceptor antagonists Dario Giardina, Rosaria Bertini, Egle Brancia, Livio Brasili, and Carlo Melchiorre pp 1354 - 1357; DOI: 10.1021/jm00147a042 |
Synthesis and biological evaluation of 9-[5'-(2-oxo-1,3,2-oxazaphosphorinan-2-yl)-.beta.-D-arabinosyl]adenine and 9-[5'-(2-oxo-1,3,2-dioxaphosphorinan-2-yl)-.beta.-D-arabinosyl]adenine: potential neutral precursors of 9-[.beta.-D-arabinofuranosyl]adenine 5'-monophosphate David Farquhar and Ronald Smith pp 1358 - 1361; DOI: 10.1021/jm00147a043 |
Aminotetralone analogs of ketamine: synthesis and evaluation of hypnotic and locomotor properties in mice David J. Yang and John N. Davisson pp 1361 - 1365; DOI: 10.1021/jm00147a044 |
Analogs of platelet activating factor. 3. Replacement of the phosphate moiety with a sulfonylbismethylene group Allan Wissner, C. A. Kohler, and B. M. Goldstein pp 1365 - 1367; DOI: 10.1021/jm00147a045 |
Synthesis and dopamine autoreceptor activity of a 5-(methylmercapto)methyl-substituted derivative of(.+-.)-3-PPP [3-(3-hydroxyphenyl)-1-propylpiperidine] T. Ross Kelly, Harry R. Howard, B. Kenneth Koe, and Reinhard Sarges pp 1368 - 1371; DOI: 10.1021/jm00147a046 |
Preparation of biologically active ristocetin derivatives: replacements of the 1'-amino group Thomas R. Herrin, Alford M. Thomas, Thomas J. Perun, James C. Mao, and Stephen W. Fesik pp 1371 - 1375; DOI: 10.1021/jm00147a047 |
Replacement of the ribofuranose oxygen of 2-5A derivatives by methylene: synthesis of an aristeromycin analog of 2-5A core 5'-monophosphate (5'-O-phosphoryladenylyl)(2'.fwdarw.5')adenylyl(2'.fwdarw.5')adenosine 5'-monophosphate Hiroaki Sawai, Krystyna Lesiak, Jiro Imai, and Paul F. Torrence pp 1376 - 1380; DOI: 10.1021/jm00147a048 |
Book Reviews pp 1380 - 1382; DOI: 10.1021/jm00147a600 |
N6-Cycloalkyladenosines. Potent, A1-selective adenosine agonists Walter H. Moos, Deedee S. Szotek, and Robert F. Bruns pp 1383 - 1384; DOI: 10.1021/jm00148a001 |
Resolution of aristeromycin enantiomers Piet Herdewijn, Jan Balzarini, Erik De Clercq, and Hubert Vanderhaeghe pp 1385 - 1386; DOI: 10.1021/jm00148a002 |
Cyclic guanidines. 17. Novel (N-substituted amino)imidazo[2,1-b]quinazolin-2-ones: water-soluble platelet aggregation inhibitors Fumiyoshi Ishikawa, Junji Saegusa, Kazue Inamura, Kyoko Sakuma, and Shinichiro Ashida pp 1387 - 1393; DOI: 10.1021/jm00148a003 |
Design, synthesis and pharmacological activities of 2-substituted 4-phenylquinolines as potential antidepressant drugs Abdulqader A. Alhaider, M. Atef Abdelkader, and Eric J. Lien pp 1394 - 1398; DOI: 10.1021/jm00148a004 |
Conformationally defined adrenergic agents. 1. Design and synthesis of novel .alpha.2-selective adrenergic agents: electrostatic repulsion based conformational prototypes John F. DeBernardis, Daniel J. Kerkman, Martin Winn, Eugene N. Bush, David L. Arendsen, William J. McClellan, John J. Kyncl, and Fatima Z. Basha pp 1398 - 1404; DOI: 10.1021/jm00148a005 |
Cardiotonic agents. 2. Synthesis and structure-activity relationships of 4,5-dihydro-6-[4-(H-imidazol-1-yl)phenyl]-3(2H)-pyridazinones: a new class of positive inotropic agents Ila Sircar, Bradley L. Duell, George Bobowski, James A. Bristol, and Dale B. Evans pp 1405 - 1413; DOI: 10.1021/jm00148a006 |
The histamine H2-receptor agonist impromidine: synthesis and structure activity considerations G. J. Durant, C. R. Ganellin, D. W. Hills, P. D. Miles, M. E. Parsons, E. S. Pepper, and G. R. White pp 1414 - 1422; DOI: 10.1021/jm00148a007 |
N.alpha.-(O,O'-Diphenoxyphosphoryl)-L-alanyl-L-proline, N.alpha.-[O,O'-bis(4-nitrophenoxy)phosphoryl]-L-alanyl-L-proline and N.alpha.-[P-(2-phenylethyl)-O-phenoxyphosphoryl]-L-alanyl-L-proline: releasers of potent inhibitors of angiotensin converting enzyme at physiological pH and temperature Richard E. Galardy and Damian Grobelny pp 1422 - 1427; DOI: 10.1021/jm00148a008 |
Selective thromboxane synthetase inhibitors. 1. 1-[(Aryloxy)alkyl]-1H-imidazoles Peter E. Cross, Roger P. Dickinson, M. John Parry, and Michael J. Randall pp 1427 - 1432; DOI: 10.1021/jm00148a009 |
Studies on the 1-methyl-4-phenyl-2,3-dihydropyridinium species 2,3-MPDP+, the monoamine oxidase catalyzed oxidation product of the nitrostriatal toxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) Lisa A. Peterson, Patricia S. Caldera, Anthony Trevor, Kan Chiba, and N. Castagnoli pp 1432 - 1436; DOI: 10.1021/jm00148a010 |
Synthesis and hypoglycemic activity of N-alkylated hydrazonopropionic acids Hans Peter Wolff and Hans F. Kuehnle pp 1436 - 1440; DOI: 10.1021/jm00148a011 |
Synthesis and activity of 5-(aminomethyl)-1,3-cyclohexanediones: enolic analogs of .gamma.-aminobutyric acid Andre Mann, Christine Humblet, Jean Pierre Chambon, Remy Schlichter, Michel Desarmenien, Paul Feltz, and Camille Georges Wermuth pp 1440 - 1446; DOI: 10.1021/jm00148a012 |
Synthesis and biological activity of substituted [[3(S)-(acylamino)-2-oxo-1-azetidinyl]oxy]acetic acids. A new class of heteroatom-activated .beta.-lactam antibiotics Steven R. Woulfe and Marvin J. Miller pp 1447 - 1453; DOI: 10.1021/jm00148a013 |
Substituent effects on the bioactivation of 2-(N-hydroxyacetamido)fluorenes by N-arylhydroxamic acid N,O-acyltransferase Adnan A. Elfarra and Patrick E. Hanna pp 1453 - 1460; DOI: 10.1021/jm00148a014 |
Synthesis and biological activity of certain 6-substituted and 2,6-disubstituted 2'-deoxytubercidins prepared via the stereospecific sodium salt glycosylation procedure Howard B. Cottam, Zygmunt Kazimierczuk, Stewart Geary, Patricia A. McKernan, Ganapathi R. Revankar, and Roland K. Robins pp 1461 - 1467; DOI: 10.1021/jm00148a015 |
Quinazoline antifolates inhibiting thymidylate synthase: variation of the N10 substituent Terence R. Jones, A. Hilary Calvert, Ann L. Jackman, M. Allan Eakin, Michael J. Smithers, Richard F. Betteridge, David R. Newell, Anthony J. Hayter, Andrew Stocker, and et al. pp 1468 - 1476; DOI: 10.1021/jm00148a016 |
(.+-.)-2-Amino-3,4-dihydro-7-[2,3-dihydroxy-4-(hydroxymethyl)-1-cyclopentyl]-7H-pyrrolo[2,3-d]pyrimidin-4-ones: new carbocyclic analogs of 7-deazaguanosine with antiviral activity Michel Legraverend, Rose Marie Nia Ngongo-Tekam, Emile Bisagni, and Aurelio Zerial pp 1477 - 1480; DOI: 10.1021/jm00148a017 |
Purine and 8-substituted purine arabinofuranosyl and ribofuranosyl nucleoside derivatives as potential inducers of the differentiation of the Friend erythroleukemia Tai Shun Lin, Jia Chong Cheng, Kimiko Ishiguro, and Alan C. Sartorelli pp 1481 - 1485; DOI: 10.1021/jm00148a018 |
Synthesis and some pharmacological properties of 18 potent O-alkyltyrosine-substituted antagonists of the vasopressor responses to arginine-vasopressin Maurice Manning, Bernard Lammek, Krzysztof Bankowski, Janny Seto, and W. H. Sawyer pp 1485 - 1491; DOI: 10.1021/jm00148a019 |
Hydroxy derivatives of tamoxifen Allan B. Foster, Michael Jarman, On Tai Leung, Raymond McCague, Guy Leclercq, and N. Devleeschouwer pp 1491 - 1497; DOI: 10.1021/jm00148a020 |
Structural studies on some tamoxifen derivatives Reiko Kuroda, Shirley Cutbush, Stephen Neidle, and On Tai Lueng pp 1497 - 1503; DOI: 10.1021/jm00148a021 |
Synthesis and receptor-binding affinity of fluorotamoxifen, a possible estrogen-receptor imaging agent Jashovam Shani, Aviv Gazit, Tania Livshitz, and Shoshana Biran pp 1504 - 1511; DOI: 10.1021/jm00148a022 |
Synthesis and biological properties of (carboxyalkyl)amino-substituted bicyclic lactam inhibitors of angiotensin converting enzyme Jeffrey W. H. Watthey, James L. Stanton, Mahesh Desai, Joseph E. Babiarz, and Barbara M. Finn pp 1511 - 1516; DOI: 10.1021/jm00148a023 |
Angiotensin converting enzyme inhibitors: 1,5-benzothiazepine derivatives Joel Slade, James L. Stanton, Daniel Ben-David, and Gerard C. Mazzenga pp 1517 - 1521; DOI: 10.1021/jm00148a024 |
Design, synthesis, and testing of insulin hexamer-stabilizing agents D. T. Manallack, P. R. Andrews, and E. F. Woods pp 1522 - 1526; DOI: 10.1021/jm00148a025 |
Peptide sweeteners. 8. Synthesis and structure-taste relationship studies of L-aspartyl-D-alanyl tripeptides Marc Rodriguez, John M. Bland, Joseph W. Tsang, and Murray Goodman pp 1527 - 1529; DOI: 10.1021/jm00148a026 |
Synthesis of the C-terminal octapeptide of pig oxyntomodulin. Lys-Arg-Asn-Lys-Asn-Asn-Ile-Ala: a potent inhibitor of pentagastrin-induced acid secretion M. P. Audousset-Puech, C. Jarrousse, M. Dubrasquet, A. Aumelas, B. Castro, D. Bataille, and Jean Martinez pp 1529 - 1533; DOI: 10.1021/jm00148a027 |
4-[2-(Di-n-propylamino)ethyl]-2(3H)-indolone: a prejunctional dopamine receptor agonist Gregory Gallagher, Patricia G. Lavanchy, James W. Wilson, J. Paul Hieble, and Robert M. DeMarinis pp 1533 - 1536; DOI: 10.1021/jm00148a028 |
Conformationally restricted C-terminal peptides of substance P. Synthesis, mass spectral analysis and pharmacological properties Dimitrios Theodoropoulos, Constantin Poulos, Dimitrios Gatos, Pane Cordopatis, Emanuel Escher, Jacques Mizrahi, Domenico Regoli, Demetrios Dalietos, Arthur Furst, and Terry D. Lee pp 1536 - 1539; DOI: 10.1021/jm00148a029 |
Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3.alpha.,4a.alpha.,10a.beta.)-1,2,3,4,4a,5,10,10a-octahydro-6-hydroxy-1-propyl-3-benzo[g]quinolinyl]sulfamide Rene Nordmann and Armin Widmer pp 1540 - 1542; DOI: 10.1021/jm00148a030 |
Antimicrobial and antitumor properties of 9,10-dihydrophenanthrenes: structure activity studies on juncusol Dale L. Boger, Lester A. Mitscher, Michael D. Mullican, Steven D. Drake, and Paul Kitos pp 1543 - 1547; DOI: 10.1021/jm00148a031 |
Book Reviews pp 1547 - 1552; DOI: 10.1021/jm00148a600 |
Difluorostatine and difluorostatone containing peptides as potent and specific renin inhibitors Suvit Thaisrivongs, Donald T. Pals, Warren M. Kati, Steve R. Turner, and Lisa M. Thomasco pp 1553 - 1555; DOI: 10.1021/jm00149a001 |
N-(Phosphonoacetyl)amino phosphonates. Phosphonate analogs of N-(phosphonoacetyl)-L-aspartic acid (PALA) Pawel Kafarski, Barbara Lejczak, Przemyslaw Mastalerz, Danuta Dus, and Czeslaw Radzikowski pp 1555 - 1558; DOI: 10.1021/jm00149a002 |
Synthesis and structure-activity relationships of novel arylfluoroquinolone antibacterial agents Daniel T. W. Chu, Prabhavathi B. Fernandes, Akiyo K. Claiborne, Eva Pihuleac, Carl W. Nordeen, Robert E. Maleczka, and Andre G. Pernet pp 1558 - 1564; DOI: 10.1021/jm00149a003 |
4-Substituted 5-[m-(trifluoromethyl)phenoxy]primaquine analogs as potential antimalarial agents F. Ivy Carroll, Bertold Berrang, and C. P. Linn pp 1564 - 1567; DOI: 10.1021/jm00149a004 |
Potential antitumor agents. 44. Synthesis and antitumor activity of new classes of diacridines: importance of linker chain rigidity for DNA binding kinetics and biological activity William A. Denny, Graham J. Atwell, Bruce C. Baguley, and Laurence P. G. Wakelin pp 1568 - 1574; DOI: 10.1021/jm00149a005 |
Evaluation of the brain-specific delivery of radioiodinated (Iodophenyl) alkyl-substituted amines coupled to a dihydropyridine carrier M. L. Tedjamulia, P. C. Srivastava, and F. F. Knapp pp 1574 - 1580; DOI: 10.1021/jm00149a006 |
Synthesis and in vitro pharmacology of 7-oxabicyclo[2.2.1]heptane analogs of thromboxane A2/PGH2 P. W. Sprague, J. E. Heikes, J. Z. Gougoutas, M. F. Malley, D. N. Harris, and R. Greenberg pp 1580 - 1590; DOI: 10.1021/jm00149a007 |
Hypolipidemic activity of indan-1,3-dione derivatives in rodents A. R. Murthy, S. D. Wyrick, and I. H. Hall pp 1591 - 1596; DOI: 10.1021/jm00149a008 |
Synthesis and pharmacology of the potent angiotensin-converting enzyme inhibitor N-[1(S)-(ethoxycarbonyl)-3-phenylpropyl]-(S)-alanyl-(S)-pyroglutamic acid Alexander L. Johnson, William A. Price, Pancras C. Wong, Robert F. Vavala, and John M. Stump pp 1596 - 1602; DOI: 10.1021/jm00149a009 |
Angiotensin converting enzyme inhibitors: structure-activity profile of 1-benzazepin-2-one derivatives James L. Stanton, Jeffrey W. H. Watthey, Mahesh N. Desai, Barbara M. Finn, Joseph E. Babiarz, and Hollis C. Tomaselli pp 1603 - 1606; DOI: 10.1021/jm00149a010 |
Angiotensin converting enzyme inhibitors: N-substituted D-glutamic acid .gamma.-dipeptides Gary M. Ksander, Andrew M. Yuan, Clive G. Diefenbacher, and James L. Stanton pp 1606 - 1611; DOI: 10.1021/jm00149a011 |
GABA agonists. Resolution, absolute stereochemistry and enantioselectivity of (S)-(+)- and (R)-(-)-dihydromuscimol Povl Krogsgaard-Larsen, Lone Nielsen, Erik Falch, and David R. Curtis pp 1612 - 1617; DOI: 10.1021/jm00149a012 |
Synthesis and antidiarrheal activity of N-(aminoiminomethyl)-1H-pyrrole-1-acetamides related to guanfacine Doreen E. Beattie, Gillian M. Dover, and Terence J. Ward pp 1617 - 1620; DOI: 10.1021/jm00149a013 |
Structure-activity relationship studies in the field of calcium(II) antagonists. Effect of modifications at the tetrasubstituted carbon of verapamil-like compounds Fulvio Gualtieri, Elisabetta Teodori, Cristina Bellucci, Edilio Pesce, and Giuseppe Piacenza pp 1621 - 1628; DOI: 10.1021/jm00149a014 |
Pseudosymmetry and bioisosterism in biaryl pyridyl competitive histamine H2-receptor antagonists Christopher A. Lipinski, John L. LaMattina, and Lyle A. Hohnke pp 1628 - 1636; DOI: 10.1021/jm00149a015 |
Dog coronary artery adenosine receptor: structure of the N6-alkyl subregion Shozo Kusachi, Robert D. Thompson, William J. Bugni, Nobuyuki Yamada, and Ray A. Olsson pp 1636 - 1643; DOI: 10.1021/jm00149a016 |
Structure-activity relationships among benextramine-related tetraamine disulfides at peripheral .alpha.-adrenoreceptors Piero Angeli, Livio Brasili, Egle Brancia, Dario Giardina, Wilma Quaglia, and Carlo Melchiorre pp 1643 - 1647; DOI: 10.1021/jm00149a017 |
.beta.-Adrenoceptor activity of the stereoisomers of the bufuralol alcohol and ketone metabolites Peter J. Machin, David N. Hurst, and John M. Osbond pp 1648 - 1651; DOI: 10.1021/jm00149a018 |
Opioid receptor interactions and conformations of the 6.alpha. and 6.beta. epimers of oxymorphamine. Solid-state conformation of 6.alpha.-oxymorphamine O. William Lever, Ashok V. Bhatia, and Kwen Jen Chang pp 1652 - 1656; DOI: 10.1021/jm00149a019 |
Novel nonnarcotic analgesics with an improved therapeutic ratio. Structure-activity relationships of 8-(methylthio)- and 8-(acylthio)-1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocines Mikio Hori, Masatoshi Ban, Eiji Imai, Noriyuki Iwata, Yoshinari Suzuki, Yutaka Baba, Tokiko Morita, Hajime Fujimura, Masakatsu Nozaki, and Masayuki Niwa pp 1656 - 1661; DOI: 10.1021/jm00149a020 |
Inhibitors of blood platelet aggregation. Effects of some 1,2-benzisothiazol-3-ones on platelet responsiveness to adenosine diphosphate and collagen Keith H. Baggaley, Peter D. English, L. John A. Jennings, Brian Morgan, Barbara Nunn, and A. William R. Tyrrell pp 1661 - 1667; DOI: 10.1021/jm00149a021 |
Design and synthesis of new transition-state analog inhibitors of aspartate transcarbamylase G. King Farrington, Alok Kumar, and Frederick C. Wedler pp 1668 - 1673; DOI: 10.1021/jm00149a022 |
Antitrichomonal activity of mesoionic thiazolo[3,2-a]pyridines Keith A. M. Walker, Eric B. Sjogren, and Thomas R. Matthews pp 1673 - 1679; DOI: 10.1021/jm00149a023 |
5-(Haloalkyl)-2'-deoxyuridines: a novel type of potent antiviral nucleoside analog Herfried Griengl, Michael Bodenteich, Walter Hayden, Erich Wanek, Wolfgang Streicher, Peter Stuetz, Helmut Bachmayer, Ismail Ghazzouli, and Brigitte Rosenwirth pp 1679 - 1684; DOI: 10.1021/jm00149a024 |
Synthesis and properties of bis(2,2-dimethylaziridinyl)phosphinic amides: a series of new antineoplastic agents Joan E. MacDiarmid, William C. Rose, William C. Biddle, Michael E. Perlman, Robert G. Breiner, Julian L. Ambrus, and Thomas J. Bardos pp 1685 - 1691; DOI: 10.1021/jm00149a025 |
Synthesis of 6-anilino-2-thiouracils and their inhibition of human placenta iodothyronine deiodinase T. Nogimori, C. H. Emerson, L. E. Braverman, C. F. Wu, J. Gambino, and G. E. Wright pp 1692 - 1694; DOI: 10.1021/jm00149a026 |
Synthesis and evaluation of potential radioligands for the progesterone receptor R. M. Hoyte, W. Rosner, I. S. Johnson, J. Zielinski, and R. B. Hochberg pp 1695 - 1699; DOI: 10.1021/jm00149a027 |
Alkylating .beta.-blockers: activity of isomeric bromoacetyl alprenolol menthanes Andras Liptak, John W. Kusiak, and Josef Pitha pp 1699 - 1703; DOI: 10.1021/jm00149a028 |
Imidazo[1,5-d][1,2,4]triazines as potential antiasthma agents Rolf Paul, John A. Brockman, W. A. Hallett, John W. Hanifin, M. Ernestine Tarrant, Lawrence W. Torley, Francis M. Callahan, Paul F. Fabio, Bernard D. Johnson, and et al. pp 1704 - 1716; DOI: 10.1021/jm00149a029 |
Synthesis, absolute configuration and conformation of the aldose reductase inhibitor sorbinil Reinhard Sarges, Jon Bordner, Beryl W. Dominy, Michael J. Peterson, and Earl B. Whipple pp 1716 - 1720; DOI: 10.1021/jm00149a030 |
New bicyclic antidepressant agent. Synthesis and activity of napactadine and related compounds James R. McCarthy, Donald L. Wright, Albert J. Schuster, Abdul H. Abdallah, Philip J. Shea, and Randy Eyster pp 1721 - 1727; DOI: 10.1021/jm00149a031 |
Novel bis[1,6-dihydro-6,6-dimethyl-1,3,5-triazine-2,4-diamines] as antitrypanosomal agents William R. Turner and Leslie M. Werbel pp 1728 - 1740; DOI: 10.1021/jm00149a032 |
2-Fluoroformycin and 2-aminoformycin. Synthesis and biological activity John A. Secrist, Anita T. Shortnacy, and John A. Montgomery pp 1740 - 1742; DOI: 10.1021/jm00149a033 |
Antimalarial agents. 1. .alpha.-Santonin-derived cyclic peroxide as potential antimalarial agent Shohei Tani, Narihiko Fukamiya, Hiroshi Kiyokawa, H. A. Musallam, Robert O. Pick, and Kuo Hsiung Lee pp 1743 - 1744; DOI: 10.1021/jm00149a034 |
Synthesis, characterization, and anorectic testing of the four stereoisomers of cyclo(histidylproline) Michael J. Kukla, Henry J. Breslin, and Charles R. Bowden pp 1745 - 1747; DOI: 10.1021/jm00149a035 |
Synthesis and anthelmintic activity of 5(6)-[(benzimidazol-2-yl)carboxamido]- and (4-substituted piperazin-1-yl)benzimidazoles Rashmi Dubey, Syed Abuzar, Satyavan Sharma, R. K. Chatterjee, and J. C. Katiyar pp 1748 - 1750; DOI: 10.1021/jm00149a036 |
Study on the inhibition of adenosine deaminase John A. Montgomery, H. Jeanette Thomas, Alan L. Zell, Howard M. Einsphar, and Charles E. Bugg pp 1751 - 1753; DOI: 10.1021/jm00149a037 |
Book Reviews pp 1753 - 1754; DOI: 10.1021/jm00149a600 |
A uniquely potent renin inhibitor and its unanticipated plasma binding component Ben E. Evans, Kenneth E. Rittle, Mark G. Bock, Carl D. Bennett, Robert M. DiPardo, Joshua Boger, Martin Poe, Edgar H. Ulm, Bruce I. LaMont, and et al. pp 1755 - 1756; DOI: 10.1021/jm00150a001 |
N-(1,3,4,6,7,12b-hexahydro-2H-benzo[b]furo[2,3-a]quinolizin-2-yl)-N-methyl-2-hydroxyethanesulfonamide: a potent and selective .alpha.2-adrenoceptor antagonist Joel R. Huff, Paul S. Anderson, John J. Baldwin, Bradley V. Clineschmidt, James P. Guare, Victor J. Lotti, Douglas J. Pettibone, William C. Randall, and Joseph P. Vacca pp 1756 - 1759; DOI: 10.1021/jm00150a002 |
Novel vasopressin analogs that help define a minimum effective antagonist pharmacophore William F. Huffman, Fadia E. Ali, William M. Bryan, James F. Callahan, Michael L. Moore, Joanne S. Silvestri, Nelson C. F. Yim, Lewis B. Kinter, Jeanne E. McDonald, and et al. pp 1759 - 1760; DOI: 10.1021/jm00150a003 |
Stereoselectivity of muscarinic receptors in vivo and in vitro for oxotremorine analogs. N-[4-tert-amino-2-butynyl]-5-methyl-2-pyrrolidones Rene Amstutz, Bjoern Ringdahl, Bo Karlen, Margareth Roch, and Donald J. Jenden pp 1760 - 1765; DOI: 10.1021/jm00150a004 |
Synthesis and activity profiles of novel cyclic opioid peptide monomers and dimers Peter W. Schiller, Thi M. D. Nguyen, Carole Lemieux, and Louise A. Maziak pp 1766 - 1771; DOI: 10.1021/jm00150a005 |
Synthesis and antibacterial activity of 2,2'-dithiobis(benzamide) derivatives against Mycobacterium species Ryo Okachi, Hideki Niino, Kozo Kitaura, Kazuyuki Mineura, Yoshinobu Nakamizo, Yo Murayama, Takeshi Ono, and Akio Nakamizo pp 1772 - 1779; DOI: 10.1021/jm00150a006 |
Renin inhibitors. Syntheses of subnanomolar, competitive, transition-state analog inhibitors containing a novel analog of statine Joshua Boger, Linda S. Payne, Debra S. Perlow, Nancy S. Lohr, Martin Poe, Edward H. Blaine, Edgar H. Ulm, Terry W. Schorn, Bruce I. LaMont, and et al. pp 1779 - 1790; DOI: 10.1021/jm00150a007 |
1,2-Dihydro-2-oxo-6-(2,2-dimethylpropyl)-3-pyridinecarboxylic acid. Analogs, and derivatives. A new class of oral hypoglycemic agents Gilbert A. Youngdale and Thomas F. Oglia pp 1790 - 1796; DOI: 10.1021/jm00150a008 |
Antiandrogenic activity of a series of des-A-steroid derivatives Hilda Morales-Alanis, Marie Josephe Brienne, Jean Jacques, Marie M. Bouton, Lucien Nedelec, Vesperto Torelli, and Colette Tournemine pp 1796 - 1803; DOI: 10.1021/jm00150a009 |
Dopamine receptor agonist activity of some 5-(2-aminoethyl)carbostyril derivatives Carl Kaiser, Penelope A. Dandridge, Eleanor Garvey, Kathryn E. Flaim, Robert L. Zeid, and J. Paul Hieble pp 1803 - 1810; DOI: 10.1021/jm00150a010 |
Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8-triazaspiro[4.5]decan-4-ones as potential antipsychotic agents Lawrence D. Wise, Ian C. Pattison, Donald E. Butler, Horace A. DeWald, Edward P. Lewis, Sandra J. Lobbestael, Haile Tecle, Linda L. Coughenour, David A. Downs, and B. P. H. Poschel pp 1811 - 1817; DOI: 10.1021/jm00150a011 |
3-Phenyl-1-indanamines. Potential antidepressant activity and potent inhibition of dopamine, norepinephrine, and serotonin uptake Klaus P. Bogeso, A. Vibeke Christensen, John Hyttel, and Tommy Liljefors pp 1817 - 1828; DOI: 10.1021/jm00150a012 |
Inhibition of human leukocyte elastase, porcine pancreatic elastase, and chymotrypsin by elasnin and other 4-hydroxy-2-pyrones Robin W. Spencer, Leslie J. Copp, and Jurg R. Pfister pp 1828 - 1832; DOI: 10.1021/jm00150a013 |
New antiallergic pyrano[3,2-g]quinoline-2,8-dicarboxylic acids with potential for the topical treatment of asthma Hugh Cairns, David Cox, Ken J. Gould, Anthony H. Ingall, and John L. Suschitzky pp 1832 - 1842; DOI: 10.1021/jm00150a014 |
Substituted benzamides with conformationally restricted side chains. 1. Quinolizidine derivatives as selective gastric prokinetic agents Michael S. Hadley, Frank D. King, Brian McRitchie, David H. Turner, and Eric A. Watts pp 1843 - 1847; DOI: 10.1021/jm00150a015 |
Synthesis and LTD4 antagonist activity of 2-norleukotriene analogs Thomas W. Ku, Mary E. McCarthy, Barry M. Weichman, and John G. Gleason pp 1847 - 1853; DOI: 10.1021/jm00150a016 |
Factors affecting binding of trans-N-[2-(methylamino)cyclohexyl]benzamides at the primary morphine receptor B. Vernon Cheney, Jacob Szmuszkovicz, Robert A. Lahti, and Dominic A. Zichi pp 1853 - 1864; DOI: 10.1021/jm00150a017 |
Pyrimidinones. 1. 2-Amino-5-halo-6-aryl-4(3H)-pyrimidinones. Interferon-inducing antiviral agents Harvey I. Skulnick, Sheldon D. Weed, Emerson E. Eidson, Harold E. Renis, Dale A. Stringfellow, and Wendell Wierenga pp 1864 - 1869; DOI: 10.1021/jm00150a018 |
Monocyclic pteridine analogs. Inhibition of Escherichia coli dihydropteroate synthase by 6-amino-5-nitrosoisocytosines O. William Lever, Lawrence N. Bell, H. Michael McGuire, and Robert Ferone pp 1870 - 1874; DOI: 10.1021/jm00150a019 |
Synthesis and biological activities of some pseudo-peptide analogs of tetragastrin: the importance of the peptide backbone Jean Martinez, Jean Pierre Bali, Marc Rodriguez, B. Castro, R. Magous, Jeanine Laur, and Marie Francoise Lignon pp 1874 - 1879; DOI: 10.1021/jm00150a020 |
Acetoxy-substituted 1,1,2-triphenylbut-1-enes with antiestrogenic and mammary tumor inhibiting properties Martin R. Schneider, Hartwig Ball, and Helmut Schoenenberger pp 1880 - 1885; DOI: 10.1021/jm00150a021 |
Orally absorbable cephalosporin antibiotics. 1. Structure-activity relationships of benzothienyl- and naphthylglycine derivatives of 7-aminodeacetoxycephalosporanic acid Stjepan Kukolja, Susan E. Draheim, Janice L. Pfeil, Robin D. G. Cooper, Bernard J. Graves, Richard E. Holmes, David A. Neel, George W. Huffman, J. Alan Webber, and et al. pp 1886 - 1896; DOI: 10.1021/jm00150a022 |
Orally absorbable cephalosporin antibiotics. 2. Structure-activity studies of bicyclic glycine derivatives of 7-aminodeacetoxycephalosporanic acid Stjepan Kukolja, Susan E. Draheim, Bernard J. Graves, David C. Hunden, Janice L. Pfeil, Robin D. G. Cooper, John L. Ott, and Fred T. Counter pp 1896 - 1903; DOI: 10.1021/jm00150a023 |
Orally absorbable cephalosporin antibiotics. 3. Preparation of biologically active R-isomer of 7-(3-benzothienylglycylamido)deacetoxycephalosporanic acid Stjepan Kukolja, Janice L. Pfeil, Susan E. Draheim, and John L. Ott pp 1903 - 1906; DOI: 10.1021/jm00150a024 |
[[(4,5-Dihydro-2-oxazolyl)phenoxy]alkyl]isoxazoles. Inhibitors of picornavirus uncoating G. D. Diana, M. A. McKinlay, M. J. Otto, V. Akullian, and C. Oglesby pp 1906 - 1910; DOI: 10.1021/jm00150a025 |
Quantitative structure-activity relationship of antifolate inhibition of bacteria cell cultures resistant and sensitive to methotrexate Eugene A. Coats, Clara S. Genther, Cynthia Dias Selassie, Cynthia D. Strong, and Corwin Hansch pp 1910 - 1916; DOI: 10.1021/jm00150a026 |
Acylamido boronic acids and difluoroborane analogs of amino acids: potent inhibitors of chymotrypsin and elastase David H. Kinder and John A. Katzenellenbogen pp 1917 - 1925; DOI: 10.1021/jm00150a027 |
New antihistaminic N-heterocyclic 4-piperidinamines. 1. Synthesis and antihistaminic activity of N-(4-piperidinyl)-1H-benzimidazol-2-amines Frans Janssens, Joseph Torremans, Marcel Janssen, Raymond A. Stokbroekx, Marcel Luyckx, and Paul A. J. Janssen pp 1925 - 1933; DOI: 10.1021/jm00150a028 |
New antihistaminic N-heterocyclic 4-piperidinamines. 2. Synthesis and antihistaminic activity of 1-[(4-fluorophenyl)methyl]-N-(4-piperidinyl)-1H-benzimidazol-2-amines Frans Janssens, Joseph Torremans, Marcel Janssen, Raymond A. Stokbroekx, Marcel Luyckx, and Paul A. J. Janssen pp 1934 - 1943; DOI: 10.1021/jm00150a029 |
New antihistaminic N-heterocyclic 4-piperidinamines. 3. Synthesis and antihistaminic activity of N-(4-piperidinyl)-3H-imidazo[4,5-b]pyridin-2-amines Frans Janssens, Joseph Torremans, Marcel Janssen, Raymond A. Stokbroekx, Marcel Luyckx, and Paul A. J. Janssen pp 1943 - 1947; DOI: 10.1021/jm00150a030 |
Racemic and optically active 1,3,3-trimethyl-4-phenyl-4-(propionyloxy)piperidine F. R. Ahmed, G. F. Laws, A. E. Madani, and A. F. Casy pp 1947 - 1949; DOI: 10.1021/jm00150a031 |
Hybromet: a ligand for purifying opioid receptors Sydney Archer, Josephine Michael, Peter Osei-Gyimah, Ahmad Seyed-Mozaffari, R. Suzanne Zukin, Rhoda Maneckjee, Eric J. Simon, and Theresa L. Gioannini pp 1950 - 1953; DOI: 10.1021/jm00150a032 |
1-Benzylcyclopropylamine and 1-(aminomethyl)-1-phenylcyclopropane: an inactivator and a substrate of monoamine oxidase Richard B. Silverman and Paul A. Zieske pp 1953 - 1957; DOI: 10.1021/jm00150a033 |
A dipeptide derived from kainic and L-glutamic acids: a selective antagonist of amino acid induced neuroexcitation with anticonvulsant properties Ora Goldberg and Vivian I. Teichberg pp 1957 - 1958; DOI: 10.1021/jm00150a034 |
Sulfur-interrupted 8-amino side chain analogs of 4-methyl-5-[m-(trifluoromethyl)phenoxy]primaquine as potential antimalarial agents F. Ivy Carroll, Bertold Berrang, and C. P. Linn pp 1959 - 1962; DOI: 10.1021/jm00150a035 |
3,4-O-Diacetylisoproterenol. Preparation, structure proof and .beta.-receptor effect Palle Jakobsen, Svend Treppendahl, Peter H. Andersen, Rene Klysner, Arne Geisler, and Lene Teuber pp 1962 - 1964; DOI: 10.1021/jm00150a036 |
Additions and Corrections - A Mechanism for the Addition of Multiple Moles of Glutamate by Folypolyglutamate Synthetase. Richard G. Moran, Paul D. Colman, Ronald A. Forsch, and Andre Rosowsky pp 1965 - 1965; DOI: 10.1021/jm00150a600 |
Additions and Corrections - N-Allyl Analogues of Phencyclidine: Chemical Synthesis and Pharmacological Properties. Asher Kalir, Shoshana Teomy, Adina Amir, P. Fuchs, Sung A. Lee, Elzbieta J. Holsztynska, Wieslaw Rocki, and Edward F. Domino pp 1965 - 1965; DOI: 10.1021/jm00150a601 |
Additions and Corrections - 5-Cinnamoyl-6-aminouracil Derivatives as Novel Anticancer Agents. Synthesis, Biological Evaluation, and Structure-Activity Relationships. Jean-Luc Bernier, Jean-Pierre Hénichart, Vincent Warin, Chantal Trentasaux, and Jean-Claude Jardillier pp 1965 - 1965; DOI: 10.1021/jm00150a602 |
Additions and Corrections - Synthesis and Central Dopaminergic Effects of N-(4,6-Dimethyl-2-pyridinyl)benzamides. Said Bouhayat, Sylvie Piessard, Guillaume LeBaut, Louis Sparfel, Jean-Yves Petit, François Piriou, and Lucien Welin pp 1965 - 1965; DOI: 10.1021/jm00150a603 |
Additions and Corrections - Effect of Structural Modification of the Hydantoin Ring on Anticonvulsant Activity Sergio Cortes, Zeng-Kun Liao, Darrell Watson, and Harold Kohn pp 1965 - 1965; DOI: 10.1021/jm00150a604 |
Additions and Corrections - Peptide Sweeteners. 8. Synthesis and Structure-Taste Relationship Studies of L-Aspartyl-D-alanyl Tripeptides. Marc Rodriguez, John M. Bland, Joseph W. Tsang, and Murray Goodman pp 1965 - 1965; DOI: 10.1021/jm00150a605 |
Additions and Corrections - Resolution of Aristeromycin Enantiomers. Piet Herdewijn, Jan Balzarini, Erik De Clercq, and Hubert Vanderhaeghe pp 1965 - 1965; DOI: 10.1021/jm00150a606 |
Book Reviews pp 1966 - 1968; DOI: 10.1021/jm00150a607 |
N-(2,3-Butadienyl)-1,4-butanediamine derivatives: potent irreversible inactivators of mammalian polyamine oxidase Philippe Bey, Frank N. Bolkenius, Nikolaus Seiler, and Patrick Casara pp 1 - 2; DOI: 10.1021/jm00379a001 |
1H-2-Benzopyran-1-one derivatives, microbial products with pharmacological activity. Conversion into orally active derivatives with antiinflammatory and antiulcer activities Yukiji Shimojima, Takashi Shirai, Tsuneo Baba, and Hiroshi Hayashi pp 3 - 9; DOI: 10.1021/jm00379a002 |
Comparison of the hypolipidemic activity of cyclic vs. acyclic imides P. Josee Voorstad, J. M. Chapman, G. H. Cocolas, S. D. Wyrick, and Iris H. Hall pp 9 - 12; DOI: 10.1021/jm00379a003 |
2-(.beta.-Arylethylamino)- and 4-(.beta.-arylethylamino)quinazolines as phosphodiesterase inhibitors J. Millen, Thomas N. Riley, I. W. Waters, and M. E. Hamrick pp 12 - 17; DOI: 10.1021/jm00379a004 |
Mechanism-based inactivation of N-arylhydroxamic acid N,O-acyltransferase by 7-substituted-N-hydroxy-2-acetamidofluorenes Virginia C. Marhevka, Nancy A. Ebner, Russell D. Sehon, and Patrick E. Hanna pp 18 - 24; DOI: 10.1021/jm00379a005 |
[1,4]Benzoxazine-2,3-diones as antiallergic agents Bernard Loev, Howard Jones, Richard E. Brown, Fu Chih Huang, Atul Khandwala, Mitchell J. Leibowitz, and Paula Sonnino-Goldman pp 24 - 27; DOI: 10.1021/jm00379a006 |
Sleep-inducing N-alkyl-5-[m-(trifluoromethyl)phenyl]-5-hydroxy-2-pyrrolidinones and N-alkyl-3-(trifluoromethyl)cinnamamides William J. Houlihan, John H. Gogerty, Eileen A. Ryan, and Gemma Schmitt pp 28 - 31; DOI: 10.1021/jm00379a007 |
Lack of influence of the carbamoyl group on the stereochemistry of the acid-catalyzed opening of the aziridine ring of the mitomycins and of congeners Ulfert Hornemann, Paul J. Keller, and Kazuyoshi Takeda pp 31 - 36; DOI: 10.1021/jm00379a008 |
Inhibition of liver alcohol dehydrogenase and ethanol metabolism by 3-substituted thiolane 1-oxides Vijay K. Chadha, Kevin G. Leidal, and Bryce V. Plapp pp 36 - 40; DOI: 10.1021/jm00379a009 |
Uridine 5'-diphosphate glucose analogs. Inhibitors of protein glycosylation that show antiviral activity Maria Jose Camarasa, Piedad Fernandez-Resa, Maria Teresa Garcia-Lopez, Federico G. De las Heras, Paloma P. Mendez-Castrillon, Balbino Alarcon, and Luis Carrasco pp 40 - 46; DOI: 10.1021/jm00379a010 |
Metabolism of phencyclidine. The role of the carbinolamine intermediate in the formation of lactam and amino acid metabolites of nitrogen heterocycles John K. Baker and Thomas L. Little pp 46 - 50; DOI: 10.1021/jm00379a011 |
Drug glycosides: potential prodrugs for colon-specific drug delivery David R. Friend and George W. Chang pp 51 - 57; DOI: 10.1021/jm00379a012 |
Angiotensin-converting enzyme inhibitors. New orally active antihypertensive (mercaptoalkanoyl)- and [(acylthio)alkanoyl]glycine derivatives John T. Suh, Jerry W. Skiles, Bruce E. Williams, Raymond D. Youssefyeh, Howard Jones, Bernard Loev, Edward S. Neiss, Alfred Schwab, William S. Mann, and et al. pp 57 - 66; DOI: 10.1021/jm00379a013 |
3-(1-Indolinyl)benzylamines: a new class of analgesic agents Edward J. Glamkowski, James M. Fortunato, Theodore C. Spaulding, Jeffrey C. Wilker, and Daniel B. Ellis pp 66 - 73; DOI: 10.1021/jm00379a014 |
Facile synthesis of platelet-activating factor and racemic analogs containing unsaturation in the sn-1-alkyl chain Jefferson R. Surles, Robert L. Wykle, Joseph T. O'Flaherty, William L. Salzer, Michael J. Thomas, Fred Snyder, and Claude Piantadosi pp 73 - 78; DOI: 10.1021/jm00379a015 |
[(Aminomethyl)aryloxy]acetic acid esters. A new class of high-ceiling diuretics. 3. Variation in the bridge between the aromatic rings to complete mapping of the receptor Jacob J. Plattner, Yvonne C. Martin, Jill R. Smital, Cheuk Man Lee, Anthony K. L. Fung, Bruce W. Horrom, Steven R. Crowley, Andre G. Pernet, Paul R. Bunnell, and Ki H. Kim pp 79 - 93; DOI: 10.1021/jm00379a016 |
Diterpenoid sweeteners. Synthesis and sensory evaluation of stevioside analogs with improved organoleptic properties Grant E. DuBois and Rebecca A. Stephenson pp 93 - 98; DOI: 10.1021/jm00379a017 |
Ribavirin, tiazofurin, and selenazofurin: mononucleotides and nicotinamide adenine dinucleotide analogs. Synthesis, structure, and interactions with IMP dehydrogenase Gulilat Gebeyehu, Victor E. Marquez, Anne Van Cott, David A. Cooney, James A. Kelley, Hiremagalur N. Jayaram, Gurpreet S. Ahluwalia, Robert L. Dion, Yvonne A. Wilson, and David G. Johns pp 99 - 105; DOI: 10.1021/jm00379a018 |
.gamma.-Aminobutyric acid esters. 2. Synthesis, brain uptake, and pharmacological properties of lipid esters of .gamma.-aminobutyric acid James N. Jacob, Victor E. Shashoua, Alexander Campbell, and Ross J. Baldessarini pp 106 - 110; DOI: 10.1021/jm00379a019 |
Synthesis of some quaternary ammonium alkylating agents and their effects on soman-inhibited acetylcholinesterase Allan P. Gray, Robert D. Platz, Timothy C. P. Chang, Theresa R. Leverone, David A. Ferrick, and David N. Kramer pp 111 - 116; DOI: 10.1021/jm00379a020 |
Synthesis and characterization of selected heteroarotinoids. Pharmacological activity as assessed in vitamin A deficient hamster tracheal organ cultures. Single-crystal x-ray diffraction analysis of 4,4-dimethylthiochroman-6-yl methyl ketone 1,1-dioxide and ethyl (E)-p-[2-(4,4-dimethylthiochroman-6-yl)propenyl]benzoate Kristy M. Waugh, K. Darrell Berlin, Warren T. Ford, Elizabeth M. Holt, John P. Carrol, Paul R. Schomber, M. Daniel Thompson, and Leonard J. Schiff pp 116 - 124; DOI: 10.1021/jm00379a021 |
Conformational properties of central nervous system active thyrotropin releasing hormone analogs: probing structure-activity relationships at the molecular level Emil Eckle and John J. Stezowski pp 125 - 137; DOI: 10.1021/jm00379a022 |
The covalent linking of two nucleotide analogs to antibodies Esther Hurwitz, Rina Kashi, Ruth Arnon, Meir Wilchek, and Michael Sela pp 137 - 140; DOI: 10.1021/jm00379a023 |
Substrate specificity of pyroglutamylaminopeptidase John T. Capecchi and Gordon Marc Loudon pp 140 - 143; DOI: 10.1021/jm00379a024 |
Potentiation of fasciolicidal agents by benzoyl side chains, synthesis of benzoylsalicylanilides George R. Brown, Glynn J. Chesterson, and Gerald C. Coles pp 143 - 146; DOI: 10.1021/jm00379a025 |
Reactivators of organophosphorus-inhibited acetylcholinesterase. 1. Imidazole oxime derivatives M. Mar Herrador, Jesus Saenz de Buruaga, and M. Dolores Suarez pp 146 - 149; DOI: 10.1021/jm00379a026 |
Relationship between structure and antineoplastic activity of (arylsulfonyl)hydrazones of 4-pyridinecarboxaldehyde Krishnamurthy Shyam, Lucille A. Cosby, and Alan C. Sartorelli pp 149 - 152; DOI: 10.1021/jm00379a027 |
An interdisciplinary approach to the design of new structures active at the .beta.-adrenergic receptor. Aliphatic oxime ether derivatives B. Macchia, A. Balsamo, A. Lapucci, A. Martinelli, F. Macchia, M. C. Breschi, B. Fantoni, and E. Martinotti pp 153 - 160; DOI: 10.1021/jm00380a001 |
Syntheses and complement inhibitory activities of 4-(2-phenyl-1H-indol-3-yl)cyclohexane-1-carboxylic acids Denis M. Bailey, George D. DeGrazia, E. John Alexander, Ronald G. Powles, Robert E. Johnson, Richard A. Patrick, Barbara G. Heerdt, Margo E. Fairbain, and Donald J. Pruden pp 160 - 164; DOI: 10.1021/jm00380a002 |
Imidazo[1,5-a]pyridines: a new class of thromboxane A2 synthetase inhibitors Neville F. Ford, Leslie J. Browne, Thomas Campbell, Charles Gemenden, Robert Goldstein, Candido Gude, and Jan W. F. Wasley pp 164 - 170; DOI: 10.1021/jm00380a003 |
Nucleoside conjugates. 6. Synthesis and comparison of antitumor activity of 1-.beta.-D-arabinofuranosylcytosine conjugates of corticosteroids and selected lipophilic alcohols Chung I. Hong, Alan J. Kirisits, Alexander Nechaev, David J. Buchheit, and Charles R. West pp 171 - 177; DOI: 10.1021/jm00380a004 |
Synthesis, stereochemistry, and analgesic activity of 4-mono- and 4,4-disubstituted 1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocines Abiodun O. Ogundaini and Robert T. Parfitt pp 177 - 181; DOI: 10.1021/jm00380a005 |
Structure-activity studies on the N-terminal region of growth hormone releasing factor David H. Coy, William A. Murphy, Javier Sueiras-Diaz, Esther J. Coy, and Valentine A. Lance pp 181 - 185; DOI: 10.1021/jm00380a006 |
Enzyme-activated irreversible inhibitors of monoamine oxidase: phenylallylamine structure-activity relationships Ian A. McDonald, Jean Michel Lacoste, Philippe Bey, Michael G. Palfreyman, and Monique Zreika pp 186 - 193; DOI: 10.1021/jm00380a007 |
22-Hydroxycholesterol derivatives as HMG CoA reductase suppressors and serum cholesterol lowering agents Robert J. Chorvat, Bipin N. Desai, Suzanne Evans Radak, Kathleen T. Perko, James E. Miller, Charlene Jett, and Elaine Rohrbacher pp 194 - 200; DOI: 10.1021/jm00380a008 |
Analogs of aminoglutethimide: selective inhibition of aromatase Allan B. Foster, Michael Jarman, Chui Sheung Leung, Martin G. Rowlands, and Grahame N. Taylor pp 200 - 204; DOI: 10.1021/jm00380a009 |
Amino acid derived latent isocyanates: irreversible inactivation of porcine pancreatic elastase and human leukocyte elastase William C. Groutas, William R. Abrams, Michael C. Theodorakis, Annette M. Kasper, Steven A. Rude, Robert C. Badger, Timothy D. Ocain, Kevin E. Miller, Min K. Moi, and et al. pp 204 - 209; DOI: 10.1021/jm00380a010 |
Chemistry and antitumor evaluation of selected classical 2,4-diaminoquinazoline analogs of folic acid J. B. Hynes, S. J. Harmon, G. G. Floyd, M. Farrington, L. D. Hart, G. R. Gale, W. L. Washtien, S. S. Susten, and J. H. Freisheim pp 209 - 215; DOI: 10.1021/jm00380a011 |
Resolved monophenolic 2-aminotetralins and 1,2,3,4,4a,5,6,10b-octahydrobenzo[f]quinolines: structural and stereochemical considerations for centrally acting pre- and postsynaptic dopamine-receptor agonists Haakan Wikstroem, Bengt Andersson, Domingo Sanchez, Per Lindberg, Lars Erik Arvidsson, Anette M. Johansson, J. Lars G. Nilsson, Kjell Svensson, Stephan Hjorth, and Arvid Carlsson pp 215 - 225; DOI: 10.1021/jm00380a012 |
Substituted 5H-dibenz[b,g]-1,4-oxazocines and related amino acids with antiinflammatory activity Michael R. Stillings, Stephen Freeman, Peter L. Myers, Michael J. Readhead, Anthony P. Welbourn, Michael J. Rance, and David C. Atkinson pp 225 - 233; DOI: 10.1021/jm00380a013 |
Mineralocorticoid properties of potential metabolites of 18-hydroxydeoxycorticosterone and 18-hydroxyprogesterone John F. Weet and George R. Lenz pp 233 - 239; DOI: 10.1021/jm00380a014 |
Bile acids with cyclopropane-containing side chain. 2. Synthesis and properties of 3.alpha.,7.beta.-dihydroxy-22,23-methylene-5.beta.-cholan-24-oic acid (2-sulfoethyl)amide Roberto Pellicciari, Sergio Cecchetti, Benedetto Natalini, Aldo Roda, Brunella Grigolo, and Adamo Fini pp 239 - 242; DOI: 10.1021/jm00380a015 |
Synthesis and antitumor activity of a series of ftorafur analogs: the effect of varying electronegativity at the 1'-position Mark H. Holshouser, Annette M. Shipp, and Paul W. Ferguson pp 242 - 245; DOI: 10.1021/jm00380a016 |
N-[2-hydroxy-5-[2-(methylamino)ethyl]phenyl]methanesulfonamide. A potent agonist which releases intracellular calcium by activation of .alpha.1-adrenoceptors Robert M. DeMarinis, Patricia Lavanchy, J. Paul Hieble, Kam F. Jim, and William D. Matthews pp 245 - 248; DOI: 10.1021/jm00380a017 |
Folate antagonists. 21. Synthesis and antimalarial properties of 2,4-diamino-6-(benzylamino)pyrido[3,2-d]pyrimidines Norman L. Colbry, Edward F. Elslager, and Leslie M. Werbel pp 248 - 252; DOI: 10.1021/jm00380a018 |
Fluorine-containing amino acids and their derivatives. 4. Synthesis and antibacterial activity of threo and erythro 1-fluorodehydroxylated chloramphenicol analogs Tadahiko Tsushima, Kenji Kawada, Teruji Tsuji, and Katsuya Tawara pp 253 - 256; DOI: 10.1021/jm00380a019 |
3,4-Diphenyl-1H-pyrazole-1-propanamine antidepressants Denis M. Bailey, Philip E. Hansen, Allan G. Hlavac, Eugene R. Baizman, Jack Pearl, Albert F. DeFelice, and Martin E. Feigenson pp 256 - 260; DOI: 10.1021/jm00380a020 |
Additions and Corrections - Actinidin Hydrolysis of Substituted-Phenyl Hippurates: A Quantitative Structure-Activity Relationship and Graphics Comparison with Hydrolysis by Papain. Angelo Carotti, Corwin Hansch, Monica M. Mueller, and Jeffrey M. Blaney pp 261 - 261; DOI: 10.1021/jm00380a600 |
Pepstatin-derived inhibitors of aspartic proteinases. A close look at an apparent transition-state analog inhibitor Daniel H. Rich pp 263 - 273; DOI: 10.1021/jm00381a001 |
Structure-activity relationships of C-terminal tri- and tetrapeptide fragments that inhibit gastrin activity Jean Martinez, Jean Pierre Bali, Richard Magous, Janine Laur, Marie Francoise Lignon, Christian Briet, Dino Nisato, and Bertrand Castro pp 273 - 278; DOI: 10.1021/jm00381a002 |
Synthesis of new polyoxin derivatives and their activity against chitin synthase from Candida albicans Gerhard Emmer, Neil S. Ryder, and Maximilian A. Grassberger pp 278 - 281; DOI: 10.1021/jm00381a003 |
Alkyl esters of 3-adenin-9-yl-2-hydroxypropanoic acid: a new class of broad-spectrum antiviral agents Erik De Clercq and Antonin Holy pp 282 - 287; DOI: 10.1021/jm00381a004 |
Thromboxane synthetase inhibitors (TXSI). Design, synthesis, and evaluation of a novel series of .omega.-pyridylalkenoic acids Kaneyoshi Kato, Shigenori Ohkawa, Shinji Terao, Zenichi Terashita, and Kohei Nishikawa pp 287 - 294; DOI: 10.1021/jm00381a005 |
Synthesis and antiarrhythmic and parasympatholytic properties of substituted phenols. 3. Modifications to the linkage region (region 3) David M. Stout, W. L. Matier, Cynthia Barcelon-Yang, Robert D. Reynolds, and Barry S. Brown pp 295 - 298; DOI: 10.1021/jm00381a006 |
Synthesis and antiallergic activity of some quinolinones and imidazoquinolinones Norton P. Peet, Larry E. Baugh, Shyam Sunder, and Jon E. Lewis pp 298 - 302; DOI: 10.1021/jm00381a007 |
Receptor-based design of dihydrofolate reductase inhibitors: comparison of crystallographically determined enzyme binding with enzyme affinity in a series of carboxy-substituted trimethoprim analogs Lee F. Kuyper, Barbara Roth, David P. Baccanari, Robert Ferone, Christopher R. Beddell, John N. Champness, David K. Stammers, John G. Dann, Frank E. A. Norrington, and et al. pp 303 - 311; DOI: 10.1021/jm00381a008 |
Synthesis and dihydropteridine reductase inhibitory effects of potential metabolites of the neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine Wieslaw Gessner, Arnold Brossi, Rong Sen Shen, and Creed W. Abell pp 311 - 317; DOI: 10.1021/jm00381a009 |
Artificial siderophores. 1. Synthesis and microbial iron transport capabilities Byung Hyun Lee, Marvin J. Miller, Catherine A. Prody, and John B. Neilands pp 317 - 323; DOI: 10.1021/jm00381a010 |
Artificial siderophores. 2. Syntheses of trihydroxamate analogs of rhodotorulic acid and their biological iron transport capabilities in Escherichia coli Byung Hyun Lee, Marvin J. Miller, Catherine A. Prody, and John B. Neilands pp 323 - 327; DOI: 10.1021/jm00381a011 |
Angiotensin converting enzyme inhibitors. (Mercaptoaroyl)amino acids Paul R. Menard, John T. Suh, Howard Jones, Bernard Loev, Edward S. Neiss, Joyce Wilde, Alfred Schwab, and William S. Mann pp 328 - 332; DOI: 10.1021/jm00381a012 |
Use of physicochemical parameters in distance geometry and related three-dimensional quantitative structure-activity relationships: A demonstration using Escherichia coli dihydrofolate reductase inhibitors Arup K. Ghose and Gordon M. Crippen pp 333 - 346; DOI: 10.1021/jm00381a013 |
3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. I. Structural modification of 5-substituted 3,5-dihydroxypentanoic acids and their lactone derivatives G. E. Stokker, W. F. Hoffman, A. W. Alberts, E. J. Cragoe Jr., A. A. Deana, J. L. Gilfillan, J. W. Huff, F. C. Novello, J. D. Prugh, and et al. pp 347 - 358; DOI: 10.1021/jm00381a014 |
Acyclic analogs of 2'-deoxynucleosides related to 9-[(1,3-dihydroxy-2-propoxy)methyl]guanine as potential antiviral agents John C. Martin, Gary A. Jeffrey, Danny P. C. McGee, Michael A. Tippie, Donald F. Smee, Thomas R. Matthews, and Julien P. H. Verheyden pp 358 - 362; DOI: 10.1021/jm00381a015 |
1,2,4-Triazolo[4,3-a]quinoxaline-1,4-diones as antiallergic agents Bernard Loev, John H. Musser, Richard E. Brown, Howard Jones, Robert Kahen, Fu Chih Huang, Atul Khandwala, Paula Sonnino-Goldman, and Mitchell J. Leibowitz pp 363 - 366; DOI: 10.1021/jm00381a016 |
Octahydrobenzo[g]quinolines: potent dopamine agonists which show the relationship between ergolines and apomorphine Rene Nordmann and Trevor J. Petcher pp 367 - 375; DOI: 10.1021/jm00381a017 |
Molecular interactions of toxic chlorinated dibenzo-p-dioxins and dibenzofurans with thyroxine binding prealbumin James D. McKinney, Kun Chae, Stuart J. Oatley, and Colin C. F. Blake pp 375 - 381; DOI: 10.1021/jm00381a018 |
[3H]Batrachotoxinin A 20.alpha.-benzoate binding to voltage-sensitive sodium channels: a rapid and quanitative assay for local anesthetic activity in a variety of drugs Elizabeth T. McNeal, Gail A. Lewandowski, John W. Daly, and C. R. Creveling pp 381 - 388; DOI: 10.1021/jm00381a019 |
Bicyclic and tricyclic analogs of anthramycin T. Kaneko, H. Wong, T. W. Doyle, W. C. Rose, and W. T. Bradner pp 388 - 392; DOI: 10.1021/jm00381a020 |
Conformational analysis and active site modeling of angiotensin-converting enzyme inhibitors P. R. Andrews, J. M. Carson, A. Caselli, M. J. Spark, and R. Woods pp 393 - 399; DOI: 10.1021/jm00381a021 |
The pKa of butaclamol and the mode of butaclamol binding to central dopamine receptors Frank A. Chrzanowski, Beth A. McGrogan, and Bruce E. Maryanoff pp 399 - 400; DOI: 10.1021/jm00381a022 |
Compactin (ML-236B) and related compounds as potential cholesterol-lowering agents that inhibit HMG-CoA reductase Akira Endo pp 401 - 405; DOI: 10.1021/jm00382a001 |
Novel photoaffinity label for the dopamine D2 receptor: synthesis of 4-amino-5-iodo-2-methoxy-N-[1-(phenylmethyl)-4-piperidinyl]benzamide (iodoazidoclebopride, IAC) and the corresponding 125I-labeled analog (125IAC) John L. Neumeyer, Ji Hua Guan, H. B. Niznik, A. Dumbrille-Ross, Philip Seeman, Sreenivasan Padmanabhan, and David R. Elmaleh pp 405 - 407; DOI: 10.1021/jm00382a002 |
Myocardial imaging agents: synthesis, characterization, and evaluation of (Z)- and (Z,E)-18-[82Br]bromo-5-tellura-17-octadecenoic acids P. C. Srivastava, F. F. Knapp, A. P. Callahan, B. A. Owen, G. W. Kabalka, and K. A. R. Sastry pp 408 - 413; DOI: 10.1021/jm00382a003 |
Spiro[4.5] and spiro[4.6] carboxylic acids: cyclic analogs of valproic acid synthesis and anticonvulsant evaluation K. R. Scott, Jacqueline A. Moore, Theodore B. Zalucky, Jesse M. Nicholson, Jo Ann M. Lee, and Christine N. Hinko pp 413 - 417; DOI: 10.1021/jm00382a004 |
Synthesis and antitumor and antiviral activities of a series of 1-.beta.-D-ribofuranosyl-5-halocytosine (5-halocytidine) cyclic 3',5'-monophosphates Jozsef Beres, Wesley G. Bentrude, Gabor Kruppa, Patricia A. McKernan, and Roland K. Robins pp 418 - 422; DOI: 10.1021/jm00382a005 |
Synthesis and biological activity of a novel adenosine analog 3-.beta.-D-ribofuranosylthieno[2,3-d]pyrimidin-4-one Vemanna D. Patil, Dean S. Wise, Linda L. Wotring, Linda C. Bloomer, and Leroy B. Townsend pp 423 - 427; DOI: 10.1021/jm00382a006 |
Aldosterone antagonists. 1. Synthesis and biological activities of 11.beta.,18-epoxypregnane derivatives Susumu Kamata, Nobuhiro Haga, Takashi Mitsugi, Eiji Kondo, Wataru Nagata, Masuhisa Nakamura, Kenji Miyata, Kunihiro Odaguchi, Toshikatsu Shimizu, and et al. pp 428 - 433; DOI: 10.1021/jm00382a007 |
Angiotensin-converting enzyme inhibitors: synthesis and biological activity of acyltripeptide analogs of enalapril William J. Greenlee, Patricia L. Allibone, Debra S. Perlow, Arthur A. Patchett, Edgar H. Ulm, and Theodore C. Vassil pp 434 - 442; DOI: 10.1021/jm00382a008 |
Synthesis and platelet aggregation inhibitory activity of 4,5-bis(substituted)-1,2,3-thiadiazoles Edward W. Thomas, Edward E. Nishizawa, David C. Zimmermann, and Davey J. Williams pp 442 - 446; DOI: 10.1021/jm00382a009 |
7-Substituted-4-hydroxyquinoline-3-carboxylic acids as inhibitors of dehydrogenase enzymes and of the respiration of Ehrlich ascites tumor cells: multivariate analysis and quantitative structure-activity relationship for polar substituents S. Dove, E. Coats, P. Scharfenberg, and R. Franke pp 447 - 451; DOI: 10.1021/jm00382a010 |
Selective uptake of a toxic lipophilic anthracycline derivative by the low density lipoprotein receptor pathway in cultured fibroblasts Sigurd G. Vitols, Michele Masquelier, and Curt O. Peterson pp 451 - 454; DOI: 10.1021/jm00382a011 |
Conjugation of poly(styrene-co-maleic acid) derivatives to the antitumor protein neocarzinostatin: pronounced improvements in pharmacological properties Hiroshi Maeda, Minoru Ueda, Tetsuo Morinaga, and Tomonori Matsumoto pp 455 - 461; DOI: 10.1021/jm00382a012 |
Analgesics of the 6,14-ethenomorphinan type. 6-Deoxy-7.alpha.-orvinol and 6-deoxy-8.alpha.-orvinol Laura L. Knipmeyer and Henry Rapoport pp 461 - 466; DOI: 10.1021/jm00382a013 |
Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 8. Molecular dissections of carbocyclic 3-deazaadenosine as inhibitors of S-adenosylhomocysteine hydrolase D. Michael Houston, E. K. Dolence, Bradley T. Keller, Usha Patel-Thombre, and Ronald T. Borchardt pp 467 - 471; DOI: 10.1021/jm00382a014 |
Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 9. 2',3'-Dialdehyde derivatives of carbocyclic purine nucleosides as inhibitors of S-adenosylhomocysteine hydrolase D. Michael Houston, E. K. Dolence, Bradley T. Keller, Usha Patel-Thombre, and Ronald T. Borchardt pp 471 - 477; DOI: 10.1021/jm00382a015 |
Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 10. Base- and amino acid modified analogs of S-aristeromycinyl-L-homocysteine D. Michael Houston, Bozena Matuszewska, and Ronald T. Borchardt pp 478 - 482; DOI: 10.1021/jm00382a016 |
A new class of cardiotonic agents: structure-activity correlations for natural and synthetic analogs of the alkaloid pumiliotoxin B (8-hydroxy-8-methyl-6-alkylidene-1-azabicyclo[4.3.0]nonanes) J. W. Daly, E. T. McNeal, L. E. Overman, and D. H. Ellison pp 482 - 486; DOI: 10.1021/jm00382a017 |
1,3-Dialkyl-8-(p-sulfophenyl)xanthines: potent water-soluble antagonists for A1- and A2-adenosine receptors John W. Daly, W. Padgett, M. T. Shamim, P. Butts-Lamb, and J. Waters pp 487 - 492; DOI: 10.1021/jm00382a018 |
Structure-activity relationship of estrogens: receptor affinity and estrogen antagonist activity of certain (E)- and (2)-1,2,3-triaryl-2-propen-2-ones Shubhra Mittal, Susheel Durani, and Randhir S. Kapil pp 492 - 497; DOI: 10.1021/jm00382a019 |
5-Cinnamoyl-6-aminouracil derivatives as novel anticancer agents. Synthesis, biological evaluation, and structure-activity relationships Jean Luc Bernier, Jean Pierre Henichart, Vincent Warin, Chantal Trentesaux, and Jean Claude Jardillier pp 497 - 502; DOI: 10.1021/jm00382a020 |
Stereoselective metabolism of conformational analogs of warfarin by .beta.-naphthoflavone-inducible cytochrome P-450 L. D. Heimark and W. F. Trager pp 503 - 506; DOI: 10.1021/jm00382a021 |
Specific inhibition of benzodiazepine receptor binding by some N-(indol-3-ylglyoxylyl)amino acid derivatives Claudia Martini, Teresa Gervasio, Antonio Lucacchini, Antonio Da Settimo, Giampaolo Primofiore, and Anna M. Marini pp 506 - 509; DOI: 10.1021/jm00382a022 |
Conformational factors in cardiac glycoside activity Francis C. K. Chiu and Thomas R. Watson pp 509 - 515; DOI: 10.1021/jm00382a023 |
Synthesis and dopaminergic activity of (R)- and (S)-4-hydroxy-2-(di-n-propylamino)indan Joseph G. Cannon, Russell G. Dushin, John Paul Long, Mustafa Ilhan, Noel D. Jones, and John K. Swartzendruber pp 515 - 518; DOI: 10.1021/jm00382a024 |
Synthesis and .beta.-lactamase inhibitory properties of 2.beta.-[(acyloxy)methyl]-2.alpha.-methylpenam-3.alpha.-carboxylic acid 1,1-dioxides William J. Gottstein, Ute J. Haynes, and Donald N. McGregor pp 518 - 522; DOI: 10.1021/jm00382a025 |
Dicesium N-succinimidyl 3-(undecahydro-closo-dodecaboranyldithio)propionate, a novel heterobifunctional boronating agent Fazlul Alam, Albert H. Soloway, James E. McGuire, Rolf F. Barth, Walter E. Carey, and Dianne Adams pp 522 - 525; DOI: 10.1021/jm00382a026 |
Synthesis and evaluation of N,N'-bis(arylsulfonyl)hydrazines as antineoplastic agents Krishnamurthy Shyam, Lucille A. Cosby, and Alan C. Sartorelli pp 525 - 527; DOI: 10.1021/jm00382a027 |
Book Reviews pp 527 - 536; DOI: 10.1021/jm00382a600 |
Synthesis of pyrrolizidine alkaloids indicine, intermedine, lycopsamine, and analogs and their N-oxides. Potential antitumor agents Leon H. Zalkow, Jan A. Glinski, Leslie T. Gelbaum, Thomas J. Fleischmann, Laureen S. McGowan, and Maureen M. Gordon pp 687 - 694; DOI: 10.1021/jm00383a001 |
Synthesis and antidepressant profiles of phenyl-substituted 2-amino- and 2-[(alkoxycarbonyl)amino]-1,4,5,6-tetrahydropyrimidines Klaus Weinhardt, Marshall B. Wallach, and Michael Marx pp 694 - 698; DOI: 10.1021/jm00383a002 |
1-Azacycloalkyl-1,4-benzodiazepin-2-ones with antianxiety-antidepressant actions Tsutomu Sugasawa, Makoto Adachi, Kazuyuki Sasakura, Akira Matsushita, Masami Eigyo, Teruo Shiomi, Haruyuki Shintaku, Yukio Takahara, and Shunji Murata pp 699 - 707; DOI: 10.1021/jm00383a003 |
Synthesis and cytotoxic activity of hydroxylated derivatives of olivacine in relation with their biotransformation M. Maftouh, R. Besselievre, B. Monsarrat, P. Lesca, B. Meunier, H. P. Husson, and C. Paoletti pp 708 - 714; DOI: 10.1021/jm00383a004 |
New antiarrhythmic agents. N-Aryl-8-pyrrolizidinealkanamides Seiji Miyano, Kunihiro Sumoto, Fumio Satoh, Keiyu Shima, Mariko Hayashimatsu, Minoru Morita, Kazuo Aisaka, and Teruhisa Noguchi pp 714 - 717; DOI: 10.1021/jm00383a005 |
Structure-activity relationships of arylimidazopyridine cardiotonics: discovery and inotropic activity of 2-[2-methoxy-4-(methylsulfinyl)phenyl]-1H-imidazo[4,5-c]pyridine David W. Robertson, E. E. Beedle, Joseph H. Krushinski, G. Don Pollock, Harve Wilson, Virginia L. Wyss, and J. Scott Hayes pp 717 - 727; DOI: 10.1021/jm00383a006 |
Synthesis and antinociceptive activity of 4-(cyclopropylmethyl)-3,4,5,6-tetrahydro-2H-1,5-methano-1,4-benzodiazocin-9-amine and congeners Franklyn W. Gubitz pp 728 - 733; DOI: 10.1021/jm00383a007 |
Synthesis and antimicrobial evaluation of bicyclomycin analogs Robert M. Williams, Robert W. Armstrong, and Jen Sen Dung pp 733 - 740; DOI: 10.1021/jm00383a008 |
Nucleosides. 133. Synthesis of 5-alkenyl-1-(2-deoxy-2-fluoro-.beta.-D-arabinofuranosyl)cytosines and related pyrimidine nucleosides as potential antiviral agents Michael E. Perlman, Kyoichi A. Watanabe, Raymond F. Schinazi, and Jack J. Fox pp 741 - 748; DOI: 10.1021/jm00383a009 |
Isoxazoles with antipicornavirus activity Guy D. Diana, M. A. McKinlay, C. J. Brisson, E. S. Zalay, J. V. Miralles, and U. J. Salvador pp 748 - 752; DOI: 10.1021/jm00383a010 |
Ellipticine derivatives with an affinity to the estrogen receptor. An approach to develop intercalating drugs with a specific effect on the hormone-dependent breast cancer Alain Delbarre, Robert Oberlin, Bernard P. Roques, Jean Louis Borgna, Henri Rochefort, Jean Bernard Le Pecq, and Alain Jacquemin-Sablon pp 752 - 761; DOI: 10.1021/jm00383a011 |
Synthesis and neuroleptic activity of 3-(1-substituted-4-piperidinyl)-1,2-benzisoxazoles Joseph T. Strupczewski, Richard C. Allen, Beth Ann Gardner, Blaine L. Schmid, Ulrich Stache, Edward J. Glamkowski, Michael C. Jones, Daniel B. Ellis, Francis P. Huger, and Robert W. Dunn pp 761 - 769; DOI: 10.1021/jm00383a012 |
Synthesis and pharmacological activity of partially modified retro-inverso dermorphin tetrapeptides Severo Salvadori, Mauro Marastoni, Gianfranco Balboni, Gian Pietro Sarto, and Roberto Tomatis pp 769 - 774; DOI: 10.1021/jm00383a013 |
Thiol-containing androgens as suicide substrates of aromatase Patrick J. Bednarski, David J. Porubek, and Sidney D. Nelson pp 775 - 779; DOI: 10.1021/jm00383a014 |
Synthesis and biological activities of analogs of angiotensins II and III containing O-methyltyrosine and D-tryptophan John M. Matsoukas, Mahesh H. Goghari, Martin N. Scanlon, Kevin J. Franklin, and Graham J. Moore pp 780 - 783; DOI: 10.1021/jm00383a015 |
Hashish: synthesis and central nervous system activity of some novel analogs of cannabidiol and oxepin derivatives of .DELTA.9-tetrahydrocannabinol Vaman S. Jorapur, Zarif H. Khalil, Richard P. Duffley, Raj K. Razdan, Billy R. Martin, Louis S. Harris, and William L. Dewey pp 783 - 787; DOI: 10.1021/jm00383a016 |
Aromatase inhibitors. Synthesis and biological activity of androstenedione derivatives David A. Marsh, Harry J. Brodie, Wesley Garrett, Chon Hwa Tsai-Morris, and Angela M. H. Brodie pp 788 - 795; DOI: 10.1021/jm00383a017 |
Synthesis and antifertility activity of zoapatanol analogs Ramesh M. Kanojia, Eva Chin, Carol Smith, Robert Chen, Deborah Rowand, Seymour D. Levine, Michael P. Wachter, Richard E. Adams, and DoWon Hahn pp 796 - 803; DOI: 10.1021/jm00383a018 |
7.alpha.-Substituted derivatives of androstenedione as inhibitors of estrogen biosynthesis M. V. Darby, J. A. Lovett, R. W. Brueggemeier, M. P. Groziak, and Raymond E. Counsell pp 803 - 807; DOI: 10.1021/jm00383a019 |
Design, synthesis, and evaluation of .omega.-iodovinyl- and .omega.-iodoalkyl-substituted methyl-branched long-chain fatty acids Mark M. Goodman, A. P. Callahan, and F. F. Knapp pp 807 - 815; DOI: 10.1021/jm00383a020 |
N-Phenylpiperazine derivatives with hypocholesterolemic activity Giuseppe Cascio, Elso Manghisi, Roberto Porta, and Giancarlo Fregnan pp 815 - 818; DOI: 10.1021/jm00383a021 |
Synthesis and antiviral activity of 11-azapentacyclo[6.2.1.0.2,70.4,1005,9]decane Stephen L. Sacks, John R. Scheffer, Chong Ze Teh, and Allan Tse pp 819 - 821; DOI: 10.1021/jm00383a022 |
Synthesis of 4'-hydroxypropranolol sulfate, a major non-.beta.-blocking propranolol metabolite in man John E. Oatis, T. Walle, H. B. Daniell, T. E. Gaffney, and Daniel R. Knapp pp 822 - 824; DOI: 10.1021/jm00383a023 |
3-Amino-.beta.-carboline derivatives and the benzodiazepine receptor. Synthesis of a selective antagonist of the sedative action of diazepam Robert H. Dodd, Catherine Ouannes, Lia Prado de Carvalho, Anne Valin, Patrice Venault, Georges Chapouthier, Jean Rossier, and Pierre Potier pp 824 - 828; DOI: 10.1021/jm00383a024 |
S-(Nitrocarbobenzoxy)glutathiones: potent competitive inhibitors of mammalian glyoxalase II P. E. Bush and S. J. Norton pp 828 - 830; DOI: 10.1021/jm00383a025 |
Preparation of 20-(hydroxymethyl)-4-methyl-4-aza-2-oxa-5.alpha.-pregnan-3-one as an inhibitor of testosterone 5.alpha.-reductase Philip M. Weintraub, Thomas R. Blohm, and Marie Laughlin pp 831 - 833; DOI: 10.1021/jm00383a026 |
Synthesis and antiviral evaluation of nucleosides of 5-methylimidazole-4-carboxamide Rosario Alonso, J. Ignacio Andres, M. Teresa Garcia-Lopez, Federico G. De las Heras, Rosario Herranz, Balbino Alarcon, and Luis Carrasco pp 834 - 838; DOI: 10.1021/jm00383a027 |
Book Reviews pp 839 - 840; DOI: 10.1021/jm00383a600 |
A New Generation of Phosphodiesterase Inhibitors: Multiple Molecular Forms of Phosphodiesterase and the Potential for Drug Selectivity Ronald E. Weishaar, Michael H. Cain, and James A. Bristol pp 537 - 545; DOI: 10.1021/jm50001a001 |
Aldosterone Antagonists. 1. Synthesis and Activities of 6β,7β:15β,16β-Dimethylene Steroidal Spirolactones Klaus Nickisch, Dieter Bittler, Jorge Casals-stenzel, Henry Laurent, Robert Nickolson, Yukishige Nishino, Karl Petzoldt, and Rudolf Wiechert pp 546 - 550; DOI: 10.1021/jm50001a002 |
Synthesis and Antiviral Activity of the Carbocyclic Analogues of (E)-5-(2-Halovinyl)-2'-deoxyuridines and (E)-5-(2-Halovinyl)-2'-deoxycytidines Piet Herdewijn, Erik De Clercq, Jan Balzarini, and Hubert Vanderhaeghe pp 550 - 555; DOI: 10.1021/jm50001a003 |
Synthesis and Central Dopaminergic Effects of N-(4,6-Dimethyl-2-pyridinyl)benzamides Saïd Bouhayat, Sylvie Piessard, Guillaume Le Baut, Louis Sparfel, Jean-Yves Petit, François Piriou, and Lucien Welin pp 555 - 559; DOI: 10.1021/jm50001a004 |
Studies on Antianaphylactic Agents. 7. Synthesis of Antiallergic 5-Oxo-5H-[1]benzopyrano[2,3-b]pyridines Akira Nohara, Toshihiro Ishiguro, Kiyoshi Ukawa, Hirosada Sugihara, Yoshitaka Maki, and Yasushi Sanno pp 559 - 568; DOI: 10.1021/jm50001a005 |
Studies on 4(1H)-Quinazolinones. 5. Synthesis and Antiinflammatory Activity of 4(1H)-Quinazolinone Derivatives Ken-ichi Ozaki, Yoshihisa Yamada, Toyonari Oine, Tōru Ishizuka, and Yoshio Iwasawa pp 568 - 576; DOI: 10.1021/jm50001a006 |
Quantitative Structure-Activity Relationships in Cytokinin Agonistic and Antagonistic Pyrido[2,3-d]pyrimidine Derivates: Insights into Receptor Topology Hajime Iwamura, Shigeru Murakami, Koichi Koshimizu, and Satoshi Matsubara pp 577 - 583; DOI: 10.1021/jm50001a007 |
Cyclic Melanotropins. 9. 7-D-Phenylalanine Analogues of the Active-Site Sequence Wayne L. Cody, Mark Mahoney, James J. Knittel, Victor J. Hruby, Ana Maria de L. Castrucci, and Mac E. Hadley pp 583 - 588; DOI: 10.1021/jm50001a008 |
[(Aminomethy)aryloxy]acetic Acid Esters. A New Class of High-Ceiling Diuretics. 4. Substituted 6,7-Dichloro-2,3-dihydrobenzofurans Derived by Ring Annelation Cheuk-Man Lee, James A. Parks, Paul R. Bunnell, Jacob J. Plattner, Michael J. Field, and Gerhard H. Giebisch pp 589 - 594; DOI: 10.1021/jm50001a009 |
Phosphorus-Nitrogen Compounds. 26. Phosphaminimides. 2. 2,2'-Phosphinylidenebis(1,1,1-trimethylhydrazinium) Iodide Inner Salts as Agents Affecting Ganglionic Transmission Lindley A. Cates, Ven-Shun Li, Bashir H. Saddawi, and Karim A. Alkadhi pp 595 - 597; DOI: 10.1021/jm50001a010 |
3-Alkyl-3-hydroxyglutaric Acids: A New Class of Hypocholesterolemic HMG CoA Reductase Inhibitors. 1 John S. Baran, Ivar Laos, Donna D. Langford, James E. Miller, Charlene Jett, Beatrice Taite, and Elaine Rohrbacher pp 597 - 601; DOI: 10.1021/jm50001a011 |
Effect of Structural Modification of the Hydantoin Ring on Anticonvulsant Activity Sergio Cortes, Zeng-Kun Liao, Darrell Watson, and Harold Kohn pp 601 - 606; DOI: 10.1021/jm50001a012 |
1-[3-(Diarylamino)propyl]piperidines and Related Compounds, Potential Antipsychotic Agents with Low Cataleptogenic Profiles Lawrence D. Wise, Ian C. Pattison, Donald E. Butler, Horace A. DeWald, Edward P. Lewis, Sandra J. Lobbestael, Ivan C. Nordin, B. P. H. Poschel, and Linda L. Coughenour pp 606 - 612; DOI: 10.1021/jm50001a013 |
Interactions of Apomorphine with Serum and Tissue Proteins Robert V. Smith, Raja B. Velagapudi, Angus M. McLean, and Richard E. Wilcox pp 613 - 620; DOI: 10.1021/jm50001a014 |
"Reverse" and "Symmetrical" Analogues of Actinomycin D: Matabolic Actication and in Vitro and in Vivo Tumor Growth Inhibitory Activities Sisir K. Sengupta, Christinne Kelly, and Raj K. Sehgal pp 620 - 628; DOI: 10.1021/jm50001a015 |
One-Electron Oxidation of Vindoline and 16-O-Acetylvindoline Catalyzed by Peroxidase F. Sima Sariaslani, M. W. Duffel, and J. P. Rosazza pp 629 - 633; DOI: 10.1021/jm50001a016 |
Conjugates of Catecholamines. 5. Synthesis and β-Adrenergic Activity of N-(Aminoalkyl)norepinephrine Derivatives Allen B. Reitz, Etienne Sonveaux, Roberto P. Rosenkranz, Michael S. Verlander, Kenneth L. Melmon, Brian B. Hoffman, Yasio Akita, Neal Castagnoli, and Murray Goodman pp 634 - 642; DOI: 10.1021/jm50001a017 |
Conjugates of Catecholamines. 6. Synthesis and β-Adrenergic Activity of N - (Hydroxyalkyl)catecholamine Derivatives Allen B. Reitz, Mitchell A. Avery, Roberto P. Rosenkranz, Michael S. Verlander, Kenneth L. Melmon, Brian B. Hoffman, Yasio Akita, Neal Castagnoli, and Murry Goodman pp 642 - 647; DOI: 10.1021/jm50001a018 |
New Antihistaminic Theophylline or Theobromine Derivatives Jean-Claude Pascal, Serge Beranger, Henri Pinhas, Alain Poizot, and Jean-Pierre Désiles pp 647 - 652; DOI: 10.1021/jm50001a019 |
Orally Active and Potent Inhibitors of γ-Aminobutyric Acid Uptake Fadia E. Ali, William E. Bondinell, Penelope A. Dandridge, James S. Frazee, Eleanor Garvey, Gerald R. Girard, Carl Kaiser, Thomas W. Ku, John J. Lafferty, George I. Moonsammy, Hye-Ja Oh, Julia A. Rush, Paulette E. Setler, Orum D. Stringer, Joseph W. Venslavsky, Beth W. Volpe, Libby M. Yunger, and Charles L. Zirkle pp 653 - 660; DOI: 10.1021/jm50001a020 |
Methotrexate Analogues. 25. Chemical and Biological Studies on the γ-tert-Butyl Esters of Methotrexate and Aminopterin Andre Rosowsky, James H. Freisheim, Henry Bader, Ronald A. Forsch, Sandra S. Susten, Carol A. Cucchi, and Emil Frie pp 660 - 667; DOI: 10.1021/jm50001a021 |
Ibotenic Acid Analogues. Synthesis, Molecular Flexibility, and in Vitro Activity of Agonists and Antagonists at Central Glutamic Acid Receptors Jørn Lauridsen, Tage Honoré, and Povl Krogsgaard-Larsen pp 668 - 672; DOI: 10.1021/jm50001a022 |
Synthesis and Structure-Activity Studies on Excitatory Amino Acids Structurally Related to Ibotenic Acid Povl Krogsgaard-Larsen, Lotte Brehm, Jørgen S. Johansen, Peter Vinzents, Jørn Lauridsen, and David R. Curtis pp 673 - 679; DOI: 10.1021/jm50001a023 |
Resolution of 5,6-Dihydroxy-2-(N,N-di -n-propylamino)tetralin in Relation to the Structural and Stereochemical Requirements for Centrally Acting Dopamine Agonists Cor J. Grol, Liesbeth J. Jansen, and Hans Rollema pp 679 - 683; DOI: 10.1021/jm50001a024 |
Synthesis and Interaction of 5-(Substituted-phenyl)-3-methy1-6,7-dihydropyrazolo[4,3-e][1,4]diazepin-8(7H)-ones with Benzodiazepine Receptors in Rat Cerebral Cortex Pier Giovanni Baraldi, Stefano Manfredini, Vittorio Periotto, Daniele Simoni, Mario Guarneri, and Pier Andrea Borea pp 683 - 685; DOI: 10.1021/jm50001a025 |
Azides and Nitrenes. Reactivity and Utility. Edited by Eric F. V. Scriven Feodor Scheinman pp 686 - 686; DOI: 10.1021/jm50001a026 |
Chemistry and Biotechnology of Biologically Active Natural Products. Edited by Cs. Szántay, Á. Gottsegen, and G. Kovács Arnold Brossi pp 686 - 686; DOI: 10.1021/jm50001a027 |
Book Reviews pp 686 - 686; DOI: 10.1021/jm50001a028 |