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Volume 28
Main Index

Issue 7


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
PDF
A computational procedure for determining energetically favorable binding sites on biologically important macromolecules
P. J. Goodford
pp 849 - 857; DOI:
10.1021/jm00145a002
PDF
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
PDF
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
PDF
Tetracyclic pyridazines as potential psychopharmacological agents
Bruce S. Ross and Robert A. Wiley
pp 870 - 875; DOI:
10.1021/jm00145a005
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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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
N-[[(Mercaptoacetyl)amino]benzoyl]glycines mucolytic agents
Tellis A. Martin and William T. Comer
pp 910 - 914; DOI:
10.1021/jm00145a011
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
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Book Reviews

pp 976 - 978; DOI:
10.1021/jm00145a600
PDF

Issue 8


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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
.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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
Decomposition reactions of (hydroxyalkyl)nitrosoureas and related compounds: possible relationship to carcinogenicity
Sandra S. Singer
pp 1088 - 1093; DOI:
10.1021/jm00146a018
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
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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
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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
PDF
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
PDF
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
PDF
Book Reviews

pp 1126 - 1132; DOI:
10.1021/jm00146a600
PDF

Issue 9


Computer-assisted drug design
A. J. Hopfinger
pp 1133 - 1139; DOI:
10.1021/jm00147a001
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
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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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
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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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
Book Reviews

pp 1380 - 1382; DOI:
10.1021/jm00147a600
PDF

Issue 10


N6-Cycloalkyladenosines. Potent, A1-selective adenosine agonists
Walter H. Moos, Deedee S. Szotek, and Robert F. Bruns
pp 1383 - 1384; DOI:
10.1021/jm00148a001
PDF
Resolution of aristeromycin enantiomers
Piet Herdewijn, Jan Balzarini, Erik De Clercq, and Hubert Vanderhaeghe
pp 1385 - 1386; DOI:
10.1021/jm00148a002
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
Synthesis and hypoglycemic activity of N-alkylated hydrazonopropionic acids
Hans Peter Wolff and Hans F. Kuehnle
pp 1436 - 1440; DOI:
10.1021/jm00148a011
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
(.+-.)-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
PDF
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
PDF
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
PDF
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
PDF
Structural studies on some tamoxifen derivatives
Reiko Kuroda, Shirley Cutbush, Stephen Neidle, and On Tai Lueng
pp 1497 - 1503; DOI:
10.1021/jm00148a021
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
Book Reviews

pp 1547 - 1552; DOI:
10.1021/jm00148a600
PDF

Issue 11


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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
.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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
Alkylating .beta.-blockers: activity of isomeric bromoacetyl alprenolol menthanes
Andras Liptak, John W. Kusiak, and Josef Pitha
pp 1699 - 1703; DOI:
10.1021/jm00149a028
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
Book Reviews

pp 1753 - 1754; DOI:
10.1021/jm00149a600
PDF

Issue 12


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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
[[(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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
Additions and Corrections - Resolution of Aristeromycin Enantiomers.
Piet Herdewijn, Jan Balzarini, Erik De Clercq, and Hubert Vanderhaeghe
pp 1965 - 1965; DOI:
10.1021/jm00150a606
PDF
Book Reviews

pp 1966 - 1968; DOI:
10.1021/jm00150a607
PDF

Issue 1


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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
[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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
Drug glycosides: potential prodrugs for colon-specific drug delivery
David R. Friend and George W. Chang
pp 51 - 57; DOI:
10.1021/jm00379a012
PDF
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
PDF
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
PDF
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
PDF
[(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
PDF
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
PDF
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
PDF
.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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
Substrate specificity of pyroglutamylaminopeptidase
John T. Capecchi and Gordon Marc Loudon
pp 140 - 143; DOI:
10.1021/jm00379a024
PDF
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
PDF
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
PDF
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
PDF

Issue 2


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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF

Issue 3


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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
[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
PDF
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
PDF
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
PDF
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
PDF

Issue 4


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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
Conformational factors in cardiac glycoside activity
Francis C. K. Chiu and Thomas R. Watson
pp 509 - 515; DOI:
10.1021/jm00382a023
PDF
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
PDF
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
PDF
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
PDF
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
PDF
Book Reviews

pp 527 - 536; DOI:
10.1021/jm00382a600
PDF

Issue 6


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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
Synthesis and antimicrobial evaluation of bicyclomycin analogs
Robert M. Williams, Robert W. Armstrong, and Jen Sen Dung
pp 733 - 740; DOI:
10.1021/jm00383a008
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
N-Phenylpiperazine derivatives with hypocholesterolemic activity
Giuseppe Cascio, Elso Manghisi, Roberto Porta, and Giancarlo Fregnan
pp 815 - 818; DOI:
10.1021/jm00383a021
PDF
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
PDF
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
PDF
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
PDF
S-(Nitrocarbobenzoxy)glutathiones: potent competitive inhibitors of mammalian glyoxalase II
P. E. Bush and S. J. Norton
pp 828 - 830; DOI:
10.1021/jm00383a025
PDF
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
PDF
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
PDF
Book Reviews

pp 839 - 840; DOI:
10.1021/jm00383a600
PDF

Issue 5


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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
[(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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
"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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
PDF
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
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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
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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
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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
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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
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Azides and Nitrenes. Reactivity and Utility. Edited by Eric F. V. Scriven
Feodor Scheinman
pp 686 - 686; DOI:
10.1021/jm50001a026
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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
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Book Reviews

pp 686 - 686; DOI:
10.1021/jm50001a028
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