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Volume 30
Main Index

Issue 1


Central serotonin receptors as targets for drug research
Richard A. Glennon
pp 1 - 12; DOI:
10.1021/jm00384a001
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1-2-(Pyridinyl)piperazine derivatives with antianaphylactic, antibronchospastic and mast cell stabilizing activities
Alberto Catto, Gianni Motta, Alberto Tajana, Pietro Cazzulani, Dante Nardi, and Amedeo Leonardi
pp 13 - 19; DOI:
10.1021/jm00384a002
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Synthesis and biological properties of side-chain-modified bleomycins
Wilhelmus J. Vloon, Cornelis Kruk, Upendra K. Pandit, Hendricus P. Hofs, and John G. McVie
pp 20 - 24; DOI:
10.1021/jm00384a003
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Synthesis and antisecretory and antiulcer activities of derivatives and analogs of 2-(2-pyridyl)tetrahydrothiophene-2-carbothioamide
Jean-Claude Aloup, Jean Bouchaudon, Daniel Farge, Claude James, Jean Deregnaucourt, and Monique Hardy-Houis
pp 24 - 29; DOI:
10.1021/jm00384a004
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Phenylpiperazine-based radiopharmaceuticals for brain imaging. 3. Synthesis and evaluation of radioiodinated 1-alkyl-4-phenylpiperazines
Robert N. Hanson and Mohammad Hassan
pp 29 - 34; DOI:
10.1021/jm00384a005
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Dopamine agonists related to 3-allyl-6-chloro-2,3,4,5-tetrahydro-1-(4-hydroxyphenyl)-1H-3-benzazepine-7,8-diol, 6-position modifications
Stephen T. Ross, Robert G. Franz, Gregory Gallagher, Martin Brenner, James W. Wilson, Robert M. DeMarinis, J. Paul Hieble, and Henry M. Sarau
pp 35 - 40; DOI:
10.1021/jm00384a006
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Synthetic analogs of tetrahydrobiopterin with cofactor activity for aromatic amino acid hydroxylases
E. C. Bigham, G. K. Smith, J. F. Reinhard, W. R. Mallory, C. A. Nichol, and R. W. Morrison
pp 40 - 45; DOI:
10.1021/jm00384a007
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Cluster significance analysis contrasted with three other quantitative structure-activity relationship methods
James W. McFarland and Daniel J. Gans
pp 46 - 49; DOI:
10.1021/jm00384a008
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2,4-Diamino-6,7-dimethoxyquinazolines. 1. 2-[4-(1,4-Benzodioxan-2-ylcarbonyl)piperazin-1-yl] derivatives as .alpha.1-adrenoceptor antagonists and antihypertensive agents
Simon F. Campbell, Michael J. Davey, J. David Hardstone, Brian N. Lewis, and Michael J. Palmer
pp 49 - 57; DOI:
10.1021/jm00384a009
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Antiradiation compounds. 20. 1-Methylquinolinium(and pyridinium)-2-dithioacetic acid derivatives
William O. Foye, Robert W. Jones, Pallab K. Ghoshal, and Bijan Almassian
pp 57 - 62; DOI:
10.1021/jm00384a010
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Synthesis and antilipolytic activities of quinolyl carbanilates and related analogs
John H. Musser, Utpal Chakraborty, Kevin Bailey, Stan Sciortino, Carol Whyzmuzis, Dilip Amin, and Charles A. Sutherland
pp 62 - 67; DOI:
10.1021/jm00384a011
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(5Z)-7-(2,2-Dimethyl-4-phenyl-1,3-dioxan-cis-5-yl)heptenoic acid: a specific thromboxane A2 receptor antagonist
Andrew G. Brewster, Peter W. R. Caulkett, and Reg Jessup
pp 67 - 70; DOI:
10.1021/jm00384a012
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Analogs of the cytostatic and antimitogenic agents chlamydocin and HC-toxin: synthesis and biological activity of chloromethyl ketone and diazomethyl ketone-functionalized cyclic tetrapeptides
Richard E. Shute, Brian Dunlap, and Daniel H. Rich
pp 71 - 78; DOI:
10.1021/jm00384a013
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Polychlorinated biphenyls and related compound interactions with specific binding sites for thyroxine in rat liver nuclear extracts
J. McKinney, R Fannin, S. Jordan, K. Chae, U. Rickenbacher, and L. Pedersen
pp 79 - 86; DOI:
10.1021/jm00384a014
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5-Fluoro- and 8-fluorotrimetoquinol: selective .beta.2-adrenoceptor agonists
Michael T. Clark, Adeboye Adejare, Gamal Shams, Dennis R. Feller, and Duane D. Miller
pp 86 - 90; DOI:
10.1021/jm00384a015
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Synthesis and structure-activity relationships of pyrazolo[4,3-d]pyrimidin-7-ones as adenosine receptor antagonists
Harriet W. Hamilton, Daniel F. Ortwine, Donald F. Worth, and James A. Bristol
pp 91 - 96; DOI:
10.1021/jm00384a016
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Substituted arylmethyl phenyl ethers. 1. A novel series of 5-lipoxygenase inhibitors and leukotriene antagonists
John H. Musser, Utpal R. Chakraborty, Stanley Sciortino, Robert J. Gordon, Atul Khandwala, Edward S. Neiss, Thaddeus P. Pruss, Richard Van Inwegen, Ira Weinryb, and Stephen M. Coutts
pp 96 - 104; DOI:
10.1021/jm00384a017
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Synthesis of N-(3,6-dihydro-1(2H)-pyridinyl)benzamides with hyperglycemic-hypoglycemic activity
Jupita M. Yeung and Edward E. Knaus
pp 104 - 108; DOI:
10.1021/jm00384a018
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Synthesis, cell-growth inhibition, and antitumor screening of 2-(p-n-butylanilino)purines and their nucleoside analogs
George E. Wright, Lech W. Dudycz, Zygmunt Kazimierczuk, Neal C. Brown, and Naseema N. Khan
pp 109 - 116; DOI:
10.1021/jm00384a019
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Synthesis and antitumor activity of tropolone derivatives. 4
Masatoshi Yamato, Kuniko Hashigaki, Junko Sakai, Youko Kawasaki, Shigeru Tsukagoshi, and Tazuko Tashiro
pp 117 - 120; DOI:
10.1021/jm00384a020
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Anthrapyrazole anticancer agents. Synthesis and structure-activity relationships against murine leukemias
H. D. Hollis Showalter, Judith L. Johnson, Jeanne M. Hoftiezer, William R. Turner, Leslie M. Werbel, Wilbur R. Leopold, Joan L. Shillis, Robert C. Jackson, and Edward F. Elslager
pp 121 - 131; DOI:
10.1021/jm00384a021
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2-Phenylindoles. Effect of N-benzylation on estrogen receptor affinity, estrogenic properties, and mammary tumor inhibiting activity
Erwin Von Angerer and Josef Strohmeier
pp 131 - 136; DOI:
10.1021/jm00384a022
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Structure-activity relationships of kadsurenone analogues
Mitree M. Ponpipom, Robert L. Bugianesi, David R. Brooker, Bao-zhen Yue, San-bao Hwang, and Tsung-ying Shen
pp 136 - 142; DOI:
10.1021/jm00384a023
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Indolizidine and quinolizidine derivatives of the dopamine autoreceptor agonist 3-(3-hydroxyphenyl)-N-n-propylpiperidine (3-PPP)
Klaus P. Boegesoe, Joern Arnt, Max Lundmark, and Staffan Sundell
pp 142 - 150; DOI:
10.1021/jm00384a024
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Structural alterations that differentially affect the mutagenic and antitrichomonal activities of 5-nitroimidazoles
John S. Walsh, Regina Wang, Edward Bagan, C. C. Wang, Peter Wislocki, and Gerald T. Miwa
pp 150 - 156; DOI:
10.1021/jm00384a025
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Preparation, receptor binding, and fluorescence properties of hexestrol-fluorophore conjugates: evaluation of site of attachment, fluorophore structure, and fluorophore-ligand spacing
Thomas L. Fevig, John E. Lloyd, Jeffery A. Zablocki, and John A. Katzenellenbogen
pp 156 - 165; DOI:
10.1021/jm00384a026
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Double-headed haptens with pyrocatechol (poison ivy-like) and methylene lactone functional groups: a search for skin-tolerance inducers
Henri Mattes and Claude Benezra
pp 165 - 168; DOI:
10.1021/jm00384a027
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Preparation and antitumor activity of new mitomycin A analogs
Salah M. Sami, Bhashyam S. Iyengar, William A. Remers, and William T. Bradner
pp 168 - 173; DOI:
10.1021/jm00384a028
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Substituted (aryloxy)alkanoic acids as antagonists of slow-reacting substance of anaphylaxis
Ronald A. LeMahieu, Mathew Carson, Ru-Jen Han, William C. Nason, Margaret O'Donnell, Deborah L. Brown, Herman J. Crowley, and Ann F. Welton
pp 173 - 178; DOI:
10.1021/jm00384a029
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Conformationally defined adrenergic agents. 4. 1-(Aminomethyl)phthalans: synthesis and pharmacological consequences of the phthalan ring oxygen atom
John F. DeBernardis, David L. Arendsen, John J. Kyncl, and Daniel J. Kerkman
pp 178 - 184; DOI:
10.1021/jm00384a030
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N-(heterocyclic alkyl)pyrido[2,1-b]quinazoline-8-carboxamides as orally active antiallergy agents
Jefferson W. Tilley, Paul Levitan, Joan Lind, Ann F. Welton, Herman J. Crowley, Lawrence D. Tobias, and Margaret O'Donnell
pp 185 - 193; DOI:
10.1021/jm00384a031
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Synthesis and gastrointestinal pharmacology of a 3E,5Z diene analog of misoprostol
Paul W. Collins, Steven W. Kramer, Alan F. Gasiecki, Richard M. Weier, Peter H. Jones, Gary W. Gullikson, Robert G. Bianchi, and Raymond F. Bauer
pp 193 - 197; DOI:
10.1021/jm00384a032
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Synthesis and biological evaluation of acyclic neplanocin analogs
Mei Hua, Phillip M. Korkowski, and Robert Vince
pp 198 - 200; DOI:
10.1021/jm00384a033
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Differential blockade of muscarinic receptor subtypes by polymethylene tetraamines. Novel class of selective antagonists of cardiac M-2 muscarinic receptors
Carlo Melchiorre, Anna Cassinelli, and Wilma Quaglia
pp 201 - 204; DOI:
10.1021/jm00384a034
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Substituted 2-(2-hydroxyphenyl)benzimidazoles as potential agents for the control of periodontal diseases
Robert A. Coburn, Michael T. Clark, Richard T. Evans, and Robert J. Genco
pp 205 - 208; DOI:
10.1021/jm00384a035
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Studies on the active molecular species of the H2-receptor antagonists cimetidine and mifentidine
E. E. J. Haaksma, B. Rademaker, K. Kramer, J. C. Eriks, A. Bast, and H. Timmerman
pp 208 - 211; DOI:
10.1021/jm00384a036
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Xanthine functionalized congeners as potent ligands at A2-adenosine receptors
Kenneth A. Jacobson, Dieter Ukena, William Padgett, John W. Daly, and Kenneth L. Kirk
pp 211 - 214; DOI:
10.1021/jm00384a037
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Dopamine agonists: effects of charged and uncharged analogs of dopamine
Yu-An Chang, Jeffrey Ares, Karen Anderson, Brian Sabol, Raye Ann Wallace, Tahira Farooqui, Norman Uretsky, and Duane D. Miller
pp 214 - 218; DOI:
10.1021/jm00384a038
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Differential effects of N-terminal modifications on the biological potencies of growth hormone releasing factor analogs with varying chain lengths
David H. Coy, William A. Murphy, Valentine A. Lance, and Mark L. Heiman
pp 219 - 222; DOI:
10.1021/jm00384a039
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3-[(2-Ethoxyphenoxy)methyl]piperidine derivatives. Synthesis and antidepressant activity
A. Balsamo, I. Giorgi, A. Lapucci, A. Lucacchini, B. Macchia, F. Macchia, C. Martini, and A. Rossi
pp 222 - 225; DOI:
10.1021/jm00384a040
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Nucleosides. 139. Synthesis and anticytomegalovirus and antiherpes simplex virus activity of 5'-modified analogs of 2'-fluoroarabinosylpyrimidine nucleosides
Kazuho Harada, Jasenka Matulic-Adamic, Richard W. Price, Raymond F. Schinazi, Kyoichi A. Watanabe, and Jack J. Fox
pp 226 - 229; DOI:
10.1021/jm00384a041
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Book Reviews

pp 230 - 230; DOI:
10.1021/jm00384a600
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Issue 2


In search of the digitalis replacement
Paul W. Erhardt
pp 231 - 237; DOI:
10.1021/jm00385a001
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Bimorphinans as highly selective, potent .kappa. opioid receptor antagonists
P. S. Portoghese, A. W. Lipkowski, and A. E. Takemori
pp 238 - 239; DOI:
10.1021/jm00385a002
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Synthesis and structure-activity relationships of a series of aminopyridazine derivatives of .gamma.-aminobutyric acid acting as selective GABA-A antagonists
Camille Georges Wermuth, Jean Jacques Bourguignon, Gilbert Schlewer, Jean Pierre Gies, Angele Schoenfelder, Anita Melikian, Marie Jeanne Bouchet, Dominique Chantreux, Jean Charles Molimard, and et al.
pp 239 - 249; DOI:
10.1021/jm00385a003
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Stereochemical studies on the cytochrome P-450 catalyzed oxidation of (S)-nicotine to the (S)-nicotine .DELTA.1'(5')-iminium species
Lisa A. Peterson, Anthony Trevor, and Neal Castagnoli
pp 249 - 254; DOI:
10.1021/jm00385a004
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Structural requirements for the inhibition of 5-lipoxygenase by 15-hydroxyeicosa-5,8,11,13-tetraenoic acid analogs
Fortuna Haviv, James D. Ratajczyk, Robert W. DeNet, Yvonne C. Martin, Richard D. Dyer, and George W. Carter
pp 254 - 263; DOI:
10.1021/jm00385a005
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1-[[[5-(Substituted phenyl)-2-oxazolyl]methylene]amino]-2,4-imidazolidinediones, a new class of skeletal muscle relaxants
R. L. White, F. L. Wessels, T. J. Schwan, and K. O. Ellis
pp 263 - 266; DOI:
10.1021/jm00385a006
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Synthesis and evaluation of mono-, di-, and trifluoroethenyl-GABA derivatives as GABA-T inhibitors
Michael Kolb, Jacqueline Barth, Jean Georges Heydt, and Michel J. Jung
pp 267 - 272; DOI:
10.1021/jm00385a007
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Molecular modification of anticholinergics as probes for muscarinic receptors. 1. Amino esters of .alpha.-substituted phenylacetic acid and related analogs
Matthias C. Lu, Walley E. Wung, Lisa B. Shih, Soledad Callejas, James E. Gearien, and Emmanuel B. Thompson
pp 273 - 278; DOI:
10.1021/jm00385a008
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Molecular modification of anticholinergics as probes for muscarinic receptors. 3. Conformationally restricted analogs of benactyzine
Michael T. Flavin, Matthias C. Lu, Emmanual B. Thompson, and Hemendra N. Bhargava
pp 278 - 285; DOI:
10.1021/jm00385a009
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Inhibition of aspartic proteinases by peptides containing lysine and ornithine side-chain analogs of statine
Francesco G. Salituro, Nirankar Agarwal, Theo Hofmann, and Daniel H. Rich
pp 286 - 295; DOI:
10.1021/jm00385a010
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Inhibitors of cyclic AMP phosphodiesterase. 1. Analogs of cilostamide and anagrelide
Gordon H. Jones, Michael C. Venuti, Robert Alvarez, John J. Bruno, Andrew H. Berks, and Anthony Prince
pp 295 - 303; DOI:
10.1021/jm00385a011
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Inhibitors of cyclic AMP phosphodiesterase. 2. Structural variations of N-cyclohexyl-N-methyl-4-[(1,2,3,5-tetrahydro-2-oxoimidazo[2,1-b]quinazolin-7-yl)oxy]butyramide (RS-82856)
Michael C. Venuti, Gordon H. Jones, Robert Alvarez, and John J. Bruno
pp 303 - 318; DOI:
10.1021/jm00385a012
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1-Aryl-2-(aminomethyl)cyclopropanecarboxylic acid derivatives. A new series of potential antidepressants
Bernard Bonnaud, Henri Cousse, Gilbert Mouzin, Mike Briley, Antoine Stenger, Francois Fauran, and Jean Pierre Couzinier
pp 318 - 325; DOI:
10.1021/jm00385a013
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Structure-activity relationships of sparsomycin and its analogs. Inhibition of peptide bond formation in cell-free systems and of L1210 and bacterial cell growth
Leon A. G. M. Van den Broek, Rob M. J. Liskamp, J. Hans Colstee, Peter Lelieveld, Miguel Remacha, David Vazquez, Juan P. G. Ballesta, and Harry C. J. Ottenheijm
pp 325 - 333; DOI:
10.1021/jm00385a014
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Comparison of aminoglycoside antibiotics with respect to uptake and lethal activity in Escherichia coli
Norris E. Allen, William E. Alborn, Herbert A. Kirst, and John E. Toth
pp 333 - 340; DOI:
10.1021/jm00385a015
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Synthesis and antitumor activity of fluorine-substituted 4-amino-2(1H)-pyridinones and their nucleosides. 3-Deazacytosines
Dennis J. McNamara and P. Dan Cook
pp 340 - 347; DOI:
10.1021/jm00385a016
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2,4-Diamino-5-benzylpyrimidines as antibacterial agents. 7. Analysis of the effect of 3,5-dialkyl substituent size and shape on binding to four different dihydrofolate reductase enzymes
Barbara Roth, Barbara S. Rauckman, Robert Ferone, David P. Baccanari, John N. Champness, and Richard M. Hyde
pp 348 - 356; DOI:
10.1021/jm00385a017
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Antitumor imidazotetrazines. 14. Synthesis and antitumor activity of 6- and 8-substituted imidazo[5,1-d]-1,2,3,5-tetrazinones and 8-substituted pyrazolo[5,1-d]-1,2,3,5-tetrazinones
Edward Lunt, Christopher G. Newton, Christopher Smith, Graham P. Stevens, Malcolm F. G. Stevens, Colin G. Straw, Roger J. A. Walsh, Peter J. Warren, Christian Fizames, and et al.
pp 357 - 366; DOI:
10.1021/jm00385a018
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NMR spectroscopic studies of intermediary metabolites of cyclophosphamide. 2. Direct observation, characterization, and reactivity studies of iminocyclophosphamide and related species
Victoria L. Boyd, Michael F. Summers, Susan Marie Ludeman, William Egan, Gerald Zon, and Judith B. Regan
pp 366 - 374; DOI:
10.1021/jm00385a019
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Synthetic and enzyme inhibition studies of pepstatin analogs containing hydroxyethylene and ketomethylene dipeptide isosteres
Mark W. Holladay, Francesco G. Salituro, and Daniel H. Rich
pp 374 - 383; DOI:
10.1021/jm00385a020
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Structure-activity studies of 5-[[4-(4,5-dihydro-2-oxazolyl)phenoxy]alkyl]-3-methylisoxazoles: inhibitors of picornavirus uncoating
Guy D. Diana, Richard C. Oglesby, Vahan Akullian, Philip M. Carabateas, David Cutcliffe, John P. Mallamo, Michael J. Otto, Mark A. McKinlay, Edward G. Maliski, and Stephen J. Michalec
pp 383 - 388; DOI:
10.1021/jm00385a021
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Octahydropyrazino[2',3':3,4]pyrido[1,2-a]indoles. A new class of potent antihypertensive agents
Ivo Jirkovsky, George Santroch, Reinhardt Baudy, and George Oshiro
pp 388 - 394; DOI:
10.1021/jm00385a022
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Activation mechanisms of mafosfamide and the role of thiols in cyclophosphamide metabolism
Chul Hoon Kwon, Richard F. Borch, Jurgen Engel, and Ulf Niemeyer
pp 395 - 399; DOI:
10.1021/jm00385a023
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Leukotriene D4 antagonists and 5-lipoxygenase inhibitors. Synthesis of benzoheterocyclic [(methoxyphenyl)amino]oxoalkanoic acid esters
John H. Musser, Dennis M. Kubrak, Joseph Chang, Stephen M. DiZio, Mark Hite, James M. Hand, and Alan J. Lewis
pp 400 - 405; DOI:
10.1021/jm00385a024
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Chemical differentiating agents. Differentiation of HL-60 cells by hexamethylenebis[acetamide]analogs
Alberto Haces, Theodore R. Breitman, and John S. Driscoll
pp 405 - 409; DOI:
10.1021/jm00385a025
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5-Quinone derivatives of 2'-deoxyuridine 5'-phosphate: inhibition and inactivation of thymidylate synthase, antitumor cell, and antiviral studies
Laman A. Al-Razzak, Douglas Schwepler, Charles J. Decedue, Jan Balzarini, Erik De Clercq, and Mathias P. Mertes
pp 409 - 419; DOI:
10.1021/jm00385a026
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The influence of physicochemical parameters on the biliary excretion of a series of nitroimidazoles
Gian Luigi Biagi, Giorgio Cantelli-Forti, Anna Maria Barbaro, Maria Clelia Guerra, Patrizia Hrelia, and Pier Andrea Borea
pp 420 - 423; DOI:
10.1021/jm00385a027
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Molecular modification of anticholinergics as probes for muscarinic receptors. 2. Amino esters of .alpha.-methyltropic acid
Matthias C. Lu, Lisa B. Shih, Hwan S. Jae, James E. Gearien, and Emmanual B. Thompson
pp 424 - 427; DOI:
10.1021/jm00385a028
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The mechanism of activation of 4-hydroxycyclophosphamide
Richard F. Borch and Jo Ann Millard
pp 427 - 431; DOI:
10.1021/jm00385a029
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5-Amino-4-(diazoacetyl)-1-.beta.-D-ribofuranosylimidazole, a new antileukemic agent
H. Jeanette Thomas, Lisa N. Avery, R. Wallace Brockman, and John A. Montgomery
pp 431 - 434; DOI:
10.1021/jm00385a030
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Prostaglandin-H synthase inhibition by malonamides. Ring-opened analogs of phenylbutazone
Jonathan L. Vennerstrom and Thomas J. Holmes
pp 434 - 437; DOI:
10.1021/jm00385a031
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Synthesis and biological properties of 9-(trans-4-hydroxy-2-buten-1-yl)adenine and guanine: open-chain analogs of neplanocin A
Shashikant Phadtare and Jiri Zemlicka
pp 437 - 440; DOI:
10.1021/jm00385a032
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Synthesis and antiviral activity of various 3'-azido, 3'-amino, 2',3'-unsaturated, and 2',3'-dideoxy analogs of pyrimidine deoxyribonucleosides against retroviruses
Tai Shun Lin, Ming S. Chen, Colin McLaren, You Song Gao, Ismail Ghazzouli, and William H. Prusoff
pp 440 - 444; DOI:
10.1021/jm00385a033
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Synthetic bovine prothrombin precursor 13-29 for studies of vitamin K dependent carboxylase
Richard S. Pottorf, Daniel H. Rich, Jean Engelke, and John W. Suttie
pp 445 - 448; DOI:
10.1021/jm00385a034
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Book Reviews
Lemont B. Kier, and Lowell H. Hall
pp 448 - 450; DOI:
10.1021/jm00385a600
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Issue 3


Esters of N,N-disubstituted 2-hydroxyacetamides as a novel highly biolabile prodrug type for carboxylic acid agents
Hans Bundgaard and Niels Mork Nielsen
pp 451 - 454; DOI:
10.1021/jm00386a001
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A new thienylpyrazoloquinoline: a potent and orally active inverse agonist to benzodiazepine receptors
Susumu Takada, Hiroshisa Shindo, Takashi Sasatani, Akira Matsushita, Masami Eigyo, Kazuo Kawasaki, and Shunji Murata
pp 454 - 455; DOI:
10.1021/jm00386a002
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Synthesis of 7,12-dihydropyrido[3,4-b:5,4-b']diindoles. A novel class of rigid, planar benzodiazepine receptor ligands
Mark L. Trudell, Anthony S. Basile, Harlan E. Shannon, Phil Skolnick, and James M. Cook
pp 456 - 458; DOI:
10.1021/jm00386a003
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Quantitative structure-activity analysis in dihydropteroate synthase inhibition of sulfones. Comparison with sulfanilamides
Pier G. De Benedetti, Dario Iarossi, Cristina Menziani, Valeria Caiolfa, Chiara Frassineti, and Carlo Cennamo
pp 459 - 464; DOI:
10.1021/jm00386a004
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Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3 dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids
Violetta Cecchetti, Arnaldo Fravolini, Renata Fringuelli, Giuseppe Mascellani, Piergiuseppe Pagella, Maurizio Palmioli, Giorgio Segre, and Patrizia Terni
pp 465 - 473; DOI:
10.1021/jm00386a005
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Redox chemistry of the 9-anilinoacridine class of antitumor agents
Jeffrey L. Jurlina, Andrew Lindsay, John E. Packer, Bruce C. Baguley, and William A. Denny
pp 473 - 480; DOI:
10.1021/jm00386a006
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Nucleic acid related compounds. 51. Synthesis and biological properties of sugar-modified analogs of the nucleoside antibiotics tubercidin, toyocamycin, sangivamycin, and formycin
Erik De Clercq, Jan Balzarini, Danuta Madej, Fritz Hansske, and Morris J. Robins
pp 481 - 486; DOI:
10.1021/jm00386a007
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Multisubstrate inhibitors of dopamine .beta.-hydroxylase. 2. Structure-activity relationships at the phenethylamine binding site
Lawrence I. Kruse, Carl Kaiser, Walter E. DeWolf Jr., James S. Frazee, Stephen T. Ross, Joyce Wawro, Merrie Wise, Kathryn E. Flaim, John L. Sawyer, and et al.
pp 486 - 494; DOI:
10.1021/jm00386a008
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Dopamine autoreceptor agonists: resolution and pharmacological activity of 2,6-diaminotetrahydrobenzothiazole and an aminothiazole analog of apomorphine
Claus S. Schneider and Joachim Mierau
pp 494 - 498; DOI:
10.1021/jm00386a009
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Amnesia-reversal activity of a series of cyclic imides
Donald E. Butler, James D. Leonard, Bradley W. Caprathe, Yvon J. L'Italien, Michael R. Pavia, Fred M. Hershenson, Paul H. Poschel, and John G. Marriott
pp 498 - 503; DOI:
10.1021/jm00386a010
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Synthesis and structure-activity relationship of 1-aryl-6,8-difluoroquinolone antibacterial agents
Daniel T. W. Chu, Prabhavathi B. Fernandes, Robert E. Maleczka, Carl W. Nordeen, and Andre G. Pernet
pp 504 - 509; DOI:
10.1021/jm00386a011
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Synthesis, biological evaluation, and quantitative structure-activity relationship analysis of 2-hydroxy-1H-isoindolediones as new cytostatic agents
Carcy L. Chan, Eric J. Lien, and Zoltan A. Tokes
pp 509 - 514; DOI:
10.1021/jm00386a012
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Synthesis and 3'-substituent effects of some 7.alpha.-methoxy-1-oxacephems on antibacterial activity and alkaline hydrolysis rates
Masayuki Narisada, Junko Nishikawa, Fumihiko Watanabe, and Yoshihiro Terui
pp 514 - 522; DOI:
10.1021/jm00386a013
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Proton NMR study of degradation mechanisms of oxacephem derivatives with various 3'-substituents in alkaline solution
Junko Nishikawa, Fumihiko Watanabe, Masayoshi Shudou, Yoshihiro Terui, and Masayuki Narisada
pp 523 - 527; DOI:
10.1021/jm00386a014
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Heteroatom-activated .beta.-lactam antibiotics: considerations of differences in the biological activity of [[3(S)-(acylamino)-2-oxo-1-azetidinyl]oxy]acetic acids (oxamazins) and the corresponding sulfur analogs (thiamazins)
Donald B. Boyd, Charles Eigenbrot, Joseph M. Indelicato, Marvin J. Miller, Carol E. Pasini, and Steven R. Woulfe
pp 528 - 536; DOI:
10.1021/jm00386a015
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.alpha.-Methylproline-containing renin inhibitory peptides: in vivo evaluation in an anesthetized, ganglion-blocked, hog renin infused rat model
Suvit Thaisrivongs, Donald T. Pals, Judy A. Lawson, Steve R. Turner, and Douglas W. Harris
pp 536 - 541; DOI:
10.1021/jm00386a016
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Selective cytotoxicity of a system L specific amino acid nitrogen mustard
David R. Haines, Richard W. Fuller, Shakeel Ahmad, David T. Vistica, and Victor E. Marquez
pp 542 - 547; DOI:
10.1021/jm00386a017
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2-[(3-Pyridinylmethyl)thio]pyrimidine derivatives: New bronchosecretolytic agents
Helmut Schickaneder, Heidrun Engler, and Istvan Szelenyi
pp 547 - 551; DOI:
10.1021/jm00386a018
PDF
Synthesis and quantitative structure-activity relationship analysis of N-triiodoallyl- and N-iodopropargylazoles. New antifungal agents
Masao Koyama, Noriko Ohtani, Fumio Kai, Ikuo Moriguchi, and Shigeharu Inouye
pp 552 - 562; DOI:
10.1021/jm00386a019
PDF
Preparation and evaluation of electrophilic derivatives of phenylbutazone as inhibitors of prostaglandin-H-synthase
Jonathan L. Vennerstrom and Thomas J. Holmes
pp 563 - 567; DOI:
10.1021/jm00386a020
PDF
Functionalized DL-amino acid derivatives. Potent new agents for the treatment of epilepsy
Judith D. Conley and Harold Kohn
pp 567 - 574; DOI:
10.1021/jm00386a021
PDF
Hydroxamic acid inhibitors of 5-lipoxygenase
James B. Summers, Hormoz Mazdiyasni, James H. Holms, James D. Ratajczyk, Richard D. Dyer, and George W. Carter
pp 574 - 580; DOI:
10.1021/jm00386a022
PDF
Synthesis of D-oxa tricyclic partial ergolines as dopamine agonists
Richard N. Booher, Edmund C. Kornfeld, E. Barry Smalstig, and James A. Clemens
pp 580 - 583; DOI:
10.1021/jm00386a023
PDF
Synthesis and antitumor activity of N-terminal proline-containing peptide-(chloroethyl)nitrosoureas
Helga Suli-Vargha, Andras Jeney, Karoly Lapis, and Kalman Medzihradszky
pp 583 - 586; DOI:
10.1021/jm00386a024
PDF
Antitumor agents. 86. Synthesis and cytotoxicity of .alpha.-methylene-.gamma.-lactone-bearing purines
Kuo-Hsiung Lee, Gregory K. Rice, Iris H. Hall, and Venkataraman Amarnath
pp 586 - 588; DOI:
10.1021/jm00386a025
PDF

Issue 4


Design of alternate substrate inhibitors of serine proteases. Synergistic use of alkyl substitution to impede enzyme-catalyzed deacylation
Allen Krantz, Robin W. Spencer, Tim F. Tam, Everton Thomas, and Leslie J. Copp
pp 589 - 591; DOI:
10.1021/jm00387a001
PDF
Thienothiopyran-2-sulfonamides: a novel class of water-soluble carbonic anhydrase inhibitors
Gerald S. Ponticello, Mark B. Freedman, Charles N. Habecker, Paulette A. Lyle, Harvey Schwam, Sandor L. Varga, Marcia E. Christy, William C. Randall, and John J. Baldwin
pp 591 - 597; DOI:
10.1021/jm00387a002
PDF
Linear free energy relationships and cytotoxicities of para-substituted 2-haloethyl aryl selenides and bis(2-chloroethyl) selenides
Sang Ihn Kagn and Colin Paul Spears
pp 597 - 602; DOI:
10.1021/jm00387a003
PDF
Resolved cis- and trans-2-amino-5-methoxy-1-methyltetralins: central dopamine receptor agonists and antagonists
Anette M. Johansson, Lars Erik Arvidsson, Uli Hacksell, J. Lars G. Nilsson, Kjell Svensson, and Arvid Carlsson
pp 602 - 611; DOI:
10.1021/jm00387a004
PDF
Affinity labels for .beta.-adrenoceptors: preparation and properties of alkylating .beta.-blockers derived from indole
Josef Pitha, Wieslaw Buchowiecki, Jan Milecki, and John W. Kusiak
pp 612 - 615; DOI:
10.1021/jm00387a005
PDF
Role of the (acyloxy)methyl moiety in eliciting the adrenergic .beta.-blocking activity of 3-(acyloxy)propanolamines
B. Macchia, A. Balsamo, A. Lapucci, F. Macchia, A. Martinelli, H. L. Ammon, S. M. Prasad, M. C. Breschi, M. Ducci, and E. Martinotti
pp 616 - 622; DOI:
10.1021/jm00387a006
PDF
Molecular structure of the dihydropyridazinone cardiotonic 1,3-dihydro-3,3-dimethyl-5-(1,4,5,6-tetrahydro-6-oxo-3-pyridazinyl)-2H-indol-2-one, a potent inhibitor of cyclic AMP phosphodiesterase
David W. Robertson, Noel D. Jones, Joseph H. Krushinski, G. Don Pollock, John K. Swartzendruber, and J. Scott Hayes
pp 623 - 627; DOI:
10.1021/jm00387a007
PDF
Substituted 1,2,3,4-tetrahydroaminonaphthols: antihypertensive agents, calcium channel blockers, and adrenergic receptor blockers with catecholamine-depleting effects
Karnail S. Atwal, Brian C. O'Reilly, Eric P. Ruby, Chester F. Turk, Gunnar Aberg, Magdi M. Asaad, James L. Bergey, Suzanne Moreland, and James R. Powell
pp 627 - 635; DOI:
10.1021/jm00387a008
PDF
Synthesis and biological activity of novel calcium channel blockers: 2,5-dihydro-4-methyl-2-phenyl-1,5-benzothiazepine-3-carboxylic acid esters and 2,5-dihydro-4-methyl-2-phenyl-1,5-benzodiazepine-3-carboxylic acid esters
Karnail S. Atwal, James L. Bergey, Anders Hedberg, and Suzanne Moreland
pp 635 - 640; DOI:
10.1021/jm00387a009
PDF
Synthesis and calcium channel antagonist activity of dialkyl 4-(dihydropyridinyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylates
Lina Dagnino, Moy Cheong Li-Kwong-Ken, Hla Wynn, Michael W. Wolowyk, Christopher R. Triggle, and Edward E. Knaus
pp 640 - 646; DOI:
10.1021/jm00387a010
PDF
Steroidal silicon side-chain analogs as potential antifertility agents
Richard H. Peters, David F. Crowe, Masato Tanabe, Mitchell A. Avery, and Wesley K. M. Chong
pp 646 - 652; DOI:
10.1021/jm00387a011
PDF
Potential antitumor agents. 48. 3'-Dimethylamino derivatives of amsacrine: redox chemistry and in vivo solid tumor activity
Graham J. Atwell, Gordon W. Rewcastle, Bruce C. Baguley, and William A. Denny
pp 652 - 658; DOI:
10.1021/jm00387a012
PDF
Potential antitumor agents. 49. 5-Substituted derivatives of N-[2-(dimethylamino)ethyl]-9-aminoacridine-4-carboxamide with in vivo solid-tumor activity
William A. Denny, Graham J. Atwell, Gordon W. Rewcastle, and Bruce C. Baguley
pp 658 - 663; DOI:
10.1021/jm00387a013
PDF
Potential antitumor agents. 50. In vivo solid-tumor activity of derivatives of N-[2-(dimethylamino)ethyl]acridine-4-carboxamide
Graham J. Atwell, Gordon W. Rewcastle, Bruce C. Baguley, and William A. Denny
pp 664 - 669; DOI:
10.1021/jm00387a014
PDF
Synthesis and tumor uptake of 5-halo-1-(2'-fluoro-2'-deoxy-.beta.-D-ribofuranosyl)[2-14C]uracils
John R. Mercer, Edward E. Knaus, and Leonard I. Wiebe
pp 670 - 675; DOI:
10.1021/jm00387a015
PDF
Folate analogs as inhibitors of thymidylate synthase
Diana I. Brixner, Takamori Ueda, Yung Chi Cheng, John B. Hynes, and Arthur D. Broom
pp 675 - 678; DOI:
10.1021/jm00387a016
PDF
Analogs and derivatives of tenoxicam. 1. Synthesis and antiinflammatory activities of analogs with different residues on the ring nitrogen and the amide nitrogen
Dieter Binder, Otto Hromatka, Franz Geissler, Karl Schmied, Christian R. Noe, Kaspar Burri, Rudolf Pfister, Konrad Strub, and Paul Zeller
pp 678 - 682; DOI:
10.1021/jm00387a017
PDF
Leukotriene receptor antagonists. 1. Synthesis and structure-activity relationships of alkoxyacetophenone derivatives
Winston S. Marshall, Theodore Goodson, George J. Cullinan, Dorothy Swanson-Bean, Klaus D. Haisch, Lynn E. Rinkema, and Jerome H. Fleisch
pp 682 - 689; DOI:
10.1021/jm00387a018
PDF
Diethyl 3,6-dihydro-2,4-dimethyl-2,6-methano-1,3-benzothiazocine-5,11-dicarboxylates as calcium entry antagonists: new conformationally restrained analogs of Hantzsch 1,4-dihydropyridines related to nitrendipine as probes for receptor-site conformation
John J. Baldwin, David A. Claremon, Patricia K. Lumma, David E. McClure, Seth A. Rosenthal, Raymond J. Winquist, Elizabeth P. Faison, Gregory J. Kaczorowski, Mayme J. Trumble, and Graham M. Smith
pp 690 - 695; DOI:
10.1021/jm00387a019
PDF
Synthesis and antiarrhythmic activity of novel 3-alkyl-1-[.omega.-[4-[(alkylsulfonyl)amino]phenyl]-.omega.-hydroxyalkyl]-1H-imidazolium salts and related compounds
Randall Lis, Thomas K. Morgan, Robert J. DeVita, David D. Davey, William C. Lumma, Ronald A. Wohl, Julius Diamond, Samuel S. Wong, and Mark E. Sullivan
pp 696 - 704; DOI:
10.1021/jm00387a020
PDF
Inhibition of delayed hypersensitivity reactions by cinnamyl 1-thioglycosides
Mitree M. Ponpipom, Robert L. Bugianesi, and Thomas J. Blake
pp 705 - 710; DOI:
10.1021/jm00387a021
PDF
Structural aspects of ryanodine action and selectivity
Andrew L. Waterhouse, Issac N. Pessah, Alexander O. Francini, and John E. Casida
pp 710 - 716; DOI:
10.1021/jm00387a022
PDF
Comparative antitumor studies on platinum(II) and platinum(IV) complexes containing 1,2-diaminocyclohexane
Jean F. Vollano, Salaam Al-Baker, James C. Dabrowiak, and John E. Schurig
pp 716 - 719; DOI:
10.1021/jm00387a023
PDF
S-[(N,N'-Diarylamidino)methyl] diethyldithiocarbamates and related amides as potential radioprotectants
T. Pantev
pp 720 - 721; DOI:
10.1021/jm00387a024
PDF
.beta.-Adrenoceptor antagonist activity of bivalent ligands. 1. Diamide analogs of practolol.
H. Kizuka and R. N. Hanson
pp 722 - 726; DOI:
10.1021/jm00387a025
PDF
Benzimidazole derivatives with atypical antiinflammatory activity
Edward S. Lazer, Martha R. Matteo, and Genus J. Possanza
pp 726 - 729; DOI:
10.1021/jm00387a026
PDF
Synthesis and binding affinities of analogs of cholecystokinin-(30-33) as probes for central nervous system cholecystokinin receptors
David C. Horwell, Andrew Beeby, Colin R. Clark, and John Hughes
pp 729 - 732; DOI:
10.1021/jm00387a027
PDF
A novel synthesis of colchicide and analogs from thiocolchicine and congeners: reevaluation of colchicide as a potential antitumor agent
Raymond Dumont, Arnold Brossi, Colin F. Chignell, Frank R. Quinn, and Matthew Suffness
pp 732 - 735; DOI:
10.1021/jm00387a028
PDF
Structure-activity studies of antagonists of luteinizing hormone-releasing hormone with emphasis on the amino-terminal region
Simon J. Hocart, Mary V. Nekola, and David H. Coy
pp 735 - 739; DOI:
10.1021/jm00387a029
PDF
Effect of reductive alkylation of D-lysine in position 6 on the histamine-releasing activity of luteinizing hormone-releasing hormone antagonists
Simon J. Hocart, Mary V. Nekola, and David H. Coy
pp 739 - 743; DOI:
10.1021/jm00387a030
PDF
Synthesis and pharmacological evaluation of .gamma.-aminobutyric acid analogs. New ligand for GABAB sites
Pascal Berthelot, Claude Vaccher, Amir Musadad, Nathalie Flouquet, Michel Debaert, and Michel Luyckx
pp 743 - 746; DOI:
10.1021/jm00387a031
PDF
Resolution of racemic carbocyclic analogs of purine nucleosides through the action of adenosine deaminase. Antiviral activity of the carbocyclic 2'-deoxyguanosine enantiomers
John A. Secrist, John A. Montgomery, Y. Fulmer Shealy, C. Allen O'Dell, and Sarah Jo Clayton
pp 746 - 749; DOI:
10.1021/jm00387a032
PDF
Synthesis of 6-substituted .beta.-carbolines that behave as benzodiazepine receptor antagonists or inverse agonists
Timothy J. Hagen, Phil Skolnick, and James M. Cook
pp 750 - 753; DOI:
10.1021/jm00387a033
PDF
Book Reviews

pp 753 - 754; DOI:
10.1021/jm00387a600
PDF

Issue 5


Rational design of 4-[(methylsulfonyl)amino]benzamides as class III antiarrhythmic agents
William C. Lumma Jr., Ronald A. Wohl, David D. Davey, Thomas M. Argentieri, Robert J. DeVita, Robert P. Gomez, Vijay K. Jain, Anthony J. Marisca, Thomas K. Morgan Jr., and et al.
pp 755 - 758; DOI:
10.1021/jm00388a001
PDF
Synthesis and biological activity of partially modified retro-inverso pseudopeptide derivatives of the C-terminal tetrapeptide of gastrin
Marc Rodriguez, Philibert Dubreuil, Jean Pierre Bali, and Jean Martinez
pp 758 - 763; DOI:
10.1021/jm00388a002
PDF
Synthesis and pharmacological evaluation of a new class of 2-(2-aminothiazol-4-yl)-2-hydrazonoacetamido cephalosporins
Alberto Brandt, Marina Cerquetti, G. Bruno Corsi, Giorgio Pascucci, Antonio Simeoni, Paola Martelli, and Umberto Valcavi
pp 764 - 767; DOI:
10.1021/jm00388a003
PDF
The metabolism of carbamazepine in humans: steric course of the enzymic hydrolysis of the 10,11-epoxide
Giuseppe Bellucci, Giancarlo Berti, Cinzia Chiappe, Annalisa Lippi, and Franco Marioni
pp 768 - 773; DOI:
10.1021/jm00388a004
PDF
Synthesis and antiarrhythmic activity of new 3-[2-(.omega.-aminoalkoxy)phenoxy]-4-phenyl-3-buten-2-ones and related compounds
Aldo Salimbeni, Elso Manghisi, Giancarlo B. Fregnan, and Marco Prada
pp 773 - 780; DOI:
10.1021/jm00388a005
PDF
Synthesis and antiarrhythmic properties of novel 3-selena-7-azabicyclo[3.3.1]nonanes and derivatives. Single-crystal x-ray diffraction analysis of 7-benzyl-3-selena-7-azabicyclo[3.3.1]nonan-9-one and 7-benzyl-3-selena-7-azabicyclo[3.3.1]nonane hydroperchlorate
M. Daniel Thompson, Gary S. Smith, K. Darrell Berlin, Elizabeth M. Holt, Benjamin J. Scherlag, Dick Van der Helm, Steven W. Muchmore, and Krzysztof A. Fidelis
pp 780 - 788; DOI:
10.1021/jm00388a006
PDF
Flavones. 1. Synthesis and antihypertensive activity of (3-phenylflavonoxy)propanolamines without .beta.-adrenoceptor antagonism
E. S. C. Wu, T. E. Cole, T. A. Davidson, J. C. Blosser, A. R. Borrelli, C. R. Kinsolving, T. E. Milgate, and R. B. Parker
pp 788 - 792; DOI:
10.1021/jm00388a007
PDF
Structure-activity relationship in PAF-acether. 3. Hydrophobic contribution to agonistic activity
Jean Jacques Godfroid, Colette Broquet, Simone Jouquey, Mariya Lebbar, Francoise Heymans, Catherine Redeuilh, Efroim Steiner, Elie Michel, Eliane Coeffier, and et al.
pp 792 - 797; DOI:
10.1021/jm00388a008
PDF
Resolution, absolute stereochemistry, and enantioselective activity of nomifensine and hexahydro-1H-indeno[1,2-b]pyridines
Rudolf Kunstmann, Hermann Gerhards, Hansjoerg Kruse, Margret Leven, Erich F. Paulus, Ulrich Schacht, Karl Schmitt, and Peter U. Witte
pp 798 - 804; DOI:
10.1021/jm00388a009
PDF
6-Methyl-6-azabicyclo[3.2.1]octan-3.alpha.-ol 2,2-diphenylpropionate (azaprophen), a highly potent antimuscarinic agent
F. Ivy Carroll, Philip Abraham, Karol Parham, Ronald C. Griffith, Ateeq Ahmad, Michelle M. Richard, Felipe N. Padilla, Jeffrey M. Witkin, and Peter K. Chiang
pp 805 - 809; DOI:
10.1021/jm00388a010
PDF
Synthesis of new heparinoids with high anticoagulant activity
Kenichi Hatanaka, Takashi Yoshida, Shintaro Miyahara, Takahiro Sato, Fujihiko Ono, Toshiyuki Uryu, and Hiroyoshi Kuzuhara
pp 810 - 814; DOI:
10.1021/jm00388a011
PDF
Synthesis and neuroleptic activity of a series of 1-[1-(benzo-1,4-dioxan-2-ylmethyl)-4-piperidinyl]benzimidazolone derivatives
Rainer Henning, Rudolf Lattrell, Hermann J. Gerhards, and Margret Leven
pp 814 - 819; DOI:
10.1021/jm00388a012
PDF
Synthesis and antiinflammatory and analgesic activity of 5-aroyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids. The 6-substituted compounds.
Joseph M. Muchowski, Gary F. Cooper, Otto Halpern, Richard Koehler, Arthur F. Kluge, Robert L. Simon, Stefan H. Unger, Albert R. Van Horn, Douglas L. Wren, and et al.
pp 820 - 823; DOI:
10.1021/jm00388a013
PDF
Dihydropyridazinone cardiotonics: synthesis and inotropic activity of 5'-(1,4,5,6-tetrahydro-6-oxo-3-pyridazinyl)-spiro[cycloalkane-1,3'-[3H]indol]-2'(1'H)-ones
David W. Robertson, Joseph H. Krushinski, G. Don Pollock, Harve Wilson, Raymond F. Kauffman, and J. Scott Hayes
pp 824 - 829; DOI:
10.1021/jm00388a014
PDF
Estrogenic affinity labels: synthesis, irreversible receptor binding, and bioactivity of aziridine-substituted hexestrol derivatives
Jeffery A. Zablocki, John A. Katzenellenbogen, Kathryn E. Carlson, M. J. Norman, and Benita S. Katzenellenbogen
pp 829 - 838; DOI:
10.1021/jm00388a015
PDF
Synthesis, absolute configuration, and antibacterial activity of 6,7-dihydro-5,8-dimethyl-9-fluoro-1-oxo-1H,5H-benzo[ij]quinolizine-2-carboxylic acid
John F. Gerster, Steve R. Rohlfing, Sharon E. Pecore, Richard M. Winandy, Richard M. Stern, June E. Landmesser, Roger A. Olsen, and William B. Gleason
pp 839 - 843; DOI:
10.1021/jm00388a016
PDF
Potential antitumor agents. 51. Synthesis and antitumor activity of substituted phenazine-1-carboxamides
Gordon W. Rewcastle, William A. Denny, and Bruce C. Baguley
pp 843 - 851; DOI:
10.1021/jm00388a017
PDF
Kinetics of solvolysis and muscarinic actions of a (2-bromoethyl)methylamino analog of oxotremorine
Bjorn Ringdahl and Donald J. Jenden
pp 852 - 854; DOI:
10.1021/jm00388a018
PDF
Relationships between DNA-binding kinetics and biological activity for the 9-aminoacridine-4-carboxamide class of antitumor agents
Laurence P. G. Wakelin, Graham J. Atwell, Gordon W. Rewcastle, and William A. Denny
pp 855 - 861; DOI:
10.1021/jm00388a019
PDF
Potential anti-AIDS drugs. 2',3'-Dideoxycytidine analogs
Chong Ho Kim, Victor E. Marquez, Samuel Broder, Hiroaki Mitsuya, and John S. Driscoll
pp 862 - 866; DOI:
10.1021/jm00388a020
PDF
1-(2-Deoxy-2-fluoro-.beta.-D-arabinofuranosyl)-5-ethyluracil. A highly selective antiherpes simplex agent
Muzammil M. Mansuri, Ismail Ghazzouli, Ming S. Chen, Henry G. Howell, Paul R. Brodfuehrer, Daniel A. Benigni, and John C. Martin
pp 867 - 871; DOI:
10.1021/jm00388a021
PDF
Structure-activity relationships in the 2-arylcarbapenem series. Synthesis of 1-methyl-2-arylcarbapenems
Ravindra Nath Guthikonda, L. D. Cama, M. Quesada, M. F. Woods, T. N. Salzmann, and B. G. Christensen
pp 871 - 880; DOI:
10.1021/jm00388a022
PDF
Anticonvulsant O-alkyl sulfamates. 2,3:4,5-Bis-O-(1-methylethylidene)-.beta.-D-fructopyranose sulfamate and related compounds
Bruce E. Maryanoff, Samuel O. Nortey, Joseph F. Gardocki, Richard P. Shank, and Susanna P. Dodgson
pp 880 - 887; DOI:
10.1021/jm00388a023
PDF
Isozyme-specific enzyme inhibitors. 13. S-[5'(R)-['N-triphosphoamino)methyl]adenosyl]-L-homocysteine, a potent inhibitor of rat methionine adenosyltransferases
Vivekananda M. Vrudhula, Francis Kappler, and Alexander Hampton
pp 888 - 894; DOI:
10.1021/jm00388a024
PDF
Antisecretory activity of human, dog, and rat metabolites of fenoctimine
Malcolm K. Scott, Henry I. Jacoby, Antoinette C. Bonfilio, Thomas W. Corcoran, and Iris S. Lopez
pp 894 - 899; DOI:
10.1021/jm00388a025
PDF
A quantitative structure-activity relationship analysis of some 4-aminodiphenyl sulfone antibacterial agents using linear free energy and molecular modeling methods
Rosa L. Lopez de Compadre, R. A. Pearlstein, A. J. Hopfinger, and J. K. Seydel
pp 900 - 906; DOI:
10.1021/jm00388a026
PDF
Antimalarial drugs. 61. Synthesis and antimalarial effects of 4-[(7-chloro-4-quinolinyl)amino]-2-[(diethylamino)methyl]-6-alkylphenols and their N.omega.-oxides
Stephen J. Kesten, Judith Johnson, and Leslie M. Werbel
pp 906 - 911; DOI:
10.1021/jm00388a027
PDF
Leukotriene receptor antagonists. 2. The [[(tetrazol-5-ylaryl)oxy]methyl]acetophenone derivatives
Robert D. Dillard, F. Patrick Carr, Doris McCullough, Klaus D. Haisch, Lynn E. Rinkema, and Jerome H. Fleisch
pp 911 - 918; DOI:
10.1021/jm00388a028
PDF
Preparation and biological evaluation of a potential photoaffinity label for the prostaglandin H2/thromboxane A2 receptor
S. K. Arora, E. J. Kattelman, C. T. Lim, G. C. Le Breton, and D. L. Venton
pp 918 - 924; DOI:
10.1021/jm00388a029
PDF
Nucleosides. 141. Synthesis of 5-.beta.-D-ribofuranosylnicotinamide and its N-methyl derivative. The isosteric and isoelectronic analogs of nicotinamide nucleoside
Marek M. Kabat, Krzysztof W. Pankiewicz, and Kyoichi A. Watanabe
pp 924 - 927; DOI:
10.1021/jm00388a030
PDF
Reactive 5'-substituted 2',5'-dideoxyuridine derivatives as potential inhibitors of nucleotide biosynthesis
Robert D. Elliott, Pamela S. Pruett, R. Wallace Brockman, and John A. Montgomery
pp 927 - 930; DOI:
10.1021/jm00388a031
PDF
N-Methyl derivatives of the 5-HT2 agonist 1-(4-bromo-2,5-dimethoxyphenyl)-2-aminopropane
Richard A. Glennon, Milt Titeler, Mark Seggel, and Robert A. Lyon
pp 930 - 932; DOI:
10.1021/jm00388a032
PDF
Opioid agonist and antagonist activities of monofunctional nitrogen mustard analogs of .beta.-chlornaltrexamine (.beta.-CNA)
J. W. Schoenecker, A. E. Takemori, and P. S. Portoghese
pp 933 - 935; DOI:
10.1021/jm00388a033
PDF
O-Carbamoylsalicylates: agents for modification of hemoglobins
Kumarapuram N. Parameswaran, Guey Yeh Shi, and Irving M. Klotz
pp 936 - 939; DOI:
10.1021/jm00388a034
PDF
Imidazole anticonvulsants: structure-activity relationships of [(biphenylyloxy)alkyl]imidazoles
David W. Robertson, E. E. Beedle, Ron Lawson, and J. David Leander
pp 939 - 943; DOI:
10.1021/jm00388a035
PDF
Synthesis and biological activity of unsaturated carboacyclic purine nucleoside analogs
David R. Haines, Christopher K. H. Tseng, and Victor E. Marquez
pp 943 - 947; DOI:
10.1021/jm00388a036
PDF
Hexahydro-1H-1-pyrindines from acid rearrangement of 9-alkylidene-5-(m-methoxyphenyl)-2-methylmorphans. Structural type of narcotic antagonists
Hiroyoshi Awaya, Everette L. May, Mario D. Aceto, Louis S. Harris, James V. Silverton, Kenner C. Rice, Mariena V. Mattson, and Arthur E. Jacobson
pp 947 - 950; DOI:
10.1021/jm00388a037
PDF
Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 3. Guanidines
Christopher B. Chapleo, Peter L. Myers, Alan C. B. Smith, Ian F. Tulloch, and Donald S. Walter
pp 951 - 954; DOI:
10.1021/jm00388a038
PDF
N6-Phenyladenosines: pronounced effect of phenyl substituents on affinity for A2 adenosine receptors
Madan M. Kwatra, Edward Leung, M. Marlene Hosey, and Richard D. Green
pp 954 - 956; DOI:
10.1021/jm00388a039
PDF
Book Reviews

pp 956 - 958; DOI:
10.1021/jm00388a600
PDF

Issue 6


High-affinity leukotriene receptor antagonists. Synthesis and pharmacological characterization of 2-hydroxy-3-[(2-carboxyethyl)thio]-3-[2-(8-phenyloctyl)phenyl]propanoic acid
John G. Gleason, Ralph F. Hall, Carl D. Perchonock, Karl F. Erhard, James S. Frazee, Thomas W. Ku, Karen Kondrad, Mary E. McCarthy, Seymour Mong, and et al.
pp 959 - 961; DOI:
10.1021/jm00389a001
PDF
Investigation of peripheral cholecystokinin receptor heterogeneity by cyclic and related linear analogs of CCK26-33. Synthesis and biological properties
Bruno Charpentier, Christiane Durieux, Isabelle Menant, and Bernard P. Roques
pp 962 - 968; DOI:
10.1021/jm00389a002
PDF
Synthesis and characterization of all four isomers of the muscarinic agonist, 2'-methylspiro[1-azabicyclo[2.2.2]octane-3,4'-[1,3]dioxolane]
John Saunders, Graham A. Showell, Raymond Baker, Stephen B. Freedman, David Hill, Alexander McKnight, Nigel Newberry, John D. Salamone, Jordan Hirshfield, and James P. Springer
pp 969 - 975; DOI:
10.1021/jm00389a003
PDF
Renin inhibitors. Design of angiotensinogen transition-state analogs containing novel (2R,3R,4R,5S)-5-amino-3,4-dihydroxy-2-isopropyl-7-methyloctanoic acid
Suvit Thaisrivongs, Donald T. Pals, Lisa T. Kroll, Steve R. Turner, and Fu Son Han
pp 976 - 982; DOI:
10.1021/jm00389a004
PDF
Systematic synthesis and biological evaluation of .alpha.- and .beta.-D-lyxofuranosyl nucleosides of the five naturally occurring nucleic acid bases
Gilles Gosselin, Marie Christine Bergogne, Jean De Rudder, Erik De Clercq, and Jean Louis Imbach
pp 982 - 991; DOI:
10.1021/jm00389a005
PDF
Synthesis and structure activity relationships of potent new angiotensin converting enzyme inhibitors containing saturated bicyclic amino acids
C. J. Blankley, J. S. Kaltenbronn, D. E. DeJohn, A. Werner, L. R. Bennett, G. Bobowski, U. Krolls, D. R. Johnson, and W. M. Pearlman
pp 992 - 998; DOI:
10.1021/jm00389a006
PDF
2,4-Diamino-6,7-dimethoxyquinazolines. 2. 2-(4-Carbamoylpiperidino) derivatives as .alpha.1-adrenoceptor antagonists and antihypertensive agents
Valerie A. Alabaster, Simon F. Campbell, John C. Danilewicz, Colin W. Greengrass, and Rhona M. Plews
pp 999 - 1003; DOI:
10.1021/jm00389a007
PDF
Synthesis of a series of compounds related to betaxolol, a new .beta.1-adrenoceptor antagonist with a pharmacological and pharmacokinetic profile optimized for the treatment of chronic cardiovascular diseases
Philippe M. Manoury, Jean L. Binet, Jean Rousseau, Francoise M. Lefevre-Borg, and Icilio G. Cavero
pp 1003 - 1011; DOI:
10.1021/jm00389a008
PDF
Conformationally defined adrenergic agents. 5. Resolution, absolute configuration, and pharmacological characterization of the enantiomers of 2-(5,6-dihydroxy-1,2,3,4-tetrahydro-1-naphthyl)imidazoline: a potent agonist at .alpha.-adrenoceptors
John F. DeBernardis, Daniel J. Kerkman, David L. Arendsen, Steve A. Buckner, John J. Kyncl, and Arthur A. Hancock
pp 1011 - 1017; DOI:
10.1021/jm00389a009
PDF
Inhibition of human sputum elastase by substituted 2-pyrones. 2
Luisa Cook, Bela Ternai, and Peter Ghosh
pp 1017 - 1023; DOI:
10.1021/jm00389a010
PDF
Cardiotonic agents. 5. 1,2-Dihydro-5-[4-(1H-imidazol-1-yl)phenyl]-6-methyl-2-oxo-3-pyridinecarbonitriles and related compounds. Synthesis and inotropic activity
Ila Sircar, Bradley L. Duell, James A. Bristol, Ronald E. Weishaar, and Dale B. Evans
pp 1023 - 1029; DOI:
10.1021/jm00389a011
PDF
Selective thromboxane synthetase inhibitors and antihypertensive agents. New derivatives of 4-hydrazino-5H-pyridazino[4,5-b]indole, 4-hydrazinotriazino[4,5-a]indole, and related compounds
A. Monge, P. Parrado, M. Font, and E. Fernandez-Alvarez
pp 1029 - 1035; DOI:
10.1021/jm00389a012
PDF
Thromboxane synthetase inhibitors and antihypertensive agents. 3. N-[(1H-imidazol-1-yl)alkyl]heteroaryl amides as potent enzyme inhibitors
Jeffery B. Press, William B. Wright, Peter S. Chan, Margie F. Haug, Joseph W. Marsico, and Andrew S. Tomcufcik
pp 1036 - 1040; DOI:
10.1021/jm00389a013
PDF
Nonequilibrium opioid antagonist activity of 6,14-dideoxynaltrexone derivatives
J. W. Schoenecker, A. E. Takemori, and P. S. Portoghese
pp 1040 - 1044; DOI:
10.1021/jm00389a014
PDF
Synthesis, structure, and biological activity of certain 2-deoxy-.beta.-D-ribo-hexopyranosyl nucleosides and nucleotides
L. Dee Nord, N. Kent Dalley, Patricia A. McKernan, and Roland K. Robins
pp 1044 - 1054; DOI:
10.1021/jm00389a015
PDF
Synthesis and oral antifungal activity of novel azolylpropanolones and related compounds
Masaru Ogata, Hiroshi Matsumoto, Kimio Takahashi, Sumio Shimizu, Shiro Kida, Akira Murabayashi, Motoo Shiro, and Katsuya Tawara
pp 1054 - 1068; DOI:
10.1021/jm00389a016
PDF
Synthesis and structure-activity studies of corticosteroid 17-heterocyclic aromatic esters. 1. 9.alpha.,11.beta.-Dichloro series
Elliot L. Shapiro, Margaret J. Gentles, Robert L. Tiberi, Thomas L. Popper, Joseph Berkenkopf, Barry Lutsky, and Arthur S. Watnick
pp 1068 - 1073; DOI:
10.1021/jm00389a017
PDF
Inhibition of the mammalian .beta.-lactamase renal dipeptidase (dehydropeptidase-I) by Z-2-(acylamino)-3-substituted-propenoic acids
Donald W. Graham, Wallace T. Ashton, Louis Barash, Jeannette E. Brown, Ronald D. Brown, Laura F. Canning, Anna Chen, James P. Springer, and Edward F. Rogers
pp 1074 - 1090; DOI:
10.1021/jm00389a018
PDF
Synthesis and antiviral evaluation of carbocyclic analogs of 2-amino-6-substituted-purine 3'-deoxyribofuranosides
Y. Fulmer Shealy, C. Allen O'Dell, and Gussie Arnett
pp 1090 - 1094; DOI:
10.1021/jm00389a019
PDF
Resolution of (.+-.)-2-tetradecyloxiranecarboxylic acid. Absolute configuration and chiral synthesis of the hypoglycemic R enantiomer and biological activity of enantiomers
Winston Ho, Okan Tarhan, Timothy C. Kiorpes, Gene F. Tutwiler, and Richard J. Mohrbacher
pp 1094 - 1097; DOI:
10.1021/jm00389a020
PDF
Long-acting angiotensin II inhibitors containing hexafluorovaline in position 8
Kun Hwa Hsieh, Philip Needleman, and Garland R. Marshall
pp 1097 - 1100; DOI:
10.1021/jm00389a021
PDF
Psychotropic agents: synthesis and antipsychotic activity of substituted .beta.-carbolines
Magid Abou-Gharbia, Usha R. Patel, John A. Moyer, and Eric A. Muth
pp 1100 - 1105; DOI:
10.1021/jm00389a022
PDF
2-Amino- and 2-guanidino-1,2,3,4-tetrahydro-1,4-epoxynaphthalenes as conformationally defined analogs of .alpha.-adrenergic agents
Edward C. R. Smith, Thomas N. Riley, Ronald F. Borne, and I. W. Waters
pp 1105 - 1110; DOI:
10.1021/jm00389a023
PDF
Spectroscopic detection of iminocyclophosphamide and its possible role in cyclophosphamide metabolism
Chul Hoon Kwon, Marion C. Kirk, Robert F. Struck, and Richard F. Borch
pp 1110 - 1114; DOI:
10.1021/jm00389a024
PDF

Issue 7


Conformational analysis of 2-aminoindans and 2-(aminomethyl)indans in relation to their central dopaminergic effects and a dynamic dopamine receptor concept
Hakan Wikstrom, Jenn-Huei Lii, and Norman L. Allinger
pp 1115 - 1120; DOI:
10.1021/jm00390a001
PDF
The role of solvent-accessible surface area in determining partition coefficients
W. J. Dunn, M. G. Koehler, and Stelian Grigoras
pp 1121 - 1126; DOI:
10.1021/jm00390a002
PDF
Peptide quantitative structure-activity relationships, a multivariate approach
Sven Hellberg, Michael Sjoestroem, Bert Skagerberg, and Svante Wold
pp 1126 - 1135; DOI:
10.1021/jm00390a003
PDF
C3-Methylated 5-hydroxy-2-(dipropylamino)tetralins: conformational and steric parameters of importance for central dopamine receptor activation
Anette M. Johansson, J. Lars G. Nilsson, Anders Karlen, Uli Hacksell, Kjell Svensson, Arvid Carlsson, Lennart Kenne, and Staffan Sundell
pp 1135 - 1144; DOI:
10.1021/jm00390a004
PDF
N,N-Dialkylated leucine enkephalins as potential .delta. opioid receptor antagonists
Jane A. Lovett and Philip S. Portoghese
pp 1144 - 1149; DOI:
10.1021/jm00390a005
PDF
Zwitterionic analogs of cimetidine as H2 receptor antagonists
Rodney C. Young, C. Robin Ganellin, Michael J. Graham, Robert C. Mitchell, Michael L. Roantree, and Zev Tashma
pp 1150 - 1156; DOI:
10.1021/jm00390a006
PDF
A novel class of cardiotonics. Synthesis and pharmacological properties of [4-(substituted-amino)phenyl]pyridazinones and related derivatives
Hiromi Okushima, Akihiro Narimatsu, Makio Kobayashi, Rikizo Furuya, Kunio Tsuda, and Yoshimi Kitada
pp 1157 - 1161; DOI:
10.1021/jm00390a007
PDF
Solid-phase synthesis and biological properties of .psi.[CH2NH] pseudopeptide analogs of a highly potent somatostatin octapeptide
Yusuke Sasaki, William A. Murphy, Mark L. Heiman, Valentine A. Lance, and David H. Coy
pp 1162 - 1166; DOI:
10.1021/jm00390a008
PDF
Synthesis and evaluation of non-catechol D-1 and D-2 dopamine receptor agonists: benzimidazol-2-one, benzoxazol-2-one, and the highly potent: benzothiazol-2-one 7-ethylamines
Joseph Weinstock, Dimitri E. Gaitanopoulos, Orum D. Stringer, Robert G. Franz, J. Paul Hieble, Lewis B. Kinter, William A. Mann, Kathryn E. Flaim, and George Gessner
pp 1166 - 1176; DOI:
10.1021/jm00390a009
PDF
Synthesis and 5-lipoxygenase inhibitory activity of 5-hydroperoxy-6,8,11,14-eicosatetraenoic acid analogs
Francis A. J. Kerdesky, Steven P. Schmidt, James H. Holms, Richard D. Dyer, George W. Carter, and Dee W. Brooks
pp 1177 - 1186; DOI:
10.1021/jm00390a010
PDF
Structure-activity relationships among di- and tetramine disulfides related to benextramine
M. Alvarez, R. Granados, D. Mauleon, G. Rosell, M. Salas, J. Salles, and N. Valls
pp 1186 - 1193; DOI:
10.1021/jm00390a011
PDF
Modifications of primaquine as antimalarials. 4. 5-Alkoxy derivatives of primaquine
Eugene H. Chen, Keiichi Tanabe, Andrew J. Saggiomo, and Edward A. Nodiff
pp 1193 - 1199; DOI:
10.1021/jm00390a012
PDF
2'-Fluorinated arabinonucleosides of 5-(2-haloalkyl)uracil: synthesis and antiviral activity
Herfried Griengl, Erich Wanek, Wolfgang Schwarz, Wolfgang Streicher, Brigitte Rosenwirth, and Erik De Clercq
pp 1199 - 1204; DOI:
10.1021/jm00390a013
PDF
Synthesis and biological properties of some 6H-pyrido[4,3-b]carbazoles
Sydney Archer, Bruce S. Ross, Livia Pica-Mattoccia, and Donato Cioli
pp 1204 - 1210; DOI:
10.1021/jm00390a014
PDF
N,N-Disubstituted 6-alkoxy-2-pyridinamines as anticonvulsant agents
Michael R. Pavia, Charles P. Taylor, Fred M. Hershenson, and Sandra J. Lobbestael
pp 1210 - 1214; DOI:
10.1021/jm00390a015
PDF
Synthesis and anticonvulsant activity of analogs of 4-amino-N-(1-phenylethyl)benzamide
C. Randall Clark and Timothy W. Davenport
pp 1214 - 1218; DOI:
10.1021/jm00390a016
PDF
Quantitative structure-activity relationship of triazine-antifolate inhibition of Leishmania dihydrofolate reductase and cell growth
Raymond G. Booth, Cynthia Dias Selassie, Corwin Hansch, and Daniel V. Santi
pp 1218 - 1224; DOI:
10.1021/jm00390a017
PDF
Novel renin inhibitors containing analogs of statine retro-inverted at the C-termini. Specificity at the P2 histidine site
Saul H. Rosenberg, Jacob J. Plattner, Keith W. Woods, Herman H. Stein, Patrick A. Marcotte, Jerome Cohen, and Thomas J. Perun
pp 1224 - 1228; DOI:
10.1021/jm00390a018
PDF
Design of nonpeptidal ligands for a peptide receptor: cholecystokinin antagonists
B. E. Evans, K. E. Rittle, M. G. Bock, R. M. DiPardo, R. M. Freidinger, W. L. Whitter, N. P. Gould, G. F. Lundell, C. F. Homnick, and et al.
pp 1229 - 1239; DOI:
10.1021/jm00390a019
PDF
Chemical and enzymatic oxidative coupling of 5-hydroxy-N-dimethyltryptamine with amines
Fabienne Babin and Tam Huynh-Dinh
pp 1239 - 1241; DOI:
10.1021/jm00390a020
PDF
Radioiodinated p-iodoclonidine. A high-affinity probe for the .alpha.2-adrenergic receptor
M. Van Dort, R. Neubig, and R. E. Counsell
pp 1241 - 1244; DOI:
10.1021/jm00390a021
PDF
Synthesis and antitumor activity of tropolone derivatives. 5
Masatoshi Yamato, Kuniko Hashigaki, Junko Sakai, Yasuo Takeuchi, Shigeru Tsukagoshi, Tazuko Tashiro, and Takashi Tsuruo
pp 1245 - 1248; DOI:
10.1021/jm00390a022
PDF
Synthesis of .beta.-carboline-benzodiazepine hybrid molecules: use of the known structural requirements for benzodiazepine and .beta.-carboline binding in designing a novel, high-affinity ligand for the benzodiazepine receptor
Robert H. Dodd, Catherine Ouannes, Marie Claude Potier, Lia Prado de Carvalho, Jean Rossier, and Pierre Potier
pp 1248 - 1254; DOI:
10.1021/jm00390a023
PDF
N10-Substituted 5,8-dideazafolate inhibitors of glycinamide ribonucleotide transformylase
Carol A. Caperelli
pp 1254 - 1256; DOI:
10.1021/jm00390a024
PDF
Folate analogs. 30. Synthesis and biological evaluation of N10-propargyl-5,8-dideaza-5,6,7,8-tetrahydrofolic acid and related compounds.
M. G. Nair, Rashmi Dhawan, M. Ghazala, T. I. Kalman, Y. Gaumont, R. L. Kisliuk, and R. Ferone
pp 1256 - 1261; DOI:
10.1021/jm00390a025
PDF
Additions and Corrections-Enantiomers of 3-(3,4-Dihydroxyphenyl)- and 3-(3-Hydroxyphenyl)-N-n-propylpiperdine: Central Pre- and Postsynaptic Dopaminergic Effects and Pharmacokinetics
Hans Rollema, Dora Mastebroek, Hakan Wikstrom, Kjell Svensson, Arvid Carlsson, and Staffan Sundell
pp 1261 - 1261; DOI:
10.1021/jm00390a600
PDF
Book Reviews

pp 1262 - 1264; DOI:
10.1021/jm00390a601
PDF

Issue 8


Dissociation of hypolipidemic and antiplatelet actions from adverse myotonic effects of clofibric acid related enantiomers
Dennis R. Feller, Vaijinath S. Kamanna, Howard A. I. Newman, Karl J. Romstedt, Donald T. Witiak, Giancarlo Bettoni, Shirley H. Bryant, Diana Conte-Camerino, Fulvio Loiodice, and Vincenzo Tortorella
pp 1265 - 1267; DOI:
10.1021/jm00391a001
PDF
Stereospecificity of the chloride ion channel: the action of chiral clofibric acid analogs
Giancarlo Bettoni, Fulvio Loiodice, Vincenzo Tortorella, Diana Conte-Camerino, Mercede Mambrini, Ermanno Ferrannini, and Shirley H. Bryant
pp 1267 - 1270; DOI:
10.1021/jm00391a002
PDF
3'-Substituted 2',3'-dideoxynucleoside analogs as potential anti-HIV (HTLV-III/LAV) agents
Piet Herdewijn, Jan Balzarini, Erik De Clercq, Rudi Pauwels, Masanori Baba, Samuel Broder, and Hubert Vanderhaeghe
pp 1270 - 1278; DOI:
10.1021/jm00391a003
PDF
Nonsteroidal cardiotonics. 1. 2-Pyridyl-6,7-dihydro-3H,5H-pyrrolo[2,3-f]benzimidazol-6-ones, a novel class of cardiotonic agents
A. Mertens, B. Mueller-Beckmann, W. Kampe, J. P. Hoelck, and W. Von der Saal
pp 1279 - 1287; DOI:
10.1021/jm00391a004
PDF
Analysis of structure-activity relationships in renin substrate analog inhibitory peptides
Kwan Y. Hui, William D. Carlson, Michael S. Bernatowicz, and Edgar Haber
pp 1287 - 1295; DOI:
10.1021/jm00391a005
PDF
Limited nerve impulse blockade by "leashed" local anesthetics
John F. Butterworth, John R. Moran, George M. Whitesides, and Gary R. Strichartz
pp 1295 - 1302; DOI:
10.1021/jm00391a006
PDF
Synthesis, conformation, and dopaminergic activity of 5,6-ethano-bridged derivatives of selective dopaminergic 3-benzazepines
Joseph Weinstock, Hye Ja Oh, Charles W. DeBrosse, Drake S. Eggleston, Margaret Wise, Kathryn E. Flaim, George W. Gessner, John L. Sawyer, and Carl Kaiser
pp 1303 - 1308; DOI:
10.1021/jm00391a007
PDF
Inhibitors of dopamine .beta.-hydroxylase. 3. Some 1-(pyridylmethyl)imidazole-2-thiones
Stephen T. Ross, Lawrence I. Kruse, Eliot H. Ohlstein, Robert W. Erickson, Mildred Ezekiel, Kathryn E. Flaim, John L. Sawyer, and Barry A. Berkowitz
pp 1309 - 1313; DOI:
10.1021/jm00391a008
PDF
New antitumor agents containing the anthracene nucleus
Timothy P. Wunz, Robert T. Dorr, David S. Alberts, Cynthia L. Tunget, Janine Einspahr, Sharlene Milton, and William A. Remers
pp 1313 - 1321; DOI:
10.1021/jm00391a009
PDF
Antianaphylactic benzophenones and related compounds
Delme Evans, Mark E. Cracknell, John C. Saunders, Christine E. Smith, W. R. Nigel Williamson, William Dawson, and W. John F. Sweatman
pp 1321 - 1327; DOI:
10.1021/jm00391a010
PDF
Stereocontrolled syntheses for the six diastereomeric 1,2-dihydroxy-4,5-diaminocyclohexanes: PtII complexes and P-388 antitumor properties
Donald T. Witiak, David P. Rotella, Joyce A. Filippi, and Judith Gallucci
pp 1327 - 1336; DOI:
10.1021/jm00391a011
PDF
Cardiotonic agents. 1. Novel 8-aryl substituted imidazo[1,2-a]- and -[1,5-a]pyridines and imidazo[1,5-a]pyridinones as potential positive inotropic agents
David Davey, Paul W. Erhardt, William C. Lumma, Jay Wiggins, Mark Sullivan, David Pang, and Elinor Cantor
pp 1337 - 1342; DOI:
10.1021/jm00391a012
PDF
Cardiotonic agents. 2. (Imidazolyl)aroylimidazolones, highly potent and selective positive inotropic agents
Alfred A. Hagedorn, III, Paul W. Erhardt, William C. Lumma Jr., Ronald A. Wohl, Elinor Cantor, Yuo Ling Chou, William R. Ingebretsen, John W. Lampe, David Pang, and et al.
pp 1342 - 1347; DOI:
10.1021/jm00391a013
PDF
Synthesis and antifungal activity of new 1-vinylimidazoles
Masaru Ogata, Hiroshi Matsumoto, Sumio Shimizu, Shiro Kida, Motoo Shiro, and Katsuya Tawara
pp 1348 - 1354; DOI:
10.1021/jm00391a014
PDF
Berbanes: a new class of selective .alpha.2-adrenoceptor antagonists
E. Sylvester Vizi, Istvan Toth, George T. Somogyi, Lajos Szabo, Laszlo G. Harsing, and Csaba Szantay
pp 1355 - 1359; DOI:
10.1021/jm00391a015
PDF
Aromatase inhibition by 5-substituted pyrimidines and dihydropyrimidines
Harold M. Taylor, C. David Jones, James D. Davenport, Kenneth S. Hirsch, T. J. Kress, and Dix Weaver
pp 1359 - 1365; DOI:
10.1021/jm00391a016
PDF
Synthesis and biological activities of pseudopeptide analogs of the C-terminal heptapeptide of cholecystokinin. On the importance of the peptide bonds
Marc Rodriguez, Marie Francoise Lignon, Marie Christine Galas, Pierre Fulcrand, Christiane Mendre, Andre Aumelas, Jeanine Laur, and Jean Martinez
pp 1366 - 1373; DOI:
10.1021/jm00391a017
PDF
.beta.-Substituted cysteines as sequestering agents for ethanol-derived acetaldehyde in vivo
Herbert T. Nagasawa, James A. Elberling, and Jeanette C. Roberts
pp 1373 - 1378; DOI:
10.1021/jm00391a018
PDF
Tricyclic compounds as selective antimuscarinics. 1. Structural requirements for selectivity towards the muscarinic acetylcholine receptor in a series of pirenzepine and imipramine analogs
Wolfgang G. Eberlein, Guenter Trummlitz, Wolfhard W. Engel, Guenther Schmidt, Helmut Pelzer, and Norbert Mayer
pp 1378 - 1382; DOI:
10.1021/jm00391a019
PDF
Synthesis of glycopyranosylphosphonate analogs of certain natural nucleoside diphosphate sugars as potential inhibitors of glycosyltransferases
Morteza M. Vaghefi, Ralph J. Bernacki, N. Kent Dalley, Bruce E. Wilson, and Roland K. Robins
pp 1383 - 1391; DOI:
10.1021/jm00391a020
PDF
Synthesis of certain nucleoside methylenediphosphonate sugars as potential inhibitors of glycosyltransferases
Morteza M. Vaghefi, Ralph J. Bernacki, William J. Hennen, and Roland K. Robins
pp 1391 - 1399; DOI:
10.1021/jm00391a021
PDF
Effects of derivatives of kahweol and cafestol on the activity of glutathione S-transferase in mice
Luke K. T. Lam, Velta L. Sparnins, and Lee W. Wattenberg
pp 1399 - 1403; DOI:
10.1021/jm00391a022
PDF
Aldosterone antagonists. 2. New 7.alpha.-(acetylthio)-15,16-methylene spirolactones
Klaus Nickisch, Dieter Bittler, Henry Laurent, Wolfgang Losert, Jorge Casals-Stenzel, Yukishige Nishino, Ekkehard Schillinger, and Rudolf Wiechert
pp 1403 - 1409; DOI:
10.1021/jm00391a023
PDF
Synthesis of two glucagon antagonists: receptor binding, adenylate cyclase, and effects on blood plasma glucose levels
Beat Gysin, David G. Johnson, Dev Trivedi, and Victor J. Hruby
pp 1409 - 1415; DOI:
10.1021/jm00391a024
PDF
Amplification of bleomycin-mediated degradation of DNA
L. Strekowski, A. Strekowska, R. A. Watson, F. A. Tanious, L. T. Nguyen, and W. D. Wilson
pp 1415 - 1420; DOI:
10.1021/jm00391a025
PDF
Synthesis and cardiotonic activity of a series of substituted 4-alkyl-2(1H)-quinazolinones
Victor T. Bandurco, Charles F. Schwender, Stanley C. Bell, Donald W. Combs, Ramesh M. Kanojia, Seymour D. Levine, Dennis M. Mulvey, Mary A. Appollina, Marianne S. Reed, and et al.
pp 1421 - 1426; DOI:
10.1021/jm00391a026
PDF
gem-Diphosphonate and gem-phosphonate-phosphate compounds with specific high density lipoprotein inducing activity
Nguyen Lan Mong, Eric Niesor, and Craig L. Bentzen
pp 1426 - 1433; DOI:
10.1021/jm00391a027
PDF
Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships
Bruce E. Maryanoff, David F. McComsey, Joseph F. Gardocki, Richard P. Shank, Michael J. Costanzo, Samuel O. Nortey, Craig R. Schneider, and Paulette E. Setler
pp 1433 - 1454; DOI:
10.1021/jm00391a028
PDF
Specific dopamine D-1 and DA1 properties of 4-(mono- and -dihydroxyphenyl)-1,2,3,4-tetrahydroisoquinoline and its tetrahydrothieno[2,3c]pyridine analog
Robert M. Riggs, David E. Nichols, Mark M. Foreman, Lewis L. Truex, Dana Glock, and Jai D. Kohli
pp 1454 - 1458; DOI:
10.1021/jm00391a029
PDF
Chemistry of emeriamine and its analogs and their inhibitory activity in long-chain fatty acid oxidation
Susumu Shinagawa, Tsuneo Kanamaru, Setsuo Harada, Mitsuko Asai, and Hisayoshi Okazaki
pp 1458 - 1463; DOI:
10.1021/jm00391a030
PDF
Methotrexate analogs. 30. Dihydrofolate reductase inhibition and in vitro tumor cell growth inhibition by N.epsilon.-(haloacetyl)-L-lysine and N.delta.-(haloacetyl)-L-ornithine analogs and an acivicin analog of methotrexate
Andre Rosowsky, Vishnu C. Solan, Ronald A. Forsch, Tavner J. Delcamp, David P. Baccanari, and James H. Freisheim
pp 1463 - 1469; DOI:
10.1021/jm00391a031
PDF
Synthesis and .beta.-lactamase inhibitory properties of 2.beta.-[(1,2,3-triazol-1-yl)methyl]-2.alpha.-methylpenam-3.alpha.-carboxylic acid 1,1-dioxide and related triazolyl derivatives
Ronald G. Micetich, Samarendra N. Maiti, Paul Spevak, Tse W. Hall, Shigeru Yamabe, Naobumi Ishida, Motoaki Tanaka, Tomio Yamazaki, Akira Nakai, and Kazuo Ogawa
pp 1469 - 1474; DOI:
10.1021/jm00391a032
PDF
Heteroarotinoids. Synthesis, characterization, and biological activity in terms of an assessment of these systems to inhibit the induction of ornithine decarboxylase activity and to induce terminal differentiation of HL-60 cells
Lyle W. Spruce, Shirish N. Rajadhyaksha, K. Darrell Berlin, Jonathan B. Gale, Edgar T. Miranda, Warren T. Ford, Erich C. Blossey, A. K. Verma, M. B. Hossain, and et al.
pp 1474 - 1482; DOI:
10.1021/jm00391a033
PDF
Synthesis and antidepressant properties of novel 2-substituted 4,5-dihydro-1H-imidazole derivatives
Mark P. Wentland, Denis M. Bailey, E. John Alexander, Michael J. Castaldi, Richard A. Ferrari, Dean R. Haubrich, Daniel A. Luttinger, and Mark H. Perrone
pp 1482 - 1489; DOI:
10.1021/jm00391a034
PDF
X-ray crystal structure of the opioid ligand naltrexonazine
Z. Urbanczyk-Lipkowska, A. W. Lipkowski, M. C. Etter, E. F. Hahn, G. W. Pasternak, and P. S. Portoghese
pp 1489 - 1494; DOI:
10.1021/jm00391a035
PDF
Synthesis and biological activity of 5-(2,2-difluorovinyl)-2'-deoxyuridine
M. Bobek, I. Kavai, and E. De Clercq
pp 1494 - 1497; DOI:
10.1021/jm00391a036
PDF
Synthesis and antifungal activity of a series of novel 1,2-disubstituted propenones
Masaru Ogata, Hiroshi Matsumoto, Shiro Kida, Sumio Shimizu, Katsuya Tawara, and Yoshimi Kawamura
pp 1497 - 1502; DOI:
10.1021/jm00391a037
PDF
Progesterone derivatives that bind to the digitalis receptor: synthesis of 14.beta.-hydroxyprogesterone: a novel steroid with positive inotropic activity
J. F. Templeton, V. P. Sashi Kumar, D. Cote, D. Bose, D. Elliott, R. S. Kim, and F. S. LaBella
pp 1502 - 1505; DOI:
10.1021/jm00391a038
PDF
Endoperoxides as potential antimalarial agents
John A. Kepler, Abraham Philip, Y. W. Lee, H. A. Musallam, and F. Ivy Carroll
pp 1505 - 1509; DOI:
10.1021/jm00391a039
PDF
Synthesis and biological activities of arginine-vasopressin analogs with 4-hydroxyproline in position 7
Angeliki Buku, Irving L. Schwartz, Nocif Yamin, Herman R. Wyssbrod, and Diana Gazis
pp 1509 - 1512; DOI:
10.1021/jm00391a040
PDF
Structure activity studies on the C-terminal hexapeptide of substance P with modifications at the glutaminyl and methioninyl residues
Constantine Poulos, George Stavropoulos, John R. Brown, and Christopher C. Jordan
pp 1512 - 1515; DOI:
10.1021/jm00391a041
PDF
Synthesis of 5-chloro-5,8-dideaza analogs of folic acid and aminopterin targeted for colon adenocarcinoma
J. B. Hynes, A. Kumar, A. Tomazic, and W. L. Washtien
pp 1515 - 1519; DOI:
10.1021/jm00391a042
PDF
Lysosomotropic agents. 7. Broad-spectrum antifungal activity of lysosomotropic detergents
Raymond A. Firestone, Judith M. Pisano, George M. Garrity, Robert A. Fromtling, and Sheldon B. Zimmerman
pp 1519 - 1521; DOI:
10.1021/jm00391a043
PDF
Preparation and antileukemic screening of some new 6'-deoxyhexopyranosyladenine nucleosides
Leon M. Lerner, Bertrum Sheid, and Eric Gaetjens
pp 1521 - 1525; DOI:
10.1021/jm00391a044
PDF
[1-Desamino,7-lysine,8-arginine]vasotocin: attachment of reporter groups and affinity ligands through the lysine side chain
Angeliki Buku, Patrick Eggena, Herman R. Wyssbrod, Irving L. Schwartz, Diana Gazis, Lisa I. Somoza, and John D. Glass
pp 1526 - 1529; DOI:
10.1021/jm00391a045
PDF
Binary drugs: conjugates of purines and a peptide that bind to both adenosine and substance P receptors
Kenneth A. Jacobson, Andrzej W. Lipkowski, Terry W. Moody, William Padgett, Evelyn Pijl, Kenneth L. Kirk, and John W. Daly
pp 1529 - 1532; DOI:
10.1021/jm00391a046
PDF
Book Reviews

pp 1533 - 1534; DOI:
10.1021/jm00391a600
PDF

Issue 9


Indazoles as indole bioisosteres: synthesis and evaluation of the tropanyl ester and amide of indazole-3-carboxylate as antagonists at the serotonin 5HT3 receptor
Pawel Fludzinski, Deborah A. Evrard, William E. Bloomquist, William B. Lacefield, William Pfeifer, Noel D. Jones, Jack B. Deeter, and Marlene L. Cohen
pp 1535 - 1537; DOI:
10.1021/jm00392a001
PDF
Synthesis and activity profiles of new dermorphin-(1-4) peptide analogs
Mauro Marastoni, Severo Salvadori, Gianfranco Balboni, Pier Andrea Borea, Giuliano Marzola, and Roberto Tomatis
pp 1538 - 1542; DOI:
10.1021/jm00392a002
PDF
Nitrogen bridgehead compounds. 66. Bronchodilator nitrogen bridgehead compounds with a pyrimidinone moiety
Istvan Hermecz, Lelle Vasvari-Debreczy, Agnes Horvath, Maria Balogh, Jozsef Kokosi, Christine DeVos, and Ludovic Rodriguez
pp 1543 - 1549; DOI:
10.1021/jm00392a003
PDF
Analogs of 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione as selective inhibitors of aromatase: derivatives with variable 1-alkyl and 3-alkyl substituents
Chui Sheung Leung, Martin G. Rowlands, Michael Jarman, Allan B. Foster, Leslie J. Griggs, and Derry E. V. Wilman
pp 1550 - 1554; DOI:
10.1021/jm00392a004
PDF
.alpha.2-Adrenergic agonists/antagonists: the synthesis and structure-activity relationships of a series of indolin-2-yl and tetrahydroquinolin-2-yl imidazolines
Dennis J. Hlasta, Daniel Luttinger, Mark H. Perrone, Marla J. Silbernagel, Susan J. Ward, and Dean R. Haubrich
pp 1555 - 1562; DOI:
10.1021/jm00392a005
PDF
Carbostyril derivatives having potent .beta.-adrenergic agonist properties
Jan Milecki, Stephen P. Baker, Kelly M. Standifer, Takashi Ishizu, Yasuhiro Chida, John W. Kusiak, and Josef Pitha
pp 1563 - 1566; DOI:
10.1021/jm00392a006
PDF
Resolved cis-10-hydroxy-4-n-propyl-1,2,3,4,4a,5,6,10b-octahydrobenzo[f]quinoline: central serotonin stimulating properties
Haakan Wikstroem, Bengt Andersson, Thomas Elebring, John Jacyno, Norman L. Allinger, Kjell Svensson, Arvid Carlsson, and Staffan Sundell
pp 1567 - 1573; DOI:
10.1021/jm00392a007
PDF
.gamma.-Aminobutyric acid esters. 3. Synthesis, brain uptake, and pharmacological properties of C-18 glyceryl lipid esters of GABA with varying degree of unsaturation
James N. Jacob, Gary W. Hesse, and Victor E. Shashoua
pp 1573 - 1576; DOI:
10.1021/jm00392a008
PDF
Potential antitumor agents. 52. Carbamate analogs of amsacrine with in vivo activity against multidrug-resistant P388 leukemia
Gordon W. Rewcastle, Bruce C. Baguley, Graham J. Atwell, and William A. Denny
pp 1576 - 1581; DOI:
10.1021/jm00392a009
PDF
17-Heteroaroyl esters of corticosteroids. 2. 11.beta.-Hydroxy series
Elliot L. Shapiro, Margaret J. Gentles, Robert L. Tiberi, Thomas L. Popper, Joseph Berkenkopf, Barry Lutsky, and Arthur S. Watnick
pp 1581 - 1588; DOI:
10.1021/jm00392a010
PDF
Structure-activity relationships in an imidazole-based series of thromboxane synthase inhibitors
Paul W. Manley, Nigel M. Allanson, Robert F. G. Booth, Philip E. Buckle, Edward J. Kuzniar, Nagin Lad, Steve M. F. Lai, David O. Lunt, and David P. Tuffin
pp 1588 - 1595; DOI:
10.1021/jm00392a011
PDF
Novel inhibitors of rat lens aldose reductase: N-[[(substituted amino)phenyl]sulfonyl]glycines
Charles A. Mayfield and Jack DeRuiter
pp 1595 - 1598; DOI:
10.1021/jm00392a012
PDF
Isozyme-specific enzyme inhibitors. 14. 5'(R)-C-[(L-homocystein-S-yl)methyl]adenosine 5'-(.beta.,.gamma.-imidotriphosphate), a potent inhibitor of rat methionine adenosyltransferases
Francis Kappler, Vivekananda M. Vrudhula, and Alexander Hampton
pp 1599 - 1603; DOI:
10.1021/jm00392a013
PDF
Phosphorus amino acid analogs as inhibitors of leucine aminopeptidase
Peter P. Giannousis and Paul A. Bartlett
pp 1603 - 1609; DOI:
10.1021/jm00392a014
PDF
New inhibitors of human renin that contain novel Leu-Val replacements
Jay R. Luly, Nwe Yi, Jeff Soderquist, Herman Stein, Jerome Cohen, Thomas J. Perun, and Jacob J. Plattner
pp 1609 - 1616; DOI:
10.1021/jm00392a015
PDF
Fluoro ketone containing peptides as inhibitors of human renin
Karen Fearon, Andreas Spaltenstein, Paul B. Hopkins, and Michael H. Gelb
pp 1617 - 1622; DOI:
10.1021/jm00392a016
PDF
Pyridonecarboxylic acids as antibacterial agents. 9. Synthesis and antibacterial activity of 1-substituted 6-fluoro-1,4-dihydro-4-oxo-7-(4-pyridyl)-1,8-naphthyridine-3-carboxylic acids
Yoshiro Nishimura and Junichi Matsumoto
pp 1622 - 1626; DOI:
10.1021/jm00392a017
PDF
Synthesis and biological properties of actinomycin D chromophoric analogs substituted at the 7-carbon with aziridine and aminopropoxy functions
Raj K. Sehgal, Bijan Almassian, David P. Rosenbaum, Ruth Zadrozny, and Sisir K. Sengupta
pp 1626 - 1631; DOI:
10.1021/jm00392a018
PDF
Charged analogs of chlorpromazine as dopamine antagonists
Marc W. Harrold, Yu An Chang, Raye Ann Wallace, Tahira Farooqui, Lane J. Wallace, Norman Uretsky, and Duane D. Miller
pp 1631 - 1635; DOI:
10.1021/jm00392a019
PDF
Synthesis and antiviral activity of 9-[4-hydroxy-3-(hydroxymethyl)but-1-yl]purines
Michael R. Harnden, Richard L. Jarvest, Teresa H. Bacon, and Malcolm R. Boyd
pp 1636 - 1642; DOI:
10.1021/jm00392a020
PDF
1-Amino-substituted 4-methyl-5H-pyrido[3',4':4,5]pyrrolo[3,2-c]pyridines: a new class of antineoplastic agents
Nguyen Chin Hung, Emile Bisagni, Odile Pepin, Alain Pierre, and Paul De Cointet
pp 1642 - 1647; DOI:
10.1021/jm00392a021
PDF
Aldosterone antagonists. 2. Synthesis and biological activities of 11,12-dehydropregnane derivatives
Susumu Kamata, Takeaki Matsui, Nobuhiro Haga, Masuhisa Nakamura, Kunihiro Odaguchi, Takako Itoh, Toshikatsu Shimizu, Tetsuro Suzuki, Masahiro Ishibashi, and et al.
pp 1647 - 1658; DOI:
10.1021/jm00392a022
PDF
Analgesic dipeptide derivatives. 3. Synthesis and structure-activity relationships of o-nitrophenyl-modified analogs of the analgesic compound H-Lys-Trp(NPS)-OMe
M. Teresa Garcia-Lopez, Rosario Gonzalez-Muniz, M. Teresa Molinero, Jose R. Naranjo, and J. Del Rio
pp 1658 - 1663; DOI:
10.1021/jm00392a023
PDF
5-Acyl-3-substituted benzofuran-2(3H)-ones as potential antiinflammatory agents
Jiban K. Chakrabarti, Richard J. Eggleton, Peter T. Gallagher, Janette Harvey, Terence A. Hicks, E. Ann Kitchen, and Colin W. Smith
pp 1663 - 1668; DOI:
10.1021/jm00392a024
PDF
Synthesis and evaluation of melphalan-containing N,N-dialkylenkephalin analogs as irreversible antagonists of the .delta. opioid receptor
Jane A. Lovett and Philip S. Portoghese
pp 1668 - 1674; DOI:
10.1021/jm00392a025
PDF
Carbonylacrylic derivatives as potential antimicrobial agents. Correlations between activity and reactivity toward cysteine
Alma Dal Pozzo, Maurizio Acquasaliente, Giovanni Donzelli, Paolo De Maria, and M. Christina Nicoli
pp 1674 - 1677; DOI:
10.1021/jm00392a026
PDF
Toward a rationalization of the sensitizing potency of substituted p-benzoquinones. Reaction of nucleophiles with p-benzoquinones
D. Cremer, B. M. Hausen, and H. W. Schmalle
pp 1678 - 1681; DOI:
10.1021/jm00392a027
PDF
Structural modification study of mitoxantrone (DHAQ). Chloro-substituted mono- and bis[(aminoalkyl)amino]anthraquinones
Robert K.-Y. Zee-Cheng, Abraham E. Mathew, Pei-Ling Xu, Raymond V. Northcutt, and C. C. Cheng
pp 1682 - 1686; DOI:
10.1021/jm00392a028
PDF
Improved synthesis and antitumor activity of 1-deazaadenosine
Gloria Cristalli, Palmarisa Franchetti, Mario Grifantini, Sauro Vittori, Teresa Bordoni, and Cristina Geroni
pp 1686 - 1688; DOI:
10.1021/jm00392a029
PDF
Anticoagulant peptides. Nature of the interaction of the C-terminal region of hirudin with a noncatalytic binding site on thrombin
John L. Krstenansky, Thomas J. Owen, Mark T. Yates, and Simon J. T. Mao
pp 1688 - 1691; DOI:
10.1021/jm00392a030
PDF
Book Reviews

pp 1691 - 1704; DOI:
10.1021/jm00392a600
PDF

Issue 10


Inactivation of thymidylate synthase at an alternate high-affinity binding site
Laman A. Al-Razzak, Douglas Schwepler, Charles J. Decedue, and Mathias P. Mertes
pp 1705 - 1706; DOI:
10.1021/jm00393a001
PDF
Diketopiperazines as a new class of platelet-activating factor inhibitors
Norihiko Shimazaki, Ichiro Shima, Keiji Hemmi, and Masashi Hashimoto
pp 1706 - 1709; DOI:
10.1021/jm00393a002
PDF
N6-(2,2-diphenylethyl)adenosine, a novel adenosine receptor agonist with antipsychotic-like activity
Alexander J. Bridges, Walter H. Moos, Deedee L. Szotek, Bharat K. Trivedi, James A. Bristol, Thomas G. Heffner, Robert F. Bruns, and David A. Downs
pp 1709 - 1711; DOI:
10.1021/jm00393a003
PDF
Enantiomers of 1-ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid: preparation and biological activity
Townley P. Culbertson, John M. Domagala, Jeffery B. Nichols, Stephen Priebe, and Richard W. Skeean
pp 1711 - 1715; DOI:
10.1021/jm00393a004
PDF
Synthesis and biological properties of N3-(4-methoxyfumaroyl)-L-2,3-diaminopropanoic acid dipeptides. A novel group of antimicrobial agents
Ryszard Andruszkiewicz, Henryk Chmara, Slawomir Milewski, and Edward Borowski
pp 1715 - 1719; DOI:
10.1021/jm00393a005
PDF
Synthesis of angiotensin II antagonists with variations in position 5
Olga Nyeki, Katalin S. Szalay, Lajos Kisfaludy, Egon Karpati, Laszlo Szporny, Gabor B. Makara, and Bertalan Varga
pp 1719 - 1724; DOI:
10.1021/jm00393a006
PDF
Cardiotonic agents. 6. Synthesis and inotropic activity of 2,4-dihydro-5-[4-(1H-imidazol-1-yl)phenyl]-3H-pyrazol-3-ones: ring-contracted analogs of imazodan (CI-914)
Ila Sircar, Glenn C. Morrison, Sandra E. Burke, Richard Skeean, and Ronald E. Weishaar
pp 1724 - 1728; DOI:
10.1021/jm00393a007
PDF
Renin inhibitors. Dipeptide analogs of angiotensinogen incorporating transition-state, nonpeptidic replacements at the scissile bond
Giorgio Bolis, Anthony K. L. Fung, Jonathan Greer, Hollis D. Kleinert, Patrick A. Marcotte, Thomas J. Perun, Jacob J. Plattner, and Herman H. Stein
pp 1729 - 1737; DOI:
10.1021/jm00393a008
PDF
1,3-Diarylpyrazolo[4,5-c]- and -[5,4-c]quinolin-4-ones. 4. Synthesis and specific inhibition of benzodiazepine receptor binding
Giovanna Palazzino, Lucia Cecchi, Fabrizio Melani, Vittoria Colotta, Guido Filacchioni, Claudia Martini, and Antonio Lucacchini
pp 1737 - 1742; DOI:
10.1021/jm00393a009
PDF
Discovery and anticonvulsant activity of the potent metabolic inhibitor 4-amino-N-(2,6-dimethylphenyl)-3,5-dimethylbenzamide
David W. Robertson, J. David Leander, Ron Lawson, E. E. Beedle, C. Randall Clark, Brian D. Potts, and C. John Parli
pp 1742 - 1746; DOI:
10.1021/jm00393a010
PDF
Synthesis of potential anticancer agents: imidazo[4,5-c]pyridines and imidazo[4,5-b]pyridines
Carroll Temple, Jerry D. Rose, Robert N. Comber, and Gregory A. Rener
pp 1746 - 1751; DOI:
10.1021/jm00393a011
PDF
In vivo antitumor activity of 6-benzyl-1,3-benzodioxole derivatives against the P388, L1210, B16, and M5076 murine models
Leonard Jurd, V. L. Narayanan, and Kenneth D. Paull
pp 1752 - 1756; DOI:
10.1021/jm00393a012
PDF
Synthesis and biological studies of iodinated (127/125I) derivatives of rhodamine 123
Berma M. Kinsey, Amin I. Kassis, Fahed Fayad, Warren W. Layne, and S. James Adelstein
pp 1757 - 1761; DOI:
10.1021/jm00393a013
PDF
Synthesis, conformational considerations, and estrogen receptor binding of diastereoisomers and enantiomers of 1-[4-[2-(dimethylamino)ethoxy]phenyl]-1,2-diphenylbutane (dihydrotamoxifen)
Raymond McCague and Guy Leclercq
pp 1761 - 1767; DOI:
10.1021/jm00393a014
PDF
Synthesis and antineoplastic activity of 1a-formyl and 1a-thioformyl derivatives of mitomycin C and 2-methylaziridine
Paul L. Fishbein and Harold Kohn
pp 1767 - 1773; DOI:
10.1021/jm00393a015
PDF
Plant antitumor agents. 25. Total synthesis and antileukemic activity of ring A substituted camptothecin analogs. Structure-activity correlations
Mansukh C. Wani, Allan W. Nicholas, Govindarajan Manikumar, and Monroe E. Wall
pp 1774 - 1779; DOI:
10.1021/jm00393a016
PDF
Synthesis and structure-activity relationships of 1-substituted 4-(1,2-diphenylethyl)piperazine derivatives having narcotic agonist and antagonist activity
Kagayaki Natsuka, Hideo Nakamura, Yoshinori Nishikawa, Toshiyuki Negoro, Hitoshi Uno, and Haruki Nishimura
pp 1779 - 1787; DOI:
10.1021/jm00393a017
PDF
Studies on histamine H2 receptor antagonists. 2. Synthesis and pharmacological activities of N-sulfamoyl and N-sulfonyl amidine derivatives
Isao Yanagisawa, Yasufumi Hirata, and Yoshio Ishii
pp 1787 - 1793; DOI:
10.1021/jm00393a018
PDF
2,4-Diamino-6,7-dimethoxyquinazolines. 3. 2-(4-heterocyclylpiperazin-1-yl) derivatives as .alpha.1-adrenoceptor antagonists and antihypertensive agents
Simon F. Campbell and Rhona M. Plews
pp 1794 - 1798; DOI:
10.1021/jm00393a019
PDF
Effects of [(N-alkyl-1,3-dioxo-1H,3H-isoindolin-5-yl)oxy]alkanoic acids, [(N-alkyl-1-oxo-1H,3H-isoindolin-5-yl)oxy]butanoic acids, and related derivatives on chloride influx in primary astroglial cultures
Steven D. Wyrick, Forrest T. Smith, W. Evans Kemp, and Anne A. Grippo
pp 1798 - 1806; DOI:
10.1021/jm00393a020
PDF
1,3-Dialkyl-4-(iminoarylmethyl)-1H-pyrazol-5-ols. A series of novel potential antipsychotic agents
Lawrence D. Wise, Donald E. Butler, Horace A. DeWald, David M. Lustgarten, Ian C. Pattison, Dieter N. Schweiss, Linda L. Coughenour, David A. Downs, Thomas G. Heffner, and Thomas A. Pugsley
pp 1807 - 1812; DOI:
10.1021/jm00393a021
PDF
Thromboxane synthase inhibitors. Synthesis and pharmacological activity of (R)-, (S)-, and (.+-.)-2,2-dimethyl-6-[2-(1H-imidazol-1-yl)-1-[[(4-methoxyphenyl)methoxy]methyl]ethoxy]hexanoic acids
Paul W. Manley, David P. Tuffin, Nigel M. Allanson, Philip E. Buckle, Nagin Lad, Steve M. F. Lai, David O. Lunt, Roderick A. Porter, and Patricia J. Wade
pp 1812 - 1818; DOI:
10.1021/jm00393a022
PDF
Antipsychotic activity of substituted .gamma.-carbolines
Magid Abou-Gharbia, Usha R. Patel, Michael B. Webb, John A. Moyer, Terrance H. Andree, and Eric A. Muth
pp 1818 - 1823; DOI:
10.1021/jm00393a023
PDF
6-Methylergoline-8-carboxylic acid esters as serotonin antagonists: N1-substituent effects on 5HT2 receptor affinity
Gifford Marzoni, William L. Garbrecht, Pawel Fludzinski, and Marlene L. Cohen
pp 1823 - 1826; DOI:
10.1021/jm00393a024
PDF
C1- and C3-methyl-substituted derivatives of 7-hydroxy-2-(di-n-propylamino)tetralin: activities at central dopamine receptors
Anette M. Johansson, J. Lars G. Nilsson, Anders Karlen, Uli Hacksell, Domingo Sanchez, Kjell Svensson, Stephan Hjorth, Arvid Carlsson, Staffan Sundell, and Lennart Kenne
pp 1827 - 1837; DOI:
10.1021/jm00393a025
PDF
.alpha.,.alpha.-Difluoro-.beta.-aminodeoxystatine-containing renin-inhibitory peptides
Suvit Thaisrivongs, Heinrich J. Schostarez, Donald T. Pals, and Steve R. Turner
pp 1837 - 1842; DOI:
10.1021/jm00393a026
PDF
Conformational analysis of antineoplastic antifolates: the crystal structure of trimetrexate and the aminopterine derivative 4-[N-[(2,4-diamino-6-pteridinyl)methyl]amino]benzoic acid
Paul A. Sutton and Vivian Cody
pp 1843 - 1848; DOI:
10.1021/jm00393a027
PDF
Isothiourea derivatives of 6-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole with broad-spectrum anthelmintic activity
Malcolm D. Brewer, Roderick J. J. Dorgan, Brian R. Manger, Patrick Mamalis, and Richard A. B. Webster
pp 1848 - 1853; DOI:
10.1021/jm00393a028
PDF
Renin inhibitors. Statine-containing tetrapeptides with varied hydrophobic carboxy termini
Mark G. Bock, Robert M. DiPardo, Ben E. Evans, Kenneth E. Rittle, Joshua Boger, Martin Poe, Bruce I. LaMont, Robert J. Lynch, Edgar H. Ulm, and et al.
pp 1853 - 1857; DOI:
10.1021/jm00393a029
PDF
Total synthesis and biological evaluation of structural analogs of compactin and dihydromevinolin
Clayton H. Heathcock, Cheri R. Hadley, Terry Rosen, Peter D. Theisen, and Scott J. Hecker
pp 1858 - 1873; DOI:
10.1021/jm00393a030
PDF
Quantitative structure-activity relationships of the bitter thresholds of amino acids, peptides, and their derivatives
Masaaki Asao, Hajime Iwamura, Miki Akamatsu, and Toshio Fujita
pp 1873 - 1879; DOI:
10.1021/jm00393a031
PDF
Synthesis of some [N-(2-haloalkyl)amino]tetralin derivatives as potential irreversible labels for bovine anterior pituitary D2 dopamine receptors
A. W. Hall, R. J. K. Taylor, S. H. Simmonds, and P. G. Strange
pp 1879 - 1887; DOI:
10.1021/jm00393a032
PDF
Evaluation of isomeric 4-(chlorohydroxyphenyl)-1,2,3,4-tetrahydroisoquinolines as dopamine D-1 antagonists
Robert M. Riggs, David E. Nichols, Mark M. Foreman, and Lewis L. Truex
pp 1887 - 1891; DOI:
10.1021/jm00393a033
PDF
Prodrugs of L-cysteine as protective agents against acetaminophen-induced hepatotoxicity. 2-(Polyhydroxyalkyl)- and 2-(polyacetoxyalkyl)thiazolidine-4(R)-carboxylic acids
Jeanette C. Roberts, Herbert T. Nagasawa, Richard T. Zera, Robert F. Fricke, and David J. W. Goon
pp 1891 - 1896; DOI:
10.1021/jm00393a034
PDF
Synthesis and antitumor activity of tropolone derivatives. 6. Structure-activity relationships of antitumor-active tropolone and 8-hydroxyquinoline derivatives
Masatoshi Yamato, Kuniko Hashigaki, Yoshiko Yasumoto, Junko Sakai, Richard F. Luduena, Asok Banerjee, Shigeru Tsukagoshi, Tazuko Tashiro, and Takashi Tsuruo
pp 1897 - 1900; DOI:
10.1021/jm00393a035
PDF
Novel irreversible ligands specific for "peripheral" type benzodiazepine receptors: (.+-.)-, (+)- and (-)-1-(2-chlorophenyl)-N-(1-methylpropyl)-N-(2-isothiocyanatoethyl)-3-isoquinolinecarboxamide and 1-(2-isothiocyanatoethyl)-7-chloro-1,3-dihydro-5-(4-chlorophenyl)-2H-1,4-benzodiazepin-2-one
Amy Hauck Newman, Hartmut W. M. Lueddens, Phil Skolnick, and Kenner C. Rice
pp 1901 - 1905; DOI:
10.1021/jm00393a036
PDF
Combined analgesic/neuroleptic activity in N-butyrophenone prodine-like compounds
M. A. Iorio, T. Paszkowska Reymer, and V. Frigeni
pp 1906 - 1910; DOI:
10.1021/jm00393a037
PDF
Effect of reductive alkylation of lysine in positions 6 and/or 8 on the histamine-releasing activity of luteinizing hormone-releasing hormone antagonists
Simon J. Hocart, Mary V. Nekola, and David H. Coy
pp 1910 - 1914; DOI:
10.1021/jm00393a038
PDF
Effect of .beta.-alkyl substitution on D-1 dopamine agonist activity: absolute configuration of .beta.-methyldopamine
Robert M. Riggs, Ann T. McKenzie, Stephen R. Byrn, David E. Nichols, Mark M. Foreman, and Lewis L. Truex
pp 1914 - 1918; DOI:
10.1021/jm00393a039
PDF
Streptonigrin and lavendamycin partial structures. Probes for the minimum, potent pharmacophore of streptonigrin, lavendamycin, and synthetic quinoline-5,8-diones
Dale L. Boger, Masami Yasuda, Lester A. Mitscher, Steven D. Drake, Paul A. Kitos, and Sandra Collins Thompson
pp 1918 - 1928; DOI:
10.1021/jm00393a040
PDF
The dopaminergic moiety of the ergots. A controversial topic studied with molecular mechanics
Hakaan Wikstroem, Jenn Huei Lii, and Norman L. Allinger
pp 1928 - 1934; DOI:
10.1021/jm00393a041
PDF
Molecular requirements of the recognition site of the cholinergic receptor. 24. Resolution, absolute configuration, and cholinergic enantioselectivity of (-)- and (+)-c-2-methyl-r-5-[(dimethylamino)methyl]-1,3-oxathiolane t-3-oxide methiodide and related sulfones
E. Teodori, F. Gualtieri, P. Angeli, L. Brasili, and M. Giannella
pp 1934 - 1938; DOI:
10.1021/jm00393a042
PDF
Additions and Corrections - In Search of the Digitalis Replacement
P.W. Erhardt
pp 1938 - 1938; DOI:
10.1021/jm00393a600
PDF
Book Reviews

pp 1939 - 1940; DOI:
10.1021/jm00393a601
PDF

Issue 11


Macrolides with gastrointestinal motor stimulating activity
Satoshi Omura, Kazuo Tsuzuki, Toshiaki Sunazuka, Shogo Marui, Hajime Toyoda, Nobuhiro Inatomi, and Zen Itoh
pp 1941 - 1943; DOI:
10.1021/jm00394a001
PDF
Antimalarial activity of 2-(substituted amino)-4,6-bis(trichloromethyl)-1,3,5-triazines and N-(chlorophenyl)-N'-[4-(substituted amino)-6-(trichloromethyl)-1,3,5-triazin-2-yl]guanidines
Leslie M. Werbel, Edward F. Elslager, Carolyn Hess, and Marland P. Hutt
pp 1943 - 1948; DOI:
10.1021/jm00394a002
PDF
Stereospecificity in allergic contact dermatitis to simple substituted methylene lactones derivatives
Henri Mattes, Kaoru Hamada, and Claude Benezra
pp 1948 - 1951; DOI:
10.1021/jm00394a003
PDF
Synthesis and gastrointestinal pharmacology of the 4-fluoro analog of enisoprost
Paul W. Collins, Steven W. Kramer, and Gary W. Gullikson
pp 1952 - 1955; DOI:
10.1021/jm00394a004
PDF
Cardiotonic agents. 7. Inhibition of separated forms of cyclic nucleotide phosphodiesterase from guinea pig cardiac muscle by 4,5-dihydro-6-[4-(1H-imidazol-1-yl)phenyl]-3(2H)-pyridazinones and related compounds. Structure-activity relationships and correlation with in vivo positive inotropic activity
Ila Sircar, Ronald E. Weishaar, Dianne Kobylarz, Walter H. Moos, and James A. Bristol
pp 1955 - 1962; DOI:
10.1021/jm00394a005
PDF
Cardiotonic agents. 8. Selective inhibitors of adenosine 3',5'-cyclic phosphate phosphodiesterase III. Elaboration of a five-point model for positive inotropic activity
Walter H. Moos, Christine C. Humblet, Ila Sircar, Christopher Rithner, Ronald E. Weishaar, James A. Bristol, and Andrew T. McPhail
pp 1963 - 1972; DOI:
10.1021/jm00394a006
PDF
Design, synthesis, and testing of potential antisickling agents. 10. 2,2-Dimethylchroman-6-ylalkanoic acids
Majekodunmi O. Fatope and Donald J. Abraham
pp 1973 - 1977; DOI:
10.1021/jm00394a007
PDF
Renin inhibitors based on novel dipeptide analogs. Incorporation of the dehydrohydroxyethylene isostere at the scissile bond
Dale J. Kempf, Ed De Lara, Herman H. Stein, Jerome Cohen, and Jacob J. Plattner
pp 1978 - 1983; DOI:
10.1021/jm00394a008
PDF
Angiotensin-converting enzyme inhibitors. Perhydro-1,4-thiazepin-5-one derivatives
Hiroaki Yanagisawa, Sadao Ishihara, Akiko Ando, Takuro Kanazaki, Shuichi Miyamoto, Hiroyuki Koike, Yasuteru Iijima, Kiyoshi Oizumi, Yoichi Matsushita, and Tadashi Hata
pp 1984 - 1991; DOI:
10.1021/jm00394a009
PDF
Hybrid bivalent ligands with opiate and enkephalin pharmacophores
Philip S. Portoghese, D. L. Larson, G. Ronsisvalle, P. W. Schiller, Nguyen Thi Mai Dung, C. Lemieux, and A. E. Takemori
pp 1991 - 1994; DOI:
10.1021/jm00394a010
PDF
Synthesis and antiinflammatory activities of 3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones
H. Ikuta, H. Shirota, S. Kobayashi, Y. Yamagishi, K. Yamada, I. Yamatsu, and K. Katayama
pp 1995 - 1998; DOI:
10.1021/jm00394a011
PDF
2,4-Diamino-5-benzylpyrimidines as antibacterial agents. 8. The 3,4,5-triethyl isostere of trimethoprim. A study of specificity
Barbara Roth and Edward Aig
pp 1998 - 2004; DOI:
10.1021/jm00394a012
PDF
Antitumor agents. 89. Psychorubrin, a new cytotoxic naphthoquinone from Psychotria rubra and its structure-activity relationships
Toshimitsu Hayashi, Forrest T. Smith, and Kuo Hsiung Lee
pp 2005 - 2008; DOI:
10.1021/jm00394a013
PDF
Carbamate ester derivatives as potential prodrugs of the presynaptic dopamine autoreceptor agonist (-)-3-(3-hydroxyphenyl)-N-propylpiperidine
Seth Olov Thorberg, Stefan Berg, Jan Lundstroem, Bodil Pettersson, Agneta Wijkstroem, Domingo Sanchez, Per Lindberg, and J. Lars G. Nilsson
pp 2008 - 2012; DOI:
10.1021/jm00394a014
PDF
Facile synthesis of 2-[(3-aminopropyl)thio]adenosine 5'-diphosphate: a key intermediate for the synthesis of molecular probes of adenosine 5'-diphosphate function
John R. Jefferson, John B. Hunt, and G. A. Jamieson
pp 2013 - 2016; DOI:
10.1021/jm00394a015
PDF
Nitrogen-bridged conformationally constrained etorphine analogs. Synthesis and biological evaluation
Peter J. Maurer and Henry Rapoport
pp 2016 - 2026; DOI:
10.1021/jm00394a016
PDF
Synthesis and antiviral activity of carbocyclic analogs of xylofuranosides of 2-amino-6-substituted-purines and 2-amino-6-substituted-8-azapurines
Robert Vince, Rajesh H. Turakhia, William M. Shannon, and Gussie Arnett
pp 2026 - 2030; DOI:
10.1021/jm00394a017
PDF
Antiulcer agents. 2. Gastric antisecretory, cytoprotective, and metabolic properties of substituted imidazo[1,2-a]pyridines and analogs
James J. Kaminski, James M. Hilbert, B. N. Pramanik, Daniel M. Solomon, David J. Conn, Razia K. Rizvi, Arthur J. Elliott, Henry Guzik, Raymond G. Lovey, and et al.
pp 2031 - 2046; DOI:
10.1021/jm00394a018
PDF
Antiulcer agents. 3. Structure-activity-toxicity relationships of substituted imidazo[1,2-a]pyridines and a related imidazo[1,2-a]pyrazine
James J. Kaminski, D. G. Perkins, J. D. Frantz, Daniel M. Solomon, Arthur J. Elliott, P. J. S. Chiu, and James F. Long
pp 2047 - 2051; DOI:
10.1021/jm00394a019
PDF
Metabolic synthesis of arylacetic acid antiinflammatory drugs from arylhexenoic acids. 2. Indomethacin
J. W. Gillard and P. Belanger
pp 2051 - 2058; DOI:
10.1021/jm00394a020
PDF
Synthesis and physicochemical properties of thiadiazolo[3,2-a]pyrimidinesulfonamides and thiadiazolo[3,2-a]triazinesulfonamides as candidates for topically effective carbonic anhydrase inhibitors
Alan R. Katritzky, Kenneth C. Caster, Thomas H. Maren, Curtis W. Conroy, and Amir Bar-Ilan
pp 2058 - 2062; DOI:
10.1021/jm00394a021
PDF
Design and synthesis of phosphonate inhibitors of glutamine synthetase
G. King Farrington, Alok Kumar, and Frederick C. Wedler
pp 2062 - 2067; DOI:
10.1021/jm00394a022
PDF
A 500-MHz proton nuclear magnetic resonance study of .mu. opioid peptides in a simulated receptor environment
M. A. Castiglione-Morelli, F. Lelj, A. Pastore, S. Salvadori, T. Tancredi, R. Tomatis, E. Trivellone, and P. A. Temussi
pp 2067 - 2073; DOI:
10.1021/jm00394a023
PDF
Modulation of the antitumor activity by methyl substitutions in the series of 7H-pyridocarbazole monomers and dimers
P. Leon, C. Garbay-Jaureguiberry, M. C. Barsi, J. B. Le Pecq, and Bernard P. Roques
pp 2074 - 2080; DOI:
10.1021/jm00394a024
PDF
Potential antitumor agents. 53. Synthesis, DNA binding properties, and biological activity of perimidines designed as minimal DNA-intercalating agents
John M. Herbert, Paul D. Woodgate, and William A. Denny
pp 2081 - 2086; DOI:
10.1021/jm00394a025
PDF
Phenylephrine derivatives as leukotriene D4 antagonists
John H. Musser, Dennis M. Kubrak, Reinhold H. W. Bender, Anthony F. Kreft, Susan T. Nielsen, Allan M. Lefer, Joseph Chang, Alan J. Lewis, and James M. Hand
pp 2087 - 2093; DOI:
10.1021/jm00394a026
PDF
Structure-activity relationships of cyclic opioid peptide analogs containing a phenylalanine residue in the 3-position
Peter W. Schiller, Louise A. Maziak, Brian C. Wilkes, Carole Lemieux, and Nguyen Thi Mai Dung
pp 2094 - 2099; DOI:
10.1021/jm00394a027
PDF
2-Phenylpyrroles as conformationally restricted benzamide analogs. A new class of potential antipsychotics. 1
Ineke Van Wijngaarden, Chris G. Kruse, Roelof Van Hes, Jan A. M. Van der Heyden, and Martin T. M. Tulp
pp 2099 - 2104; DOI:
10.1021/jm00394a028
PDF
(+)-cis-8-Hydroxy-1-methyl-2-(di-n-propylamino)tetralin: a potent and highly stereoselective 5-hydroxytryptamine receptor agonist
Lars Erik Arvidsson, Anette M. Johansson, Uli Hacksell, J. Lars G. Nilsson, K. Svewnsson, Stephan Hjorth, Tor Magnusson, Arvid Carlsson, Bengt Andersson, and Hakan Wikstroem
pp 2105 - 2109; DOI:
10.1021/jm00394a029
PDF
Vinylogous carbinolamine tumor inhibitors. 21. Synthesis, chemical reactivity, and antileukemic activity of 5-substituted 6,7-bis(hydroxymethyl)pyrrolo[1,2-c]thiazole biscarbamates and the corresponding sulfoxides and sulfones
Wayne K. Anderson and Robert H. Mach
pp 2109 - 2115; DOI:
10.1021/jm00394a030
PDF
Congener derivatives and conjugates of histamine: synthesis and tissue and receptor selectivity of the derivatives
M. M. Khan, K. L. Melmon, D. Marr-Leisy, M. S. Verlander, M. Egli, S. Lok, and M. Goodman
pp 2115 - 2120; DOI:
10.1021/jm00394a031
PDF
In vivo characterization of hydroxamic acid inhibitors of 5-lipoxygenase
James B. Summers, Bruce P. Gunn, Hormoz Mazdiyasni, Andrew M. Goetze, Patrick R. Young, Jennifer B. Bouska, Richard D. Dyer, Dee W. Brooks, and George W. Carter
pp 2121 - 2126; DOI:
10.1021/jm00394a032
PDF
.alpha.-Melanotropin: the minimal active sequence in the frog skin bioassay
Victor J. Hruby, Brian C. Wilkes, Mac E. Hadley, Fahad Al-Obeidi, Tomi K. Sawyer, Douglas J. Staples, Ann E. DeVaux, Orin Dym, Ana Maria de L. Castrucci, and et al.
pp 2126 - 2130; DOI:
10.1021/jm00394a033
PDF
Synthesis and anti-HIV activity of various 2'- and 3'-substituted 2',3'-dideoxyadenosines: a structure-activity analysis
P. Herdewijn, R. Pauwels, M. Baba, J. Balzarini, and E. De Clercq
pp 2131 - 2137; DOI:
10.1021/jm00394a034
PDF
Optimization and in vivo evaluations of a series of small, potent, and specific renin inhibitors containing a novel Leu-Val replacement
Joseph F. Dellaria, Robert G. Maki, Barbara A. Bopp, Jerome Cohen, Hollis D. Kleinert, Jay R. Luly, Ilmar Merits, Jacob J. Plattner, and Herman H. Stein
pp 2137 - 2144; DOI:
10.1021/jm00394a035
PDF
3-Pyrroline N-oxide bis(carbamate) tumor inhibitors as analogs of indicine N-oxide
Wayne K. Anderson and Arnold S. Milowsky
pp 2144 - 2147; DOI:
10.1021/jm00394a036
PDF
Antimalarial activity of new water-soluble dihydroartemisinin derivatives
Ai Jeng Lin, Daniel L. Klayman, and Wilbur K. Milhous
pp 2147 - 2150; DOI:
10.1021/jm00394a037
PDF
Antimalarial drugs. 63. Synthesis and antimalarial and antitumor effects of 2-amino-4-(hydrazino and hydroxyamino)-6-[(aryl)thio]quinazolines
Leslie M. Werbel and Margaret J. Degnan
pp 2151 - 2154; DOI:
10.1021/jm00394a038
PDF
Acetylenic nucleosides. 4. 1-(.beta.-D-Arabinofuranosyl)-5-ethynylcytosine. Improved synthesis and evaluation of biochemical and antiviral properties
Miroslav Bobek, I. Kavai, R. A. Sharma, S. Grill, G. Dutschman, and Y. C. Cheng
pp 2154 - 2157; DOI:
10.1021/jm00394a039
PDF
1,2-Bis(sulfonyl)hydrazines. 3. Effects of structural modification on antineoplastic activity
Krishnamurthy Shyam, Robert T. Hrubiec, Ryosuke Furubayashi, Lucille A. Cosby, and Alan C. Sartorelli
pp 2157 - 2161; DOI:
10.1021/jm00394a040
PDF
Book Reviews

pp 2162 - 2162; DOI:
10.1021/jm00394a600
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Issue 12


Synthesis of antimicrobial agents. 1. Syntheses and antibacterial activities of 7-(azole substituted)quinolones
Toshio Uno, Masanori Takamatsu, Yoshimasa Inoue, Yoshihiro Kawahata, Koji Iuchi, and Goro Tsukamoto
pp 2163 - 2169; DOI:
10.1021/jm00395a001
PDF
N-Substituted 1,2,3,4,4a,5,6,10b-octahydrobenzo[f]quinolines and 3-phenylpiperidines: effects on central dopamine and .sigma. receptors
Haakan Wikstroem, Bengt Andersson, Thomas Elebring, Kjell Svensson, Arvid Carlsson, and Brian Largent
pp 2169 - 2174; DOI:
10.1021/jm00395a002
PDF
Quantitative structure-activity relationships and eudismic analyses of the presynaptic dopaminergic activity and dopamine D2 and .sigma. receptor affinities of 3-(3-hydroxyphenyl)piperidines and octahydrobenzo[f]quinolines
Han Van de Waterbeemd, Nabil El Tayar, Bernard Testa, Haakan Wikstroem, and Brian Largent
pp 2175 - 2181; DOI:
10.1021/jm00395a003
PDF
Antitumor activity of bis(diphenylphosphino)alkanes, their gold(I) coordination complexes, and related compounds
Christopher K. Mirabelli, David T. Hill, Leo F. Faucette, Francis L. McCabe, Gerald R. Girard, Deborah B. Bryan, Blaine M. Sutton, Joan O. Leary Barus, Stanley T. Crooke, and Randall K. Johnson
pp 2181 - 2190; DOI:
10.1021/jm00395a004
PDF
Conformationally defined adrenergic agents. 10. Binding orientation of amphetamine and norfenfluramine analogs in the benzonorbornene and benzobicyclo[3.2.1]octane ring systems at the active site of phenylethanolamine N-methyltransferase (PNMT)
Gary L. Grunewald, Kimberly M. Markovich, and Daniel J. Sall
pp 2191 - 2208; DOI:
10.1021/jm00395a005
PDF
Inhibition of phenylethanolamine N-methyltransferase (PNMT) by aromatic hydroxy-substituted 1,2,3,4-tetrahydroisoquinolines. Further studies on the hydrophilic pocket of the aromatic ring binding region of the active site
Daniel J. Sall and Gary L. Grunewald
pp 2208 - 2216; DOI:
10.1021/jm00395a006
PDF
Novel 1H-benzimidazol-4-ols with potent 5-lipoxygenase inhibitory activity
Derek R. Buckle, Keith A. Foster, John F. Taylor, John M. Tedder, Veronica E. Thody, Richard A. B. Webster, Jose Bermudez, Roger E. Markwell, and Stephen A. Smith
pp 2216 - 2221; DOI:
10.1021/jm00395a007
PDF
Aryl diazo compounds and diazonium salts as potential irreversible probes of the GABA receptor
Marie Jeanne Bouchet, Alvaro Rendon, Camille G. Wermuth, Maurice Goeldner, and Christian Hirth
pp 2222 - 2227; DOI:
10.1021/jm00395a008
PDF
N-Substituted oxopyrimidines and nucleosides: structure-activity relationship for hypnotic activity as CNS depressant
Ikuo Yamamoto, Toshiyuki Kimura, Yuji Tateoka, Kazuhito Watanabe, and Ing Kang Ho
pp 2227 - 2231; DOI:
10.1021/jm00395a009
PDF
New antifilarial agents. 1. Epoxy sulfonamides and ethynesulfonamides
Marie Josephe Brienne, Daniel Varech, Martine Leclercq, Jean Jacques, Nathalie Radembino, Christine Dessalles, Georges Mahuzier, Chantal Gueyouche, Christian Bories, and et al.
pp 2232 - 2239; DOI:
10.1021/jm00395a010
PDF
Synthesis of new antiinflammatory steroidal 20-carboxamides: (20R)- and (20S)-21-(N-substituted amino)-11.beta.,17,20-trihydroxy-3,21-dioxo-1,4-pregnadiene
Hyun P. Kim, John Bird, Ann S. Heiman, George F. Hudson, Irach B. Taraporewala, and Henry J. Lee
pp 2239 - 2244; DOI:
10.1021/jm00395a011
PDF
C-Terminal deletions in antagonistic analogs of vasopressin that improve their specificities for antidiuretic (V2) and vasopressor (V1) receptors
Maurice Manning, Aleksandra Misicka, Aleksandra Olma, Wieslaw A. Klis, Krzysztof Bankowski, Eleonora Nawrocka, Marian Kruszynski, Aleksander Kolodziejczyk, Ling Ling Cheng, and et al.
pp 2245 - 2252; DOI:
10.1021/jm00395a012
PDF
Synthesis and 5-hydroxytryptamine antagonist activity of 2-[[2-(dimethylamino)ethyl]thio]-3-phenylquinoline and its analogs
Thomas P. Blackburn, Barry Cox, Allen J. Guildford, David J. Le Count, Derek N. Middlemiss, Robert J. Pearce, and Craig W. Thornber
pp 2252 - 2259; DOI:
10.1021/jm00395a013
PDF
Synthesis and cardiac electrophysiological activity of 2- and 3-[(substituted phenyl)alkyl]quinuclidines. Structure-activity relationships
Thomas K. Morgan, Randall Lis, Anthony J. Marisca, Thomas M. Argentieri, Mark E. Sullivan, and Samuel S. Wong
pp 2259 - 2269; DOI:
10.1021/jm00395a014
PDF
2-Oxo-1,8-naphthyridine-3-carboxylic acid derivatives with potent gastric antisecretory properties
Arthur A. Santilli, Anthony C. Scotese, Raymond F. Bauer, and Stanley C. Bell
pp 2270 - 2277; DOI:
10.1021/jm00395a015
PDF
Thromboxane synthetase inhibitors and antihypertensive agents. 4. N-[(1H-imidazol-1-yl)alkyl] derivatives of quinazoline-2,4(1H,3H)-diones, quinazolin-4(3H)-ones, and 1,2,3-benzotriazin-4(3H)-ones
William B. Wright, Andrew S. Tomcufcik, Peter S. Chan, Joseph W. Marsico, and Jeffery B. Press
pp 2277 - 2283; DOI:
10.1021/jm00395a016
PDF
Chiral DNA gyrase inhibitors. 2. Asymmetric synthesis and biological activity of the enantiomers of 9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid (ofloxacin)
Lester A. Mitscher, Padam N. Sharma, Daniel T. W. Chu, Linus L. Shen, and Andre G. Pernet
pp 2283 - 2286; DOI:
10.1021/jm00395a017
PDF
Renin inhibitors. Free-Wilson and correlation analysis of the inhibitory potency of a series of pepstatin analogs on plasma renin
Dino Nisato, Jean Wagnon, Georges Callet, Daniel Mettefeu, Jean Louis Assens, Claude Plouzane, Bernard Tonnerre, Vladimir Pliska, and Jean Luc Fauchere
pp 2287 - 2291; DOI:
10.1021/jm00395a018
PDF
Potent vasopressin antagonist modified at the carboxy-terminal tripeptide tail
Fadia El-Fehail Ali, Hsin Lan Chang, William F. Huffman, Grace Heckman, Lewis B. Kinter, Edwin F. Weidley, Richard Edwards, Dulcie Schmidt, Daryl Ashton-Shue, and Frans L. Stassen
pp 2291 - 2294; DOI:
10.1021/jm00395a019
PDF
[(6,7-Dichlorobenzo[b]thien-5-yl)oxy]acetic acids and 1,1-dioxides. 1. A structurally novel class of diuretics with hypotensive activity
Helen H. Ong, Steven R. Caldwell, James A. Profitt, John J. Tegeler, Marc N. Agnew, Jeffrey C. Wilker, Rudyard J. Ress, and Jan M. Kitzen
pp 2295 - 2303; DOI:
10.1021/jm00395a020
PDF
Synthesis and antiarrhythmic activity of novel 3-alkyl-1-[.omega.-[4-[(alkylsulfonyl)amino]phenyl]-.omega.-hydroxyalkyl]-1H-imidazolium salts and related compounds. 2
Randall Lis, David D. Davey, Thomas K. Morgan, William C. Lumma, Ronald A. Wohl, Vijay K. Jain, Chung Nan Wan, Thomas M. Argentieri, Mark E. Sullivan, and Elinor H. Cantor
pp 2303 - 2309; DOI:
10.1021/jm00395a021
PDF
Design and synthesis of peptide derivatives of a 3-deoxy-D-manno-2-octulosonic acid (KDO) analog as novel antibacterial agents acting upon lipopolysaccharide biosynthesis
Alf Claesson, Anita M. Jansson, Brian G. Pring, Stephen M. Hammond, and Bertil Ekstroem
pp 2309 - 2313; DOI:
10.1021/jm00395a022
PDF
Nucleosides. 146. 1-Methyl-5-(2-deoxy-2-fluoro-.beta.-D-arabinofuranosyl)uracil, the C-nucleoside isostere of the potent antiviral agent, 1-(2-deoxy-2-fluoro-.beta.-D-arabinofuranosyl)thymine (FMAU). Studies directed toward the synthesis of 2'-deoxy-2'-substituted arabino nucleosides. 6
Krzysztof W. Pankiewicz, Barbara Nawrot, Hakan Gadler, Pichard W. Price, and Kyoichi A. Watanabe
pp 2314 - 2316; DOI:
10.1021/jm00395a023
PDF
Plant antitumor agents. 28. Resolution of a key tricyclic synthon, 5'(RS)-1,5-dioxo-5'-hydroxy-2'H,5'H,6'H-6'-oxopyrano[3',4'-f].DELTA.6,8-tetrahydroindolizine: total synthesis and antitumor activity of 20(S)- and 20(R)-camptothecin
Mansukh C. Wani, Allan W. Nicholas, and Monroe E. Wall
pp 2317 - 2319; DOI:
10.1021/jm00395a024
PDF
Additions and Corrections-Synthesis and Antiviral Activity of Various 3'-Azido, 3'-Amino, 2',3'-Unsaturated, and 2',3'-Dideoxy Analogues of Pyrimidine Deoxyribonucleosides against Retroviruses
Tai-Shun Lin, Ming S. Chen, Colin McLaren, You-Song Gao, Ismail Ghazzouli, and William H. Prusoff
pp 2319 - 2319; DOI:
10.1021/jm00395a600
PDF
Book Reviews

pp 2320 - 2322; DOI:
10.1021/jm00395a601
PDF