Journal of Medicinal Chemistry: Volume 31, Issue 7 (ACS Publications)

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Table of Contents

July 1988

Volume 31, Issue 7

Pages 1269-1486

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Articles

Oxidants, oxidant drugs, and malaria

Jonathan L. Vennerstrom, John W. Eaton

pp 1269–1277

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a001

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(.+-.)-9-Amino-1,2,3,4-tetrahydroacridin-1-ol. A potential Alzheimer's disease therapeutic of low toxicity

Gregory M. Shutske, Frank A. Pierrat, Michael L. Cornfeldt, Mark R. Szewczak, Francis P. Huger, Gina M. Bores, Vahram Haroutunian, Kenneth L. Davis

pp 1278–1279

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a002

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Methyl mercapturate episulfonium ion: a model reactive metabolite of dihaloethanes

James G. Henkel, George S. Amato

pp 1279–1282

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a003

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N6-[2-(3,5-dimethoxyphenyl)-2-(2-methylphenyl)ethyl]adenosine and its uronamide derivatives. Novel adenosine agonists with both high affinity and high selectivity for the adenosine A2 receptor

Alexander J. Bridges, Robert F. Bruns, Daniel F. Ortwine, Steven R. Priebe, Deedee L. Szotek, Bharat K. Trivedi

pp 1282–1285

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a004

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Nonisomerizable analogs of (Z)- and (E)-4-hydroxytamoxifen. Synthesis and endocrinological properties of substituted diphenylbenzocycloheptenes

Raymond McCague, Guy Leclercq, V. Craig Jordan

pp 1285–1290

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a005

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Electrophysiologic and antiarrhythmic activities of 4-amino-N-[2-(diethylamino)ethyl]-3,5-dimethylbenzamide, a sterically hindered procainamide analog

David W. Robertson, E. E. Beedle, Harve Wilson, C. John Parli, Jeffrey K. Smallwood, Mitchell I. Steinberg

pp 1290–1295

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a006

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Synthesis and antitumor activity of quaternary ellipticine glycosides, a series of novel and highly active antitumor agents

Tadashi Honda, Mika Kato, Minako Inoue, Tetsuo Shimamoto, Keiyuu Shima, Toshihiro Nakanishi, Takako Yoshida, Teruhisa Noguchi

pp 1295–1305

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a007

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Dinucleotide analogs as inhibitors of thymidine kinase, thymidylate kinase and ribonucleotide reductase

Lawrence C. Davies, John A. Stock, S. Elaine Barrie, Rosanne M. Orr, Kenneth R. Harrap

pp 1305–1308

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a008

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Synthesis of the tumorigenic 3,4-dihydrodiol metabolites of dibenz[a,j]anthracene and 7,14-dimethyldibenz[a,j]anthracene

Ronald G. Harvey, Cecilia Cortez, Thomas W. Sawyer, John DiGiovanni

pp 1308–1312

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a009

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Heterocyclic muscarinic agonists. Synthesis and biological activity of some bicyclic sulfonium arecoline bioisosteres

Per Sauerberg, Erik Falch, Eddi Meier, Hanne L. Lemboel, Povl Krogsgaard-Larsen

pp 1312–1316

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a010

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2,3-Diarylindenes and 2,3-diarylindenones: synthesis, molecular structure, photochemistry, estrogen receptor binding affinity, and comparisons with related triarylethylenes

Gregory M. Anstead, Robert J. Altenbach, Scott R. Wilson, John A. Katzenellenbogen

pp 1316–1326

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a011

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Methotrexate analog. 32. Chain extension, .alpha.-carboxyl deletion, and .gamma. carboxyl replacement by sulfonate and phosphate. Effect on enzyme binding and cell-growth inhibition

Andre Rosowsky, Ronald A. Forsch, Richard G. Moran, William Kohler, James H. Freisheim

pp 1326–1331

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a012

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Methotrexate analogs. 33. N.delta.-Acyl-N.alpha.-(4-amino-4-deoxypteroyl)-L-ornithine derivatives. Synthesis and in vitro antitumor activity

Andre Rosowsky, Henry Bader, Carol A. Cucchi, Richard G. Moran, William Kohler, James H. Freisheim

pp 1332–1337

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a013

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Methotrexate analogs. 34. Replacement of the glutamate moiety in methotrexate and aminopterin by long-chain 2-aminoalkanedioic acids

Andre Rosowsky, Henry Bader, William Kohler, James H. Freisheim, Richard G. Moran

pp 1338–1344

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a014

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Stereochemical studies on medicinal agents. 31. Only one pharmacophore is required for the .kappa. opioid antagonist selectivity of norbinaltorphimine

P. S. Portoghese, H. Nagase, A. E. Takemori

pp 1344–1347

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a015

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7-Aminoquinolines. A novel class of agents active against herpes viruses

Mohamed Nasr, John C. Drach, Sandra H. Smith, Charles Shipman Jr., J. H. Burckhalter

pp 1347–1351

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a016

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Synthesis and antiviral activity of novel N-substituted derivatives of acyclovir

Jerzy Boryski, Bozenna Golankiewicz, Erik De Clercq

pp 1351–1355

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a017

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cis-4-Carboxy-6-(mercaptomethyl)-3,4,5,6-tetrahydropyrimidin-2(1H)-one, a potent inhibitor of mammalian dihydroorotase

Jerry L. Adams, Thomas D. Meek, Shau Ming Mong, Randall K. Johnson, Brian W. Metcalf

pp 1355–1359

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a018

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21-[18F]fluoro-16.alpha.-ethyl-19-norprogesterone. Synthesis and target tissue selective uptake of a progestin receptor-based radiotracer for positron emission tomography

Martin G. Pomper, John A. Katzenellenbogen, Michael J. Welch, James W. Brodack, Carla J. Mathias

pp 1360–1363

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a019

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Cardiotonic agents. Synthesis and inotropic activity of a series of isoquinolin-3-ol derivatives

Ramesh M. Kanojia, Jeffery B. Press, O. William Lever Jr., Louella Williams, James J. McNally, Alfonso J. Tobia, Robert Falotico, John B. Moore Jr.

pp 1363–1368

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a020

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Conformationally constrained renin inhibitory peptides: .gamma.-lactam-bridged dipeptide isostere as conformational restriction

Suvit Thaisrivongs, Donald T. Pals, Steve R. Turner, Lisa T. Kroll

pp 1369–1376

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a021

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Synthesis and renin inhibitory activity of angiotensinogen analogs having dehydrostatine, Lue.psi.[CH2S]Val, or Lue.psi.[CH2SO] Val at the Pt, P1' cleavage site

Clark W. Smith, Hossain H. Saneii, Tomi K. Sawyer, Donald T. Pals, Terrence A. Scahill, Bharat V. Kamdar, Judy A. Lawson

pp 1377–1382

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a022

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Polycyclic aryl- and heteroarylpiperazinyl imides as 5-HT1A receptor ligands and potential anxiolytic agents: synthesis and structure-activity relationship studies

Magid Abou-Gharbia, Usha R. Patel, Michael B. Webb, John A. Moyer, Terrance H. Andree, Eric A. Muth

pp 1382–1392

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a023

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Synthesis and dopamine agonist and antagonist effects of (R)-(-)- and (S)-(+)-11-hydroxy-N-n-propylnoraporphine

Yigong Gao, Rushi Zong, Alexander Campbell, Nora S. Kula, Ross J. Baldessarini, John L. Neumeyer

pp 1392–1396

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a024

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The hypothetical active site lattice. An approach to modelling active sites from data on inhibitor molecules

Arthur M. Doweyko

pp 1396–1406

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a025

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Synthesis and serotonin receptor affinities of a series of enantiomers of .alpha.-methyltryptamines: evidence for the binding conformation of tryptamines at serotonin 5-HT1B receptors

David E. Nichols, David H. Lloyd, Michael P. Johnson, Andrew J. Hoffman

pp 1406–1412

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a026

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The absolute configurations and pharmacological activities of the optical isomers of fluoxetine, a selective serotonin-uptake inhibitor

David W. Robertson, Joseph H. Krushinski, Ray W. Fuller, J. David Leander

pp 1412–1417

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a027

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Importance of the N-terminal domain of the type II angiotensin antagonist sarmesin for receptor blockade

John Matsoukas, Paul Cordopatis, Urania Belte, Mahesh H. Goghari, Renee C. Ganter, Kevin J. Franklin, Graham J. Moore

pp 1418–1421

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a028

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Synthesis and structure-activity relationships of 2-sulfonamido-1,3,4,6,7,11b.alpha.-hexahydro-2H-benzo[a]quinolizines as .alpha.2-adrenoceptor antagonists

Terence J. Ward, John F. White, Norman Lattimer, Keith F. Rhodes, Shobna Sharma, John F. Waterfall

pp 1421–1426

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a029

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Synthesis and antineoplastic activity of 5-aryl-2,3-dihydropyrrolo[2,1-b]thiazole-6,7-dimethanol 6,7-bis(isopropylcarbamates)

Iraj Lalezari, Edward L. Schwartz

pp 1427–1429

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a030

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Dopamine receptor modulation by conformationally constrained analogs of Pro-Leu-Gly-NH2

Kuo Long Yu, G. Rajakumar, Lalit K. Srivastava, Ram K. Mishra, Rodney L. Johnson

pp 1430–1436

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a031

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Synthetic aci-reductones. 3,4-Dihydroxy-2H-1-benzopyran-2-ones and their cis- and trans-4a,5,6,7,8,8a-hexahydro diastereomers. Antiaggregatory, antilipidemic, and redox properties compared to the 4-substituted 2-hydroxytetronic acids

Donald T. Witiak, Sung K. Kim, Ashok K. Tehim, Kent D. Sternitzke, Richard L. McCreery, Sung U. Kim, Dennis R. Feller, Karl J. Romstedt, Vaijinath S. Kamanna, Howard A. I. Newman

pp 1437–1445

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a032

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Predictive structure-activity relationships in a series of pyranoquinoline derivatives. A new primate model for the identification of antiallergic activity

Ken J. Gould, Carol N. Manners, David W. Payling, John L. Suschitzky, Edward Wells

pp 1445–1453

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a033

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4-Hydroxy-3-quinolinecarboxamides with antiarthritic and analgesic activities

Francois Clemence, Odile Le Martret, Francoise Delevallee, Josette Benzoni, Alain Jouanen, Simone Jouquey, Michel Mouren, Roger Deraedt

pp 1453–1462

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a034

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Affinity and selectivity of the optical isomers of 3-quinuclidinyl benzilate and related muscarinic antagonists

W. Janusz Rzeszotarski, Daniel W. McPherson, John W. Ferkany, William J. Kinnier, Lalita Noronha-Blob, Alicja Kirkien-Rzeszotarski

pp 1463–1466

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a035

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Preparation of 7-oxaaporphine derivatives and evaluation of their dopaminergic activity

Carlo Banzatti, Nicola Carfagna, Roberto Commisso, Franco Heidempergher, Lorenzo Pegrassi, Piero Melloni

pp 1466–1471

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a036

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Synthesis and estrogen receptor selectivity of 1,1-bis(4-hydroxyphenyl)-2-(p-halophenyl)ethylenes

Peter C. Ruenitz, Jerome R. Bagley, Nitin T. Nanavati

pp 1471–1475

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a037

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1-(2,3-Anhydro-.beta.-D-lyxofuranosyl)cytosine derivatives as potential inhibitors of the human immunodeficiency virus

Thomas R. Webb, Hiroaki Mitsuya, Samuel Broder

pp 1475–1479

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a038

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Syntheses and gastric acid antisecretory properties of the H2-receptor antagonist N-[3-[3-(1-piperidinylmethyl)phenoxy]propyl]thieno[3,4-d]isothiazol-3-amine 1,1-dioxide and related derivatives

Arthur A. Santilli, Anthony C. Scotese, Robert L. Morris, Guy A. Schiehser, Daniel M. Teller, Susan T. Nielsen, Donald P. Strike

pp 1480–1486

Publication Date: July 1988 ()

DOI: 10.1021/jm00402a039

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