Journal of Medicinal Chemistry
Volume 41, Issue 6 (March 12, 1998)
Copyright © 1998 American Chemical Society

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COMMUNICATIONS TO THE EDITOR

775-777

Acetamidine Lysine Derivative, N-(5(S)-amino-6,7-dihydroxyheptyl)ethanimidamide Dihydrochloride: A Highly Selective Inhibitor of Human Inducible Nitric Oxide Synthase E. Ann Hallinan, Sofya Tsymbalov, Patricia M. Finnegan, William M. Moore, Gina M. Jerome, Mark G. Currie, and Barnett S. Pitzele [Full Article - PDF]

ARTICLES

778-786

High-Affinity Aptamers Selectively Inhibit Human Nonpancreatic Secretory Phospholipase A2 (hnps-PLA2) Philippe Bridonneau, Ying-Fon Chang, Dan O'Connell, Stanley C. Gill, David W. Snyder, Lea Johnson, Theodore Goodson, Jr., David K. Herron, and David H. Parma [Full Article - PDF]

787-797

Dihydropyrancarboxamides Related to Zanamivir: A New Series of Inhibitors of Influenza Virus Sialidases. 1. Discovery, Synthesis, Biological Activity, and Structure-Activity Relationships of 4-Guanidino- and 4-Amino-4H-pyran-6-carboxamides Paul W. Smith, Steven L. Sollis, Peter D. Howes, Peter C. Cherry, Ian D. Starkey, Kevin N. Cobley, Helen Weston, Jan Scicinski, Andrew Merritt, Andrew Whittington, Paul Wyatt, Neil Taylor, Darren Green, Richard Bethell, Safia Madar, Robert J. Fenton, Peter J. Morley, Tony Pateman, and Alan Beresford [Full Article - PDF]

798-807

Dihydropyrancarboxamides Related to Zanamivir: A New Series of Inhibitors of Influenza Virus Sialidases. 2. Crystallographic and Molecular Modeling Study of Complexes of 4-Amino-4H-pyran-6-carboxamides and Sialidase from Influenza Virus Types A and B Neil R. Taylor, Anne Cleasby, Onkar Singh, Tadeusz Skarzynski, Alan J. Wonacott, Paul W. Smith, Steven L. Sollis, Peter D. Howes, Peter C. Cherry, Richard Bethell, Peter Colman, and Jose Varghese [Full Article - PDF]

808-820

(E)-3-(2-(N-Phenylcarbamoyl)vinyl)pyrrole-2-carboxylic Acid Derivatives. A Novel Class of Glycine Site Antagonists Cesarino Balsamini, Annalida Bedini, Giuseppe Diamantini, Gilberto Spadoni, Andrea Tontini, and Giorgio Tarzia , Romano Di Fabio, Aldo Feriani, Angelo Reggiani, Giovanna Tedesco, and Roberta Valigi [Full Article - PDF]

821-835

1,4-Cyclohexanecarboxylates: Potent and Selective Inhibitors of Phosophodiesterase 4 for the Treatment of Asthma Siegfried B. Christensen, Aimee Guider, Cornelia J. Forster, John G. Gleason, Paul E. Bender, Joseph M. Karpinski, Walter E. DeWolf, Jr., Mary S. Barnette, David C. Underwood, Don E. Griswold, Lenora B. Cieslinski, Miriam Burman, Steven Bochnowicz, Ruth R. Osborn, Carol D. Manning, Marilyn Grous, Leonard M. Hillegas, Joan O'Leary Bartus, M. Dominic Ryan, Drake S. Eggleston, R. Curtis Haltiwanger, and Theodore J. Torphy [Full Article - PDF]

836-852

Comparative Binding Energy Analysis of HIV-1 Protease Inhibitors: Incorporation of Solvent Effects and Validation as a Powerful Tool in Receptor-Based Drug Design Carlos Pérez, Manuel Pastor, Angel R. Ortiz, and Federico Gago [Full Article - PDF]

853-863

Molecular Properties and Pharmacokinetic Behavior of Cetirizine, a Zwitterionic H1-Receptor Antagonist Alessandra Pagliara, Bernard Testa, Pierre-Alain Carrupt, Pascale Jolliet, Christophe Morin, Didier Morin, Saïk Urien, Jean-Paul Tillement, and Jean-Pierre Rihoux [Full Article - PDF]

864-876

(-)-3-Substituted Ecgonine Methyl Esters as Inhibitors for Cocaine Binding and Dopamine Uptake Spencer F. Lieske, Biao Yang, Mohyee E. Eldefrawi, Alexander D. MacKerell, Jr., and Jeremy Wright [Full Article - PDF]

877-893

Inhibitors of Farnesyl Protein Transferase. 4-Amido, 4-Carbamoyl, and 4-Carboxamido Derivatives of 1-(8-Chloro-6,11-dihydro-5H-benzo[5,6]- cyclohepta[1,2-b]pyridin-11-yl)piperazine and 1-(3-Bromo-8-chloro-6,11- dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperazine Alan K. Mallams, Randall R. Rossman, Ronald J. Doll, Viyyoor M. Girijavallabhan, Ashit K. Ganguly, Joanne Petrin, Lynn Wang, Robert Patton, W. Robert Bishop, Donna M. Carr, Paul Kirschmeier, Joseph J. Catino, Matthew S. Bryant, Kwang-Jong Chen, Walter A. Korfmacher, Cymbelene Nardo, Shiyong Wang, Amin A. Nomeir, Chin-Chung Lin, Zujun Li, Jianping Chen, Suining Lee, Janet Dell, Philip Lipari, Michael Malkowski, Bodan Yaremko, Ivan King, and Ming Liu [Full Article - PDF]

894-901

Ethnobotanical-Directed Discovery of the Antihyperglycemic Properties of Cryptolepine: Its Isolation from Cryptolepis sanguinolenta, Synthesis, and in Vitro and in Vivo Activities Donald E. Bierer, Diana M. Fort, Christopher D. Mendez, Jian Luo, Patricia A. Imbach, Larisa G. Dubenko, Shivanand D. Jolad, R. Eric Gerber, Joane Litvak, Qing Lu, Pingsheng Zhang, Michael J. Reed, Nancy Waldeck, Reimar C. Bruening, Ben K. Noamesi, Richard F. Hector, Thomas J. Carlson, and Steven R. King [Full Article - PDF]

902-912

Novel 17-Azolyl Steroids, Potent Inhibitors of Human Cytochrome 17-Hydroxylase-C17,20-lyase (P45017): Potential Agents for the Treatment of Prostate Cancer Vincent C. O. Njar, Katsuya Kato, Ivo P. Nnane, Dmitry N. Grigoryev, Brian J. Long, and Angela M. H. Brodie [Full Article - PDF]

913-918

2,4-Diamino-6,7-dihydro-5H-cyclopenta[d]pyrimidine Analogues of Trimethoprim as Inhibitors of Pneumocystis carinii and Toxoplasma gondii Dihydrofolate Reductase Andre Rosowsky, Andrew T. Papoulis, and Sherry F. Queener [Full Article - PDF]

919-929

A Backbone-Cyclic, Receptor 5-Selective Somatostatin Analogue: Synthesis, Bioactivity, and Nuclear Magnetic Resonance Conformational Analysis Chaim Gilon, Martin Huenges, Barbara Mathä, Gary Gellerman, Vered Hornik, Michel Afargan, Oved Amitay, Ofer Ziv, Etty Feller, Asher Gamliel, Dvira Shohat, Mazal Wanger, Oded Arad, and Horst Kessler [Full Article - PDF]

930-939

Excitatory Amino Acid Receptor Ligands: Resolution, Absolute Stereochemistry, and Enantiopharmacology of 2-Amino-3-(4-butyl-3-hydroxyisoxazol-5-yl)propionic Acid Tommy N. Johansen, Bjarke Ebert, Hans Bräuner-Osborne, Michael Didriksen, Inge T. Christensen, Karina K. Sby, Ulf Madsen, Povl Krogsgaard-Larsen, and Lotte Brehm [Full Article - PDF]

940-951

Orally Active Antimalarial 3-Substituted Trioxanes: New Synthetic Methodology and Biological Evaluation Gary H. Posner, Jared N. Cumming, Soon-Hyung Woo, Poonsakdi Ploypradith, Suji Xie, and Theresa A. Shapiro [Full Article - PDF]

952-964

Design, Synthesis, Derivatization, and Structure-Activity Relationships of Simplified, Tricyclic, 1,2,4-Trioxane Alcohol Analogues of the Antimalarial Artemisinin Jared N. Cumming, Dasong Wang, Sheldon B. Park, Theresa A. Shapiro, and Gary H. Posner [Full Article - PDF]

965-972

Intensely Potent Doxorubicin Analogues: Structure-Activity Relationship David Farquhar, Abdallah Cherif, Elena Bakina, and J. Arly Nelson [Full Article - PDF]

973-980

Discovery of 1-(4-Fluorophenyl)-(3R)-[3-(4-fluorophenyl)-(3S)- hydroxypropyl]-(4S)-(4-hydroxyphenyl)-2-azetidinone (SCH 58235): A Designed, Potent, Orally Active Inhibitor of Cholesterol Absorption Stuart B. Rosenblum, Tram Huynh, Adriano Afonso, Harry R. Davis, Jr., Nathan Yumibe, John W. Clader, and Duane A. Burnett [Full Article - PDF]

981-987

Design, Synthesis, and Evaluation of the Multidrug Resistance-Reversing Activity of D-Glucose Mimetics of Hapalosin Tam Q. Dinh, Charles D. Smith, Xiaohui Du, and Robert W. Armstrong [Full Article - PDF]

988-995

Molecular Features Associated with Polyamine Modulation of NMDA Receptors Anita H. Lewin, Guobin Sun, Louise Fudala, Hernan Navarro, Li-Ming Zhou, Piotr Popik, Alexander Faynsteyn, and Phil Skolnick [Full Article - PDF]

NOTES

996-1000

Novel Biologically Active Nonpeptidic Inhibitors of MyristoylCoA:Protein N-Myristoyltransferase Balekudru Devadas, Sandra K. Freeman, Charles A. McWherter, Nandini S. Kishore, Jennifer K. Lodge, Emily Jackson-Machelski, Jeffrey I. Gordon, and James A. Sikorski [Full Article - PDF]

1001-1005

Synthesis and Pharmacological Evaluation of Ring-Methylated Derivatives of 3,4-(Methylenedioxy)amphetamine (MDA) Matthew A. Parker, Danuta Marona-Lewicka, Deborah Kurrasch, Alexander T. Shulgin, and David E. Nichols [Full Article - PDF]

ADDITIONS AND CORRECTIONS

1006-1006

Synthesis and Pharmacological Evaluation of N-(2,5-Disubstituted phenyl)-N'-(3-substituted phenyl)-N'-methylguanidines As N-Methyl-D-aspartate Receptor Ion-Channel Blockers Lain-Yen Hu, Junqing Guo, Sharad S. Magar, James B. Fischer, Kathleen J. Burke-Howie, and Graham J. Durant [Full Article - PDF]