Journal of Medicinal Chemistry
Volume 40, Issue 6 (March 14, 1997)
Copyright © 1997 American Chemical Society

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827-829

Simultaneous Pharmacokinetic Screening of a Mixture of Compounds in the Dog Using API LC/MS/MS Analysis for Increased Throughput Judd Berman, Kathy Halm, Kim Adkison, and Joel Shaffer [Full Article - PDF]

830-832

Design of Highly Potent Noncovalent Thrombin Inhibitors That Utilize a Novel Lipophilic Binding Pocket in the Thrombin Active Site Thomas J. Tucker, William C. Lumma, Anne M. Mulichak, Zhongguo Chen, Adel M. Naylor-Olsen, S. Dale Lewis, Robert Lucas, Roger M. Freidinger, and Lawrence C. Kuo [Full Article - PDF]

833-840

GRID/GOLPE 3D Quantitative Structure-Activity Relationship Study on a Set of Benzamides and Naphthamides, with Affinity for the Dopamine D3 Receptor Subtype Jonas Nilsson and Håkan Wikström , Age Smilde , Shelly Glase and Tom Pugsley , Gabriele Cruciani, Manuel Pastor, and Sergio Clementi [Full Article - PDF]

841-850

Substituted Indole-2-carboxylates as in Vivo Potent Antagonists Acting as the Strychnine-Insensitive Glycine Binding Site Romano Di Fabio, Anna M. Capelli, Nadia Conti, Alfredo Cugola, Daniele Donati, Aldo Feriani, Paola Gastaldi, Giovanni Gaviraghi, Cheryl T. Hewkin, Fabrizio Micheli, Andrea Missio, Manolo Mugnaini, Angelo Pecunioso, Anna M. Quaglia, Emiliangelo Ratti, Luciana Rossi, Giovanna Tedesco, David G. Trist, and Angelo Reggiani [Full Article - PDF]

851-857

3'-Chloro-3-(diphenylmethoxy)tropane But Not 4'-Chloro-3- (diphenylmethoxy)tropane Produces a Cocaine-like Behavioral Profile Richard H. Kline, Sari Izenwasser, Jonathan L. Katz, David B. Joseph, Wayne D. Bowen, and Amy Hauck Newman [Full Article - PDF]

858-863

Synthesis, Dopamine Transporter Affinity, Dopamine Uptake Inhibition, and Locomotor Stimulant Activity of 2-Substituted 3-Phenyltropane Derivatives Lifen Xu, Shreekrishna V. Kelkar, Stacey A. Lomenzo, Sari Izenwasser, Jonathan L. Katz, Richard H. Kline, and Mark L. Trudell [Full Article - PDF]

864-876

Synthesis and Pharmacology of Novel Analogues of Oxytocin and Deaminooxytocin: Directed Methods for the Construction of Disulfide and Trisulfide Bridges in Peptides Lin Chen, Ivana Zoulíková, Jiina Slaninová, and George Barany [Full Article - PDF]

877-884

Biologically Active Conformer of the Effector Region of Human C5a and Modulatory Effects of N-Terminal Receptor Binding Determinants on Activity Angela M. Finch, Shawn M. Vogen, Simon A. Sherman, Leonid Kirnarsky, Stephen M. Taylor, and Sam D. Sanderson [Full Article - PDF]

885-897

Cyclic HIV-1 Protease Inhibitors Derived from Mannitol: Synthesis, Inhibitory Potencies, and Computational Predictions of Binding Affinities Johan Hultén, Nicholas M. Bonham, Ulrika Nillroth, Tomas Hansson, Guido Zuccarello, Abderrahim Bouzide, Johan Åqvist, Björn Classon, U. Helena Danielson, Anders Karlén, Ingemar Kvarnström, Bertil Samuelsson, and Anders Hallberg [Full Article - PDF]

898-902

Unexpected Binding Mode of a Cyclic Sulfamide HIV-1 Protease Inhibitor Kristina Bäckbro, Seved Löwgren, Katrin Österlund, Johnson Atepo, and Torsten Unge , Johan Hultén, Nicholas M. Bonham, Wesley Schaal, Anders Karlén, and Anders Hallberg [Full Article - PDF]

903-919

Design, Synthesis, and Biological Activities of Four Angiotensin II Receptor Ligands with -Turn Mimetics Replacing Amino Acid Residues 3-5 Boris Schmidt, Susanna Lindman, Weimin Tong, Gunnar Lindeberg, Adolf Gogoll, Zhennan Lai, Madeleine Thörnwall, Barbro Synnergren, Annika Nilsson, Christopher J. Welch, Morgan Sohtell, Christer Westerlund, Fred Nyberg, Anders Karlén, and Anders Hallberg [Full Article - PDF]

920-929

HIV-1 Integrase Pharmacophore: Discovery of Inhibitors through Three-Dimensional Database Searching Marc C. Nicklaus, Nouri Neamati, Huixiao Hong, Abhijit Mazumder, Sanjay Sunder, Julie Chen, George W. A. Milne, and Yves Pommier [Full Article - PDF]

930-936

Discovery of HIV-1 Integrase Inhibitors by Pharmacophore Searching Huixiao Hong, Nouri Neamati, Shaomeng Wang, Marc C. Nicklaus, Abhijit Mazumder, He Zhao, Terrence R. Burke, Jr., Yves Pommier, and George W. A. Milne [Full Article - PDF]

937-941

Hydrazide-Containing Inhibitors of HIV-1 Integrase He Zhao, Nouri Neamati, Sanjay Sunder, Huixiao Hong, Shaomeng Wang, George W. A. Milne, Yves Pommier, and Terrence R. Burke, Jr. [Full Article - PDF]

942-951

Depsides and Depsidones as Inhibitors of HIV-1 Integrase: Discovery of Novel Inhibitors through 3D Database Searching Nouri Neamati, Huixiao Hong, Abhijit Mazumder, Shaomeng Wang, Sanjay Sunder, Marc C. Nicklaus, George W. A. Milne, Bohumil Proksa, and Yves Pommier [Full Article - PDF]

952-960

New Benzocycloalkylpiperazines, Potent and Selective 5-HT1A Receptor Ligands Youssef El Ahmad, Elisabeth Laurent, Philippe Maillet, Akram Talab, Jean François Teste, Raymond Dokhan, Gilles Tran, and Roland Ollivier [Full Article - PDF]

961-966

Antitumor Agents. 172. Synthesis and Biological Evaluation of Novel Deacetamidothiocolchicin-7-ols and Ester Analogs as Antitubulin Agents Qian Shi, Pascal Verdier-Pinard, Arnold Brossi, Ernest Hamel, Andrew T. McPhail, and Kuo-Hsiung Lee [Full Article - PDF]

967-971

Semisynthetic Derivatives of Purpuromycin as Potential Topical Agents for Vaginal Infections Aldo Trani, Clelia Dallanoce, Gianbattista Panzone, Franca Ripamonti, Beth P. Goldstein, and Romeo Ciabatti [Full Article - PDF]

972-979

Synthesis and Antitumor Activity of Duocarmycin Derivatives: A-Ring Pyrrole Compounds Bearing Cinnamoyl Groups Satoru Nagamura, Akira Asai, Nobuyoshi Amishiro, Eiji Kobayashi, Katsushige Gomi, and Hiromitsu Saito [Full Article - PDF]

980-989

Effect of Structural Modification of Enol-Carboxamide-Type Nonsteroidal Antiinflammatory Drugs on COX-2/COX-1 Selectivity Edward S. Lazer, Clara K. Miao, Charles L. Cywin, Ronald Sorcek, Hin-Chor Wong, Zhaoxing Meng, Ian Potocki, MaryAnn Hoermann, Roger J. Snow, Matt A. Tschantz, Terence A. Kelly, Daniel W. McNeil, Simon J. Coutts, Laurie Churchill, Anne G. Graham, Eva David, Peter M. Grob, Wolfhard Engel, Hans Meier, and Günter Trummlitz [Full Article - PDF]

990-995

Conformationally Constrained Deltorphin Analogs with 2-Aminotetralin-2-Carboxylic Acid in Position 3 Géza Tóth, Zsuzsa Darula, Antal Péter, Ferenc Fülöp, Dirk Tourwé, Hendrika Jaspers, Patricia Verheyden, Zsolt Böcskey, Zoltán Tóth, and Anna Borsodi [Full Article - PDF]

996-1004

New Non-Peptide Endothelin-A Receptor Antagonists: Synthesis, Biological Properties, and Structure-Activity Relationships of 5-(Dimethylamino)-N-pyridyl-, -N-pyrimidinyl-, -N-pyridazinyl-, and -N-pyrazinyl-1-naphthalenesulfonamides Robert H. Bradbury, Colin Bath, Roger J. Butlin, Michael Dennis, Christine Heys, Sarah J. Hunt, Roger James, Andrew A. Mortlock, Neil F. Sumner, Eric K. Tang, Berwick Telford, Elaine Whiting, and Campbell Wilson [Full Article - PDF]

1005-1017

Structural Analogues of the Calanolide Anti-HIV Agents. Modification of the trans-10,11-Dimethyldihydropyran-12-ol Ring (Ring C) David E. Zembower, Shuyuan Liao, Michael T. Flavin, Ze-Qi Xu, Tracy L. Stup, Robert W. Buckheit, Jr., Albert Khilevich, Aye Aye Mar, and Abram K. Sheinkman [Full Article - PDF]

1018-1025

Sulfonimidamide Analogs of Oncolytic Sulfonylureas,1 John E. Toth, Gerald B. Grindey, William J. Ehlhardt, James E. Ray, George B. Boder, Jesse R. Bewley, Kim K. Klingerman, Susan B. Gates, Sharon M. Rinzel, Richard M. Schultz, Leonard C. Weir, and John F. Worzalla [Full Article - PDF]

1026-1040

Inhibition of Stromelysin-1 (MMP-3) by P1'-Biphenylylethyl Carboxyalkyl Dipeptides Craig K. Esser, Robert L. Bugianesi, Charles G. Caldwell, Kevin T. Chapman, Philippe L. Durette, Narindar N. Girotra, Ihor E. Kopka, Thomas J. Lanza, Dorothy A. Levorse, Malcolm MacCoss, Karen A. Owens, Mitree M. Ponpipom, Joseph P. Simeone, Richard K. Harrison, Lisa Niedzwiecki, Joseph W. Becker, Alice I. Marcy, Melinda G. Axel, Amy J. Christen, Joseph McDonnell, Vernon L. Moore, Julie M. Olszewski, Cheryl Saphos, Denise M. Visco, Frank Shen, Adria Colletti, Philip A. Krieter, and William K. Hagmann [Full Article - PDF]

1041-1045

Repromicin Derivatives with Potent Antibacterial Activity against Pasteurella multocida James W. McFarland, Scott J. Hecker, Burton H. Jaynes, Martin R. Jefson, Kristin M. Lundy, Chi B. Vu, Edward A. Glazer, Susan A. Froshauer, Shigeru F. Hayashi, Barbara J. Kamicker, Catherine P. Reese, and Julie A. Olson [Full Article - PDF]

1046-1046

PHARMACOKINETIC ANALYSIS: A Practical Approach By Peter I. D. Lee and Gordon L. Amidon. Technomic Publishing, Lancaster, PA. 1996. xiii + 548 pp. 15.5 × 23.5 cm. ISBN 1-56676-425-4. $159.95. John J. Brennan [Full Article - PDF]

1047-1047

Comparative Molecular Field Analysis of Haptens Docked to the Multispecific Antibody IgE(Lb4) Armin M. Gamper, Rudolf H. Winger, Klaus R. Liedl, Christoph A. Sotriffer, Janos M. Varga, Romano T. Kroemer, and Bernd M. Rode [Full Article - PDF]

1048-1048

N-Aryl-3,3,3-trifluoro-2-hydroxy-2-methylpropanamides: KATP Potassium Channel Openers. Modifications on the Western Region Cyrus J. Ohnmacht, Keith Russell, James R. Empfield, Cathy A. Frank, Keith H. Gibson, Daniel R. Mayhugh, Frances M. McLaren, Howard S. Shapiro, Frederick J. Brown, Diane A. Trainor, Christopher Ceccarelli, Margaret M. Lin, Brian B. Masek, Janet M. Forst, Robert J. Harris, James M. Hulsizer, Joseph J. Lewis, Stuart M. Silverman, Reed W. Smith, Paul J. Warwick, Sen T. Kau, Alexa L. Chun, Thomas L. Grant, Burton B. Howe, Jack H. Li, Shephali Trivedi, Tracy J. Halterman, Christopher Yochim, Martin C. Dyroff, M.Kirkland, and Kathleen L. Neilson [Full Article - PDF]