Journal of Medicinal Chemistry
Volume 39, Issue 22 (October 25, 1996)
Copyright © 1996 American Chemical Society

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4349-4353

Structure-Based Design of HIV Protease Inhibitors: Sulfonamide-Containing 5,6-Dihydro-4-hydroxy-2-pyrones as Non-Peptidic Inhibitors Suvit Thaisrivongs, Harvey I. Skulnick, Steve R. Turner, Joseph W. Strohbach, Ruben A. Tommasi, Paul D. Johnson, Paul A. Aristoff, Thomas M. Judge, Ronald B. Gammill, Jeanette K. Morris, Karen R. Romines, Robert A. Chrusciel, Roger R. Hinshaw, Kong-Teck Chong, W. Gary Tarpley, Susan M. Poppe, David E. Slade, Janet C. Lynn, Miao-Miao Horng, Paul K. Tomich, Eric P. Seest, Lester A. Dolak, W. Jeffrey Howe, Gina M. Howard, Francis J. Schwende, Lisa N. Toth, Guy E. Padbury, Grace J. Wilson, Lihua Shiou, Gail L. Zipp, Karen F. Wilkinson, Bob D. Rush, Mary J. Ruwart, Kenneth A. Koeplinger, Zhiyang Zhao, Serena Cole,$ Renee M. Zaya,$ Thomas J. Kakuk,$ Musiri N. Janakiraman, and Keith D. Watenpaugh [Full Article - PDF]

4354-4357

Rapid Microscale Synthesis, a New Method for Lead Optimization Using Robotics and Solution Phase Chemistry: Application to the Synthesis and Optimization of Corticotropin-Releasing Factor1 Receptor Antagonists Jeffrey P. Whitten, Yun Feng Xie, Philip E. Erickson, Thomas R. Webb, Errol B. De Souza, Dimitri E. Grigoriadis, and James R. McCarthy [Full Article - PDF]

4358-4360

Design and Synthesis of a Series of Non-Peptide High-Affinity Human Corticotropin-Releasing Factor1 Receptor Antagonists Chen Chen, Raymond Dagnino, Jr., Errol B. De Souza, Dimitri E. Grigoriadis, Charles Q. Huang, Kyung-Il Kim, Zhengyu Liu, Terry Moran, Thomas R. Webb, Jeffrey P. Whitten, Yun Feng Xie, and James R. McCarthy [Full Article - PDF]

4361-4365

Localizing Antithrombotic and Vasodilatory Activity with a Novel, Ultrafast Nitric Oxide Donor Joseph E. Saavedra, Garry J. Southan, Keith M. Davies, Anders Lundell, Chris Markou, Stephen R. Hanson, Christophe Adrie, William E. Hurford, Warren M. Zapol, and Larry K. Keefer [Full Article - PDF]

4366-4376

Synthesis, Structure-Activity Relationships, and the Effect of Polyethylene Glycol on Inhibitors of Phosphatidylinositol-Specific Phospholipase C from Bacillus cereus Margret Ryan, Miles P. Smith, Thottumkara K. Vinod, Wai Leung Lau, John F. W. Keana, and O. Hayes Griffith [Full Article - PDF]

4377-4381

Octanol-, Chloroform-, and Propylene Glycol Dipelargonat-Water Partitioning of Morphine-6-glucuronide and Other Related Opiates Alex Avdeef , David A. Barrett, P. Nicholas Shaw, Roger D. Knaggs, and Stanley S. Davis [Full Article - PDF]

4382-4395

Heterocyclic Ureas: Inhibitors of Acyl-CoA:Cholesterol O-Acyltransferase as Hypocholesterolemic Agents Andrew D. White, Mark W. Creswell, Alexander W. Chucholowski, C. John Blankley, Michael W. Wilson, Richard F. Bousley, Arnold D. Essenburg, Katherine L. Hamelehle, Brian R. Krause, Richard L. Stanfield, Mark A. Dominick, and Martin Neub [Full Article - PDF]

4396-4405

Synthesis, Activity, and Molecular Modeling of a New Series of Tricyclic Pyridazinones as Selective Aldose Reductase Inhibitors Luca Costantino, Giulio Rastelli, Katia Vescovini, Giorgio Cignarella, Paola Vianello, Antonella Del Corso, Mario Cappiello, Umberto Mura, and Daniela Barlocco [Full Article - PDF]

4406-4420

Three-Dimensional Models for Agonist and Antagonist Complexes with 2 Adrenergic Receptor Maria Kontoyianni, Carol DeWeese, Julie E. Penzotti, and Terry P. Lybrand [Full Article - PDF]

4421-4429

Novel (R)-2-Amino-5-fluorotetralins: Dopaminergic Antagonists and Inverse Agonists Åsa Malmberg, Berit Backlund Höök, Anette M. Johansson, and Uli Hacksell [Full Article - PDF]

4430-4438

Synthesis of Chiral 1-(2'-Amino-2'-carboxyethyl)-1,4-dihydro-6,7-quinoxaline-2,3-diones: -Amino-3-hydroxy-5-methyl-4-isoxazolepropionate Receptor Agonists and Antagonists Guoping Sun, Norman J. Uretsky, Lane J. Wallace, Gamal Shams, David M. Weinstein, and Duane D. Miller [Full Article - PDF]

4439-4450

Synthesis and Structure-Activity Relationships of a New Model of Arylpiperazines. 1. 2-[[4-(o-Methoxyphenyl)piperazin-1-yl]methyl]-1,3- dioxoperhydroimidazo[1,5-a]pyridine: A Selective 5-HT1A Receptor Agonist María L. López-Rodríguez, Ma Luisa Rosado, Bellinda Benhamú, Ma José Morcillo, Antonio M. Sanz, Luis Orensanz, Ma Eugenia Beneitez, José A. Fuentes, and Jorge Manzanares [Full Article - PDF]

4451-4459

Potent Immunosuppressants, 2-Alkyl-2-aminopropane-1,3-diols Tetsuro Fujita, Ryoji Hirose, Masahiko Yoneta, Shigeo Sasaki, Kenichiro Inoue, Masatoshi Kiuchi, Susumu Hirase, Kenji Chiba, Hiroshi Sakamoto, and Masafumi Arita [Full Article - PDF]

4460-4470

The Simulated Binding of (±)-2,3-Dihydro-5,6-dimethoxy-2-[[1-(phenylmethyl)-4- piperidinyl]methyl]-1H-inden-1-one Hydrochloride (E2020) and Related Inhibitors to Free and Acylated Acetylcholinesterases and Corresponding Structure-Activity Analyses Atsushi Inoue, Takatoshi Kawai, Misako Wakita, Youichi Iimura, Hachiro Sugimoto, and Yoshiyuki Kawakami [Full Article - PDF]

4471-4477

Structure-Activity Relationships in a Series of Substituted Indolocarbazoles: Topoisomerase I and Protein Kinase C Inhibition and Antitumoral and Antimicrobial Properties Elisabète Rodrigues Pereira, Laure Belin, Martine Sancelme, Michelle Prudhomme, Monique Ollier, Maryse Rapp, Danièle Sevère, Jean-François Riou, Doriano Fabbro, and Thomas Meyer [Full Article - PDF]

4478-4482

Aspartic Acid Conjugates of 2-(3,4-Dichlorophenyl)-N-methyl-N- [(1S)-1-(3-aminophenyl)-2-(1-pyrrolidinyl)ethyl]acetamide: Opioid Receptor Agonists with Limited Access to the Central Nervous System An-Chih Chang, Alan Cowan, Akira E. Takemori, and Philip S. Portoghese [Full Article - PDF]

4483-4488

Synthesis and Immunostimulating Properties of Lipophilic Ester and Ether Muramyl Peptide Derivatives Ghada Merhi, Anthony W. Coleman, Jean-Philippe Devissaguet, and Gillian M. Barratt [Full Article - PDF]

4489-4496

4'-Methyl Derivatives of 5-MOP and 5-MOA: Synthesis, Photoreactivity, and Photobiological Activity Ornella Gia, Antonella Anselmo, Maria Teresa Conconi, Cipriano Antonello, Eugenio Uriarte, and Sergio Caffieri [Full Article - PDF]

4497-4506

Synthesis and Biological Activity of 1,25-Dihydroxy-18-norvitamin D3 and 1,25-Dihydroxy-18,19-dinorvitamin D3 Rafal R. Sicinski, Kato L. Perlman, Jean Prahl, Connie Smith, and Hector F. DeLuca [Full Article - PDF]

4507-4510

Structure-Activity Modifications of the HIV-1 Inhibitors (+)-Calanolide A and (-)-Calanolide B Deborah L. Galinis, Richard W. Fuller, Tawnya C. McKee, John H. Cardellina II, Robert J. Gulakowski, James B. McMahon, and Michael R. Boyd [Full Article - PDF]

4511-4514

Mechanism-Based Design of Parasite-Targeted Artemisinin Derivatives: Synthesis and Antimalarial Activity of Benzylamino and Alkylamino Ether Analogues of Artemisinin Paul M. O'Neill, Laurence P. Bishop, Richard C. Storr, Shaun R. Hawley, James L. Maggs, Stephen A. Ward, and B. Kevin Park [Full Article - PDF]

4515-4519

Head Group Analogs of Arachidonylethanolamide, the Endogenous Cannabinoid Ligand Atmaram D. Khanolkar, Vasiliki Abadji, Sonyuan Lin, W. Adam G. Hill, Gihan Taha, Khaled Abouzid, Zhaoxing Meng, Pusheng Fan, and Alexandros Makriyannis [Full Article - PDF]

4520-4526

Synthesis and Solution Conformation of Cyclo[RGDRGD]: A Cyclic Peptide with Selectivity for the V3 Receptor Kevin Burgess and Dongyeol Lim , Shaker A. Mousa [Full Article - PDF]