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] |