Journal of Medicinal Chemistry
Volume 42, Issue 22 (November 4, 1999)
Copyright © 1999 American Chemical Society

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COMMUNICATIONS

4473-4478

Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine Derivatives as Highly Potent and Selective Human A3 Adenosine Receptor Antagonists Pier Giovanni Baraldi, Barbara Cacciari, Romeo Romagnoli, Giampiero Spalluto, Karl-Norbert Klotz, Edward Leung, Katia Varani, Stefania Gessi, Stefania Merighi, and Pier Andrea Borea [Full Article - PDF]

EXPEDITED ARTICLES

4479-4484

Potent and Selective Inhibition of Varicella-Zoster Virus (VZV) by Nucleoside Analogues with an Unusual Bicyclic Base Christopher McGuigan, Christopher J. Yarnold, Garry Jones, Sonsoles Velázquez, Hubert Barucki, Andrea Brancale, Graciela Andrei, Robert Snoeck, Erik De Clercq, and Jan Balzarini [Full Article - PDF]

ARTICLES

4485-4499

Endothelin Antagonists: Substituted Mesitylcarboxamides with High Potency and Selectivity for ETA Receptors Chengde Wu, E. Radford Decker, Natalie Blok, Huong Bui, Qi Chen, B. Raju, Andree R. Bourgoyne, Vippra Knowles, Ronald J. Biediger, Robert V. Market, Shuqun Lin, Brian Dupré, Timothy P. Kogan, George W. Holland, Tommy A. Brock, and Richard A. F. Dixon [Full Article - PDF]

4500-4505

Design of MKC-442 (Emivirine) Analogues with Improved Activity Against Drug-Resistant HIV Mutants Andrew L. Hopkins, Jingshan Ren, Hiromichi Tanaka, Masanori Baba, Mika Okamato, David I. Stuart, and David K. Stammers [Full Article - PDF]

4506-4523

Affinity and Selectivity of Matrix Metalloproteinase Inhibitors: A Chemometrical Study from the Perspective of Ligands and Proteins Hans Matter and Wilfried Schwab [Full Article - PDF]

4524-4537

Angiotensin II Analogues Encompassing 5,9- and 5,10-Fused Thiazabicycloalkane Tripeptide Mimetics Petra Johannesson, Gunnar Lindeberg, Weimin Tong, Adolf Gogoll, Barbro Synnergren, Fred Nyberg, Anders Karlén, and Anders Hallberg [Full Article - PDF]

4538-4546

Molecular Modeling Studies on G-Quadruplex Complexes of Telomerase Inhibitors: Structure-Activity Relationships Martin A. Read, Alexis A. Wood, John R. Harrison, Sharon M. Gowan, Lloyd R. Kelland, Harvinder S. Dosanjh, and Stephen Neidle [Full Article - PDF]

4547-4562

Design, Synthesis, and Biological Evaluation of Potent Thiazine- and Thiazepine-Based Matrix Metalloproteinase Inhibitors Neil G. Almstead, Rimma S. Bradley, Stanislaw Pikul, Biswanath De, Michael G. Natchus, Yetunde O. Taiwo, Fei Gu, Lisa E. Williams, Barbara A. Hynd, Michael J. Janusz, C. Michelle Dunaway, and Glen E. Mieling [Full Article - PDF]

4563-4571

Metabolism-Based Brain-Targeting System for a Thyrotropin-Releasing Hormone Analogue Laszlo Prokai, Katalin Prokai-Tatrai, Xudong Ouyang, Ho-Seung Kim, Whei-Mei Wu, Alevtina Zharikova, and Nicholas Bodor [Full Article - PDF]

4572-4583

Specific Nonpeptide Photoprobes as Tools for the Structural Study of the Angiotensin II AT1 Receptor Sandrine Nouet, Pierre R. Dodey, Michel R. Bondoux, Didier Pruneau, Jean-Michel Luccarini, Thierry Groblewski, Renée Larguier, Colette Lombard, Jacky Marie, Patrice P. Renaut, Gérard Leclerc, and Jean-Claude Bonnafous [Full Article - PDF]

4584-4603

Design and Synthesis of Thrombin Inhibitors: Analogues of MD-805 with Reduced Stereogenicity and Improved Potency Derek Brundish, Alice Bull, Vera Donovan, Joseph D. Fullerton, Sheila M. Garman, Judy F. Hayler, Diana Janus, Peter D. Kane, Mark McDonnell, Garrick P. Smith, Robert Wakeford, Clive V. Walker, Graham Howarth, William Hoyle, Mark C. Allen, John Ambler, Keith Butler, and Mark D. Talbot [Full Article - PDF]

4604-4613

Solution Structure of Polymyxins B and E and Effect of Binding to Lipopolysaccharide: An NMR and Molecular Modeling Study Primo Pristovek and Jurka Kidri [Full Article - PDF]

4614-4620

C60 and Water-Soluble Fullerene Derivatives as Antioxidants Against Radical-Initiated Lipid Peroxidation I Chen Wang, Lin Ai Tai, Don Dar Lee, P. P. Kanakamma, Clifton K.-F. Shen, Tien-Yau Luh, Chien Hong Cheng, and Kuo Chu Hwang [Full Article - PDF]

4621-4629

Asymmetric Synthesis of 9-Alkyl-2-benzyl-6,7-benzomorphans: Characterization as Novel Receptor Ligands F. Ivy Carroll, Xu Bai, Ali Dehghani, S. Wayne Mascarella, Wanda Williams, and Wayne D. Bowen [Full Article - PDF]

4630-4639

Structural Specificity of Chloroquine-Hematin Binding Related to Inhibition of Hematin Polymerization and Parasite Growth Sudha Rani Vippagunta, Arnulf Dorn, Hugues Matile, Apurba K. Bhattacharjee, Jean M. Karle, William Y. Ellis, Robert G. Ridley, and Jonathan L. Vennerstrom [Full Article - PDF]

4640-4649

3-O-Desacyl Monophosphoryl Lipid A Derivatives: Synthesis and Immunostimulant Activities David A. Johnson, David S. Keegan, C. Gregory Sowell, Mark T. Livesay, Craig L. Johnson, Lara M. Taubner, Annalivia Harris, Kent R. Myers, Jennifer D. Thompson, Gary L. Gustafson, Michael J. Rhodes, J. Terry Ulrich, Jon R. Ward, Yvonne M. Yorgensen, John L. Cantrell, and Valerie G. Brookshire [Full Article - PDF]

4650-4658

Predicting Binding Affinities of Protein Ligands from Three-Dimensional Models: Application to Peptide Binding to Class I Major Histocompatibility Proteins Didier Rognan, Sanne Lise Lauemller, Arne Holm, Sren Buus, and Vincenzo Tschinke [Full Article - PDF]

4659-4668

5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-Based Potent and Selective CCK1 Receptor Antagonists: Structural Modifications at the Tryptophan Domain José M. Bartolomé-Nebreda, Isabel Gómez-Monterrey, M. Teresa García-López, Rosario González-Muñiz, Mercedes Martín-Martínez, Santiago Ballaz, Edurne Cenarruzabeitia, Miriam LaTorre, Joaquín Del Río, and Rosario Herranz [Full Article - PDF]

4669-4679

Amide Analogues of Trichostatin A as Inhibitors of Histone Deacetylase and Inducers of Terminal Cell Differentiation Manfred Jung, Gerald Brosch, Doris Kölle, Hans Scherf, Clarissa Gerhäuser, and Peter Loidl [Full Article - PDF]

4680-4694

Discovery of Novel Non-Peptide CCR1 Receptor Antagonists Howard P. Ng,,1 Karen May, John G. Bauman, Ameen Ghannam, Imadul Islam, Meina Liang, Richard Horuk, Joseph Hesselgesser, R. Michael Snider, H. Daniel Perez, and Michael M. Morrissey [Full Article - PDF]

4695-4704

LASSOO: A Generalized Directed Diversity Approach to the Design and Enrichment of Chemical Libraries Ryan T. Koehler, Steven L. Dixon, and Hugo O. Villar [Full Article - PDF]

4705-4713

Structure-Activity Relationships of Novel 2-Substituted Quinazoline Antibacterial Agents Pei-Pei Kung, Martin D. Casper, Kimberley L. Cook, Laura Wilson-Lingardo, Lisa M. Risen, Timothy A. Vickers, Ray Ranken, Lawrence B. Blyn, Jacqueline R. Wyatt, P. Dan Cook, and David J. Ecker [Full Article - PDF]

4714-4719

Vancomycin Binding to Low-Affinity Ligands: Delineating a Minimum Set of Interactions Necessary for High-Affinity Binding Patrick J. Loll, Jeffrey Kaplan, Barry S. Selinsky, and Paul H. Axelsen [Full Article - PDF]

BRIEF ARTICLES

4720-4724

Synthesis and Pharmacological Evaluation of Some 8-Cyanopyrido[3',2':4,5]thieno[3,2-d]triazine Derivatives as Inhibitors of Nitric Oxide and Eicosanoid Biosynthesis José Ma Quintela, Carlos Peinador, Liliana Ma González, Ricardo Riguera, Inmaculada Rioja, Ma Carmen Terencio, Amalia Ubeda, and Ma José Alcaraz [Full Article - PDF]

4725-4728

Inhibition and Substrate Activity of Conformationally Rigid Vigabatrin Analogues with -Aminobutyric Acid Aminotransferase Jian Qiu, Joyce M. Pingsterhaus, and Richard B. Silverman [Full Article - PDF]

4729-4732

Synthesis and Biological Evaluation of the First N-Alkyl Cage Dimeric 4-Aryl-1,4-dihydropyridines as Novel Nonpeptidic HIV-1 Protease Inhibitors Andreas Hilgeroth, Michael Wiese, and Andreas Billich [Full Article - PDF]