Journal of Medicinal Chemistry
Volume 44, Issue 16 (August 2, 2001)
Copyright © 2001 American Chemical Society

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LETTERS

2499-2502

Potent and Selective Carboxylic Acid-Based Inhibitors of Matrix Metalloproteinases Stanislaw Pikul, Norman E. Ohler, Greg Ciszewski, Michael C. Laufersweiler, Neil G. Almstead, Biswanath De, Michael G. Natchus, Lily C. Hsieh, Michael J. Janusz, Sean X. Peng, Todd M. Branch, Selane L. King, Yetunde O. Taiwo, and Glen E. Mieling [Full Article - PDF]

2503-2506

Experimental Precedent for the Need To Involve the Primary Hydration Layer of DNA in Lead Drug Design Sophia Y. Breusegem, Seyed E. Sadat-Ebrahimi, Kenneth T. Douglas, Elena V. Bichenkova, Robert M. Clegg, and Frank G. Loontiens [Full Article - PDF]

2507-2510

A Rational Approach to the Design of Selective Substrates and Potent Nontransportable Inhibitors of the Excitatory Amino Acid Transporter EAAC1 (EAAT3). New Glutamate and Aspartate Analogues as Potential Neuroprotective Agents Giuseppe Campiani, Meri De Angelis, Silvia Armaroli, Caterina Fattorusso, Bruno Catalanotti, Anna Ramunno, Vito Nacci, Ettore Novellino, Christof Grewer, Diana Ionescu, Thomas Rauen, Roger Griffiths, Colin Sinclair, Elena Fumagalli, and Tiziana Mennini [Full Article - PDF]

ARTICLES

2511-2522

Novel Selective PDE4 Inhibitors. 1. Synthesis, Structure-Activity Relationships, and Molecular Modeling of 4-(3,4-Dimethoxyphenyl)-2H-phthalazin-1-ones and Analogues Margaretha Van der Mey, Armin Hatzelmann, Ivonne J. Van der Laan, Geert J. Sterk, Ulrich Thibaut, and Hendrik Timmerman [Full Article - PDF]

2523-2535

Novel Selective PDE4 Inhibitors. 2. Synthesis and Structure-Activity Relationships of 4-Aryl-Substituted cis-Tetra- and cis-Hexahydrophthalazinones Margaretha Van der Mey, Armin Hatzelmann, Gerard P. M. Van Klink, Ivonne J. Van der Laan, Geert J. Sterk, Ulrich Thibaut, Wolf R. Ulrich, and Hendrik Timmerman [Full Article - PDF]

2536-2543

Design, Synthesis, DNA Binding, and Biological Evaluation of Water-Soluble Hybrid Molecules Containing Two Pyrazole Analogues of the Alkylating Cyclopropylpyrroloindole (CPI) Subunit of the Antitumor Agent CC-1065 and Polypyrrole Minor Groove Binders Pier Giovanni Baraldi, Gianfrano Balboni, Maria Giovanna Pavani, Giampiero Spalluto, Mojgan Aghazadeh Tabrizi, Erik De Clercq, Jan Balzarini, Toshikazu Bando, Hiroshi Sugiyama, and Romeo Romagnoli [Full Article - PDF]

2544-2554

Structure-Based Design, Synthesis, and Biological Evaluation of Conformationally Restricted Novel 2-Alkylthio-6-[1-(2,6-difluorophenyl)alkyl]- 3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as Non-nucleoside Inhibitors of HIV-1 Reverse Transcriptase Antonello Mai, Gianluca Sbardella, Marino Artico, Rino Ragno, Silvio Massa, Ettore Novellino, Giovanni Greco, Antonio Lavecchia, Chiara Musiu, Massimiliano La Colla, Chiara Murgioni, Paolo La Colla, and Roberta Loddo [Full Article - PDF]

2555-2564

Structural Studies on Bioactive Compounds. 34. Design, Synthesis, and Biological Evaluation of Triazenyl-Substituted Pyrimethamine Inhibitors of Pneumocystis carinii Dihydrofolate Reductase David C. M. Chan, Charles A. Laughton, Sherry F. Queener, and Malcolm F. G. Stevens [Full Article - PDF]

2565-2574

Disabling ErbB Receptors with Rationally Designed Exocyclic Mimetics of Antibodies: Structure-Function Analysis Alan Berezov, Hong-Tao Zhang, Mark I. Greene, and Ramachandran Murali [Full Article - PDF]

2575-2585

Original 2-Alkylamino-6-halogenoquinazolin-4(3H)-ones and KATP Channel Activity Fabian Somers, Raogo Ouedraogo, Marie-Hélène Antoine, Pascal de Tullio, Bénédicte Becker, Jeanine Fontaine, Jacques Damas, Léon Dupont, Benoit Rigo, Jacques Delarge, Philippe Lebrun, and Bernard Pirotte [Full Article - PDF]

2586-2592

Design and Synthesis of Potent and Selective 47 Integrin Antagonists Jürgen Boer, Dirk Gottschling, Anja Schuster, Monika Semmrich, Bernhard Holzmann, and Horst Kessler [Full Article - PDF]

2593-2600

Structure-Activity Studies of Ground- and Transition-State Analogue Inhibitors of Cyclophilin Harry C. Wang, Kyonghee Kim, Ray Bakhtiar, and Juris P. Germanas [Full Article - PDF]

2601-2611

The Effect of 1,3-Diaryl-[1H]-pyrazole-4-acetamides on Glucose Utilization in ob/ob Mice Gregory R. Bebernitz, Greg Argentieri, Beverly Battle, Christine Brennan, Bork Balkan, Bryan F. Burkey, Michele Eckhardt, Jiaping Gao, Prasad Kapa, Robert J. Strohschein, Herbert F. Schuster, Mary Wilson, and David D. Xu [Full Article - PDF]

2612-2618

Synthesis of Cytotoxic 6E-Hydroximino-4-ene Steroids: Structure/Activity Studies Noé Deive, Jaime Rodríguez, and Carlos Jiménez [Full Article - PDF]

2619-2635

Synthesis of 6- and 7- Hydroxy-8-azabicyclo[3.2.1]octanes and Their Binding Affinity for the Dopamine and Serotonin Transporters Peter C. Meltzer, Bing Wang, Zhengming Chen, Paul Blundell, Muthusamy Jayaraman, Mario D. Gonzalez, Clifford George, and Bertha K. Madras [Full Article - PDF]

2636-2660

Design, Synthesis, and Structure-Activity Relationships of Macrocyclic Hydroxamic Acids That Inhibit Tumor Necrosis Factor Release in Vitro and in Vivo Chu-Biao Xue, Matthew E. Voss, David J. Nelson, James J.-W. Duan, Robert J. Cherney, Irina C. Jacobson, Xiaohua He, John Roderick, Lihua Chen, Ronald L. Corbett, Li Wang, Dayton T. Meyer, Kenneth Kennedy, William F. DeGrado, Karl D. Hardman, Christopher A. Teleha, Bruce D. Jaffee, Rui-Qin Liu, Robert A. Copeland, Maryanne B. Covington, David D. Christ, James M. Trzaskos, Robert C. Newton, Ronald L. Magolda, Ruth R. Wexler, and Carl P. Decicco [Full Article - PDF]

2661-2666

Thiazolidine Prodrugs as Protective Agents against -Radiation-Induced Toxicity and Mutagenesis in V79 Cells Britta H. Wilmore, Pamela B. Cassidy, Raymond L. Warters, and Jeanette C. Roberts [Full Article - PDF]

BRIEF ARTICLES

2667-2670

Reduced Amide Bond Peptidomimetics. (4S)-N-(4-Amino-5-[aminoalkyl]aminopentyl)-N'-nitroguanidines, Potent and Highly Selective Inhibitors of Neuronal Nitric Oxide Synthase Jung-Mi Hah, Linda J. Roman, Pavel Martásek, and Richard B. Silverman [Full Article - PDF]

2671-2674

Synthesis and Evaluation of Oxodioxolenylmethyl Carbamate Prodrugs of Pseudomycins Xicheng Sun, Michael Rodriguez, Doug Zeckner, Bobbie Sachs, William Current, Robert Boyer, Jonathan Paschal, Carl McMillian, and Shu-Hui Chen [Full Article - PDF]

2675-2678

(-)3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic Acid [(-)DRF 2725]: A Dual PPAR Agonist with Potent Antihyperglycemic and Lipid Modulating Activity Braj B. Lohray, Vidya B. Lohray, Ashok C. Bajji, Shivaramayya Kalchar, Rajamohan R. Poondra, Srinivas Padakanti, Ranjan Chakrabarti, Reeba K. Vikramadithyan, Parimal Misra, Suresh Juluri, N. V. S. Rao Mamidi, and Ramanujam Rajagopalan [Full Article - PDF]