Journal of Medicinal Chemistry
Volume 42, Issue 26 (December 30, 1999)
Copyright © 1999 American Chemical Society

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ARTICLES

5289-5310

Synthesis and Structure-Activity Relationships of New 1,3-Disubstituted Cyclohexanes as Structurally Rigid Leukotriene B4 Receptor Antagonists Jean-Marc Poudrel, Pierre Hullot, Jean-Pierre Vidal, Jean-Pierre Girard, Jean-Claude Rossi, Agnès Muller, Claude Bonne, Vladimir Bezuglov, Igor Serkov, Pierre Renard, and Bruno Pfeiffer [Full Article - PDF]

5311-5324

Na+-Glucose Cotransporter (SGLT) Inhibitors as Antidiabetic Agents. 4. Synthesis and Pharmacological Properties of 4'-Dehydroxyphlorizin Derivatives Substituted on the B Ring Kenji Tsujihara, Mitsuya Hongu, Kunio Saito, Hiroyuki Kawanishi, Kayoko Kuriyama, Mamoru Matsumoto, Akira Oku, Kiichiro Ueta, Minoru Tsuda, and Akira Saito [Full Article - PDF]

5325-5337

Molecular Recognition of Modified Adenine Nucleotides by the P2Y1-Receptor. 1. A Synthetic, Biochemical, and NMR Approach Efrat Halbfinger, Dan T. Major, Marco Ritzmann, Joachim Ubl, Georg Reiser, Jose L. Boyer, Kendall T. Harden, and Bilha Fischer [Full Article - PDF]

5338-5347

Molecular Recognition of Modified Adenine Nucleotides by the P2Y1-Receptor. 2. A Computational Approach Dan T. Major, Efrat Halbfinger, and Bilha Fischer [Full Article - PDF]

5348-5358

Comparative Molecular Field Analysis of Fungal Squalene Epoxidase Inhibitors Vijay M. Gokhale and Vithal M. Kulkarni [Full Article - PDF]

5359-5368

Exploring the Structure-Activity Relationships of [1-(4-tert-Butyl-3'-hydroxy)benzhydryl-4-benzylpiperazine] (SL-3111), A High-Affinity and Selective -Opioid Receptor Nonpeptide Agonist Ligand Josue Alfaro-Lopez, Toru Okayama, Keiko Hosohata, Peg Davis, Frank Porreca, Henry I. Yamamura, and Victor J. Hruby [Full Article - PDF]

5369-5389

Design and Structure-Activity Relationship of a New Class of Potent VEGF Receptor Tyrosine Kinase Inhibitors Laurent F. Hennequin, Andrew P. Thomas, Craig Johnstone, Elaine S. E. Stokes, Patrick A. Plé, Jean-Jacques M. Lohmann, Donald J. Ogilvie, Mike Dukes, Steve R. Wedge, Jon O. Curwen, Jane Kendrew, and Christine Lambert-van der Brempt [Full Article - PDF]

5390-5401

Modeling of Amino-Terminal Domains of Group I Metabotropic Glutamate Receptors: Structural Motifs Affecting Ligand Selectivity Gabriele Costantino, Antonio Macchiarulo, and Roberto Pellicciari [Full Article - PDF]

5402-5414

Selective Inhibitors of Glial GABA Uptake: Synthesis, Absolute Stereochemistry, and Pharmacology of the Enantiomers of 3-Hydroxy-4-amino-4,5,6,7-tetrahydro-1,2-benzisoxazole (exo-THPO) and Analogues Erik Falch, Jens Perregaard, Bente Frlund, Birgitte Skilde, Anders Buur, Lene M. Hansen, Karla Frydenvang, Lotte Brehm, Tina Bolvig, Orla M. Larsson, Connie Sanchez, Harold S. White, Arne Schousboe, and Povl Krogsgaard-Larsen [Full Article - PDF]

5415-5425

Synthesis, Characterization, and Structure-Activity Relationships of Amidine-Substituted (Bis)benzylidene-Cycloketone Olefin Isomers as Potent and Selective Factor Xa Inhibitors William J. Guilford, Kenneth J. Shaw, Jerry L. Dallas, Sunil Koovakkat, Wheeseong Lee, Amy Liang, David R. Light, Margaret A. McCarrick, Marc Whitlow, Bin Ye, and Michael M. Morrissey [Full Article - PDF]

5426-5436

Design, Synthesis, and Biological Evaluation of Matrix Metalloproteinase Inhibitors Derived from a Modified Proline Scaffold Menyan Cheng, Biswanath De, Neil G. Almstead, Stanislaw Pikul, Martin E. Dowty, Charles R. Dietsch, C. Michelle Dunaway, Fei Gu, Lily C. Hsieh, Michael J. Janusz, Yetunde O. Taiwo, and Michael G. Natchus , Tomas Hudlicky and Martin Mandel [Full Article - PDF]

5437-5447

2-(Diethylamino)thieno[1,3]oxazin-4-ones as Stable Inhibitors of Human Leukocyte Elastase Michael Gütschow, Lars Kuerschner, Ulf Neumann, Markus Pietsch, Reik Löser, Norman Koglin, and Kurt Eger [Full Article - PDF]

5448-5454

Inhibition of Trypanosoma cruzi Trypanothione Reductase by Acridines: Kinetic Studies and Structure-Activity Relationships Susanne Bonse, Christiane Santelli-Rouvier, Jacques Barbe, and R. Luise Krauth-Siegel [Full Article - PDF]

5455-5463

Probes for Narcotic Receptor Mediated Phenomena. 26. Synthesis and Biological Evaluation of Diarylmethylpiperazines and Diarylmethylpiperidines as Novel, Nonpeptidic Opioid Receptor Ligands Xiaoyan Zhang, Kenner C. Rice, Silvia N. Calderon, Hiroshi Kayakiri, Larren Smith, Andrew Coop, Arthur E. Jacobson, Richard B. Rothman, Peg Davis, Christina M. Dersch, and Frank Porreca [Full Article - PDF]

5464-5474

Tyrosine Kinase Inhibitors. 16. 6,5,6-Tricyclic Benzothieno[3,2-d]pyrimidines and Pyrimido[5,4-b]- and -[4,5-b]indoles as Potent Inhibitors of the Epidermal Growth Factor Receptor Tyrosine Kinase H. D. Hollis Showalter, Alexander J. Bridges, Hairong Zhou, Anthony D. Sercel, Amy McMichael, and David W. Fry [Full Article - PDF]

BRIEF ARTICLES

5475-5481

Synthesis and Biological Evaluation of Dihydrobenzofuran Lignans and Related Compounds as Potential Antitumor Agents that Inhibit Tubulin Polymerization Luc Pieters, Stefaan Van Dyck, Mei Gao, Ruoli Bai, Ernest Hamel, Arnold Vlietinck, and Guy Lemière [Full Article - PDF]

5482-5486

Combined Effect of Platination and Intercalation upon DNA Binding of Novel Cytotoxic Pt-Bis(naphthalimide) Complexes José M. Pérez, Isabel López-Solera, Eva I. Montero, Miguel F. Braña, Carlos Alonso, Simon P. Robinson, and Carmen Navarro-Ranninger [Full Article - PDF]

5487-5493

Novel, Potent, Semisynthetic Antimalarial Carba Analogues of the First-Generation 1,2,4-Trioxane Artemether Paul M. O'Neill, Natalie L. Searle, Ka-Wing Kan, Richard C. Storr, James L. Maggs, Stephen A. Ward, Kaylene Raynes, and B. Kevin Park [Full Article - PDF]