Journal of Medicinal Chemistry
Volume 43, Issue 5 (March 9, 2000)
Copyright © 2000 American Chemical Society

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COMMUNICATIONS

765-768

2 Adrenoceptor Agonists as Potential Analgesic Agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphtheneas a High-Affinity Ligand for the 2D Adrenergic Receptor Tina M. Ross, Michele C. Jetter, Mark E. McDonnell, Robert E. Boyd, Charlene D. Connelly, Rebecca P. Martinez, Martin A. Lewis, Ellen E. Codd, Robert B. Raffa, and Allen B. Reitz [Full Article - PDF]

769-771

1-(2-Nitrophenyl)thiosemicarbazides: A Novel Class of Potent, Orally Active Non-Peptide Antagonist for the Bradykinin B2 Receptor Edward K. Dziadulewicz, Timothy J. Ritchie, Allan Hallett, Christopher R. Snell, Soo Y. Ko, Roger Wrigglesworth, Glyn A. Hughes, Andrew R. Dunstan, Graham C. Bloomfield, Gillian S. Drake, Michael C. Brown, Wai Lee, Gillian M. Burgess, Clare Davis, Mohammed Yaqoob, Martin N. Perkins, Elizabeth A. Campbell, Andrew J. Davis, and Humphrey P. Rang [Full Article - PDF]

772-774

Dual Function Glutamate-Related Ligands: Discovery of a Novel, Potent Inhibitor of Glutamate Carboxypeptidase II Possessing mGluR3 Agonist Activity Fajun Nan, Tomasz Bzdega, Sergey Pshenichkin, Jarda T. Wroblewski, Barbara Wroblewska, Joseph H. Neale, and Alan P. Kozikowski [Full Article - PDF]

775-777

4-[5-Methyl-3-phenylisoxazol-4-yl]- benzenesulfonamide, Valdecoxib: A Potent and Selective Inhibitor of COX-2 John J. Talley, David L. Brown, Jeffery S. Carter, Matthew J. Graneto, Carol M. Koboldt, Jaime L. Masferrer, William E. Perkins, Roland S. Rogers, Alexander F. Shaffer, Yan Y. Zhang, Ben S. Zweifel, and Karen Seibert [Full Article - PDF]

ARTICLES

778-783

Potent Anti-HIV (Type 1 and Type 2) Activity of Polyoxometalates: Structure-Activity Relationship and Mechanism of Action Myriam Witvrouw, Helmut Weigold, Christophe Pannecouque, Dominique Schols, Erik De Clercq, and George Holan [Full Article - PDF]

784-796

Design of Potent Dicyclic (4-10/5-8) Gonadotropin Releasing Hormone (GnRH) Antagonists Jean E. Rivier, R. Scott Struthers, John Porter, Sabine L. Lahrichi, Guangcheng Jiang, Laura A. Cervini, Michel Ibea, Dean A. Kirby, Steven C. Koerber, and Catherine L. Rivier [Full Article - PDF]

797-806

Design of Monocyclic (1-3) and Dicyclic (1-3/4-10) Gonadotropin Releasing Hormone (GnRH) Antagonists Jean E. Rivier, John Porter, Laura A. Cervini, Sabine L. Lahrichi, Dean A. Kirby, R. Scott Struthers, Steven C. Koerber, and Catherine L. Rivier [Full Article - PDF]

807-818

Design of Potent Dicyclic (1-5/4-10) Gonadotropin Releasing Hormone (GnRH) Antagonists Jean E. Rivier, Guangcheng Jiang, R. Scott Struthers, Steven C. Koerber, John Porter, Laura A. Cervini, Dean A. Kirby, A. Grey Craig, and Catherine L. Rivier [Full Article - PDF]

819-828

Consensus Bioactive Conformation of Cyclic GnRH Antagonists Defined by NMR and Molecular Modeling Steven C. Koerber, Josep Rizo, R. Scott Struthers, and Jean E. Rivier [Full Article - PDF]

829-842

Synthesis, Biological Activity, and Molecular Modeling of Ribose-Modified Deoxyadenosine Bisphosphate Analogues as P2Y1 Receptor Ligands Erathodiyil Nandanan, Soo-Yeon Jang, Stefano Moro, Hea Ok Kim, Maqbool A. Siddiqui, Pamela Russ, Victor E. Marquez, Roger Busson, Piet Herdewijn, T. Kendall Harden, José L. Boyer, and Kenneth A. Jacobson [Full Article - PDF]

843-858

5,6-Dihydropyran-2-ones Possessing Various Sulfonyl Functionalities: Potent Nonpeptidic Inhibitors of HIV Protease Frederick E. Boyer, J. V. N. Vara Prasad, John M. Domagala, Edmund L. Ellsworth, Christopher Gajda, Susan E. Hagen, Larry J. Markoski, Bradley D. Tait, Elizabeth A. Lunney, Alexander Palovsky, Donna Ferguson, Neil Graham, Tod Holler, Donald Hupe, Carolyn Nouhan, Peter J. Tummino, A. Urumov, Eric Zeikus, Greg Zeikus, Stephen J. Gracheck, James M. Sanders, Steven VanderRoest, Joanne Brodfuehrer, Krishna Iyer, Michael Sinz, Sergei V. Gulnik, and John W. Erickson [Full Article - PDF]

859-872

1,2-Dibenzamidobenzene Inhibitors of Human Factor Xa David K. Herron, Theodore Goodson, Jr., Michael R. Wiley, Leonard C. Weir, Jeffrey A. Kyle, Ying K. Yee, Ann Louise Tebbe, Jennifer M. Tinsley, David Mendel, John J. Masters, Jeffry B. Franciskovich, J. Scott Sawyer, Douglas W. Beight, Andrew M. Ratz, Guy Milot, Steven E. Hall, Valentine J. Klimkowski, James H. Wikel, Brian J. Eastwood, Richard D. Towner, Donetta S. Gifford-Moore, Trelia J. Craft, and Gerald F. Smith [Full Article - PDF]

873-882

N2-Aroylanthranilamide Inhibitors of Human Factor Xa Ying K. Yee, Anne Louise Tebbe, Jared H. Linebarger, Douglas W. Beight, Trelia J. Craft, Donetta Gifford-Moore, Theodore Goodson, Jr., David K. Herron, Valentine J. Klimkowski, Jeffrey A. Kyle, J. Scott Sawyer, Gerald F. Smith, Jennifer M. Tinsley, Richard D. Towner, Leonard Weir, and Michael R. Wiley [Full Article - PDF]

883-899

Structure-Based Design of Potent, Amidine-Derived Inhibitors of Factor Xa: Evaluation of Selectivity, Anticoagulant Activity, and Antithrombotic Activity Michael R. Wiley, Leonard C. Weir, Steven Briggs, Nancy A. Bryan, John Buben, Charles Campbell, Nickolay Y. Chirgadze, Richard C. Conrad, Trelia J. Craft, James V. Ficorilli, Jeffry B. Franciskovich, Larry L. Froelich, Donetta S. Gifford-Moore, Theodore Goodson, Jr., David K. Herron, Valentine J. Klimkowski, Kenneth D. Kurz, Jeffery A. Kyle, John J. Masters, Andrew M. Ratz, Guy Milot, Robert T. Shuman, Tommy Smith, Gerald F. Smith, Ann Louise Tebbe, Jennifer M. Tinsley, Richard D. Towner, Alexander Wilson, and Ying K. Yee [Full Article - PDF]

900-910

Selective ETA Antagonists. 5. Discovery and Structure-Activity Relationships of Phenoxyphenylacetic Acid Derivatives Peter C. Astles, Thomas J. Brown, Frank Halley, Caroline M. Handscombe, Neil V. Harris, Tahir N. Majid, Clive McCarthy, Iain M. McLay, Andrew Morley, Barry Porter, Alan G. Roach, Carol Sargent, Christopher Smith, and Roger J. A. Walsh [Full Article - PDF]

911-920

Inhibition of Grb2 SH2 Domain Binding by Non-Phosphate-Containing Ligands. 2. 4-(2-Malonyl)phenylalanine as a Potent Phosphotyrosyl Mimetic Yang Gao, Juliet Luo, Zhu-Jun Yao, Ribo Guo, Hong Zou, James Kelley, Johannes H. Voigt, Dajun Yang, and Terrence R. Burke, Jr. [Full Article - PDF]

921-944

Conformationally Constrained Analogues of Diacylglycerol (DAG). 16. How Much Structural Complexity Is Necessary for Recognition and High Binding Affinity to Protein Kinase C? Kassoum Nacro, Bruno Bienfait, Jeewoo Lee, Kee-Chung Han, Ji-Hye Kang, Samira Benzaria, Nancy E. Lewin, Dipak K. Bhattacharyya, Peter M. Blumberg, and Victor E. Marquez [Full Article - PDF]

945-952

Design and Synthesis of 13,14-Dihydro Prostaglandin F1 Analogues as Potent and Selective Ligands for the Human FP Receptor Yili Wang, John A. Wos, Michelle J. Dirr, David L. Soper, Mitchell A. deLong, Glen E. Mieling, Biswanath De, Jack S. Amburgey, Eric G. Suchanek, and Cynthia J. Taylor [Full Article - PDF]

953-970

Substituent Effects on the Antibacterial Activity of Nitrogen-Carbon-Linked (Azolylphenyl)oxazolidinones with Expanded Activity Against the Fastidious Gram-Negative Organisms Haemophilus influenzae and Moraxella catarrhalis Michael J. Genin, Debra A. Allwine, David J. Anderson, Michael R. Barbachyn, D. Edward Emmert, Stuart A. Garmon, David R. Graber, Kevin C. Grega, Jackson B. Hester, Douglas K. Hutchinson, Joel Morris, Robert J. Reischer, Charles W. Ford, Gary E. Zurenko, Judith C. Hamel, Ronda D. Schaadt, Douglas Stapert, and Betty H. Yagi [Full Article - PDF]

971-983

Design, Synthesis, and Enzymatic Evaluation of Multisubstrate Analogue Inhibitors of Escherichia coli Thymidine Phosphorylase Antonio Esteban-Gamboa, Jan Balzarini, Robert Esnouf, Erik De Clercq, María-José Camarasa, and María-Jesús Pérez-Pérez [Full Article - PDF]

984-994

Synthesis of N-Substituted 4-(4-Hydroxyphenyl)piperidines, 4-(4-Hydroxybenzyl)piperidines, and (±)-3-(4-Hydroxyphenyl)pyrrolidines: Selective Antagonists at the 1A/2B NMDA Receptor Subtype Anthony P. Guzikowski, Amir P. Tamiz, Manuel Acosta-Burruel, Soo Hong-Bae, Sui Xiong Cai, Jon E. Hawkinson, John F. W. Keana, Suzanne R. Kesten, Christina T. Shipp, Minhtam Tran, Edward R. Whittemore, Richard M. Woodward, Jon L. Wright, and Zhang-Lin Zhou [Full Article - PDF]

995-1010

New Azolidinediones as Inhibitors of Protein Tyrosine Phosphatase 1B with Antihyperglycemic Properties Michael S. Malamas, Janet Sredy, Iwan Gunawan, Brenda Mihan, Diane R. Sawicki, Laura Seestaller, Donald Sullivan, and Brenda R. Flam [Full Article - PDF]

1011-1018

2-Substituted Tryptamines: Agents with Selectivity for 5-HT6 Serotonin Receptors Richard A. Glennon, Mase Lee, Jagadeesh B. Rangisetty, Malgorzata Dukat, Bryan L. Roth, Jason E. Savage, Ace McBride, Laura Rauser, Sandy Hufeisen, and David K. H. Lee [Full Article - PDF]

1019-1028

Monocyclic L-Nucleosides with Type 1 Cytokine-Inducing Activity Kanda S. Ramasamy, Robert C. Tam, Josie Bard, and Devron R. Averett [Full Article - PDF]

BRIEF ARTICLES

1029-1033

N-Terminal Dipeptides of D(-)-Penicillamine as Sequestration Agents for Acetaldehyde Jonathan F. Cohen, James A. Elberling, Eugene G. DeMaster, Renee C. Lin, and Herbert T. Nagasawa [Full Article - PDF]

1034-1040

Novel 1,5-Diphenylpyrazole Nonnucleoside HIV-1 Reverse Transcriptase Inhibitors with Enhanced Activity versus the Delavirdine-Resistant P236L Mutant: Lead Identification and SAR of 3- and 4-Substituted Derivatives Michael J. Genin, Carolyn Biles, Barb J. Keiser, Susan M. Poppe, Steven M. Swaney, W. Gary Tarpley, Yoshihiko Yagi, and Donna L. Romero [Full Article - PDF]