Journal of Medicinal Chemistry
Volume 44, Issue 3 (February 1, 2001)
Copyright © 2001 American Chemical Society

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PERSPECTIVES

281-297

New Dermatological Agents for the Treatment of Psoriasis Scott M. Thacher, Jayasree Vasudevan, Kwok-Yin Tsang, Sunil Nagpal, and Roshantha A. S. Chandraratna [Full Article - PDF]

298-301

Design of Remarkably Simple, Yet Potent Urea-Based Inhibitors of Glutamate Carboxypeptidase II (NAALADase) Alan P. Kozikowski, Fajun Nan, Paola Conti, Jiazhong Zhang, Epolia Ramadan, Tomasz Bzdega, Barbara Wroblewska, Joseph H. Neale, Sergey Pshenichkin, and Jarda T. Wroblewski [Full Article - PDF]

302-304

[3H]N-2-(4-(N-Benzamido)phenyl)propyl-2- propanesulfonamide: A Novel AMPA Receptor Potentiator and Radioligand Hamideh Zarrinmayeh, David Bleakman, Mary R. Gates, Hong Yu, Dennis M. Zimmerman, Paul L. Ornstein, Tracey McKennon, M. Brian Arnold, William J. Wheeler, and Phil Skolnick [Full Article - PDF]

ARTICLES

305-315

Quinoxalinylethylpyridylthioureas (QXPTs) as Potent Non-Nucleoside HIV-1 Reverse Transcriptase (RT) Inhibitors. Further SAR Studies and Identification of a Novel Orally Bioavailable Hydrazine-Based Antiviral Agent Giuseppe Campiani, Francesca Aiello, Monica Fabbrini, Elena Morelli, Anna Ramunno, Silvia Armaroli, Vito Nacci, Antonio Garofalo, Giovanni Greco, Ettore Novellino, Giovanni Maga, Silvio Spadari, Alberto Bergamini, Laura Ventura, Barbara Bongiovanni, Marcella Capozzi, Francesca Bolacchi, Stefano Marini, Massimiliano Coletta, Giovanna Guiso, and Silvio Caccia [Full Article - PDF]

316-327

3-Aryl[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-ones: A New Class of Selective A1 Adenosine Receptor Antagonists Federico Da Settimo, Giampaolo Primofiore, Sabrina Taliani, Anna Maria Marini, Concettina La Motta, Ettore Novellino, Giovanni Greco, Antonio Lavecchia, Letizia Trincavelli, and Claudia Martini [Full Article - PDF]

328-339

Design, Synthesis, and Modeling of Novel Cyclic Thrombin Receptor-Derived Peptide Analogues of the Ser42-Phe-Leu-Leu-Arg46 Motif Sequence with Fixed Conformations of Pharmacophoric Groups: Importance of a Phe/Arg/NH2 Cluster for Receptor Activation and Implications in the Design of Nonpeptide Thrombin Receptor Mimetics Kostas Alexopoulos, Dimitris Panagiotopoulos, Thomas Mavromoustakos, Panagiotis Fatseas, Maria Christina Paredes-Carbajal, Dieter Mascher, Stefan Mihailescu, and John Matsoukas [Full Article - PDF]

340-349

Structure-Activity Relationships of Pyridoxal Phosphate Derivatives as Potent and Selective Antagonists of P2X1 Receptors Yong-Chul Kim, Sean G. Brown, T. Kendall Harden, José L. Boyer, George Dubyak, Brian F. King, Geoffrey Burnstock, and Kenneth A. Jacobson [Full Article - PDF]

350-361

Synthesis and SAR of a New Series of COX-2-Selective Inhibitors: Pyrazolo[1,5-a]pyrimidines Carmen Almansa, Alberto F. de Arriba, Fernando L. Cavalcanti, Luis A. Gómez, Agustí Miralles, Manuel Merlos, Julián García-Rafanell, and Javier Forn [Full Article - PDF]

362-371

Analogues of Prazosin That Bear a Benextramine-Related Polyamine Backbone Exhibit Different Antagonism toward 1-Adrenoreceptor Subtypes Maria L. Bolognesi, Gabriella Marucci, Piero Angeli, Michela Buccioni, Anna Minarini, Michela Rosini, Vincenzo Tumiatti, and Carlo Melchiorre [Full Article - PDF]

372-389

Behavioral Approach to Nondyskinetic Dopamine Antagonists: Identification of Seroquel Edward J. Warawa, Bernard M. Migler, Cyrus J. Ohnmacht, Ann L. Needles, George C. Gatos, Frances M. McLaren, Cynthia L. Nelson, and Karen M. Kirkland [Full Article - PDF]

390-403

Conformationally Restricted Analogues of 1N,14N-Bisethylhomospermine (BE-4-4-4): Synthesis and Growth Inhibitory Effects on Human Prostate Cancer Cells Aldonia Valasinas, Aparajita Sarkar, Venodhar K. Reddy, Laurence J. Marton, Hirak S. Basu, and Benjamin Frydman [Full Article - PDF]

404-417

Cis-Unsaturated Analogues of 3,8,13,18,23-Pentaazapentacosane (BE-4-4-4-4): Synthesis and Growth Inhibitory Effects on Human Prostate Cancer Cell Lines Venodhar K. Reddy, Aparajita Sarkar, Aldonia Valasinas, Laurence J. Marton, Hirak S. Basu, and Benjamin Frydman [Full Article - PDF]

418-428

New 1-Aryl-3-(4-arylpiperazin-1-yl)propane Derivatives, with Dual Action at 5-HT1A Serotonin Receptors and Serotonin Transporter, as a New Class of Antidepressants Javier Martínez-Esparza, Ana-M. Oficialdegui, Silvia Pérez-Silanes, Begoña Heras, Lara Orús, Juan-A. Palop, Berta Lasheras, Joan Roca, Marisa Mourelle, Ana Bosch, Juan-C. Del Castillo, Rosa Tordera, Joaquín Del Río, and Antonio Monge [Full Article - PDF]

429-440

Tyrosine Kinase Inhibitors. 18. 6-Substituted 4-Anilinoquinazolines and 4-Anilinopyrido[3,4-d]pyrimidines as Soluble, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Jeff B. Smaill, H. D. Hollis Showalter, Hairong Zhou, Alexander J. Bridges, Dennis J. McNamara, David W. Fry, James M. Nelson, Veronika Sherwood, Patrick W. Vincent, Bill J. Roberts, William L. Elliott, and William A. Denny [Full Article - PDF]

441-452

Design, Synthesis, and Biological Evaluation of a Series of Lavendustin A Analogues That Inhibit EGFR and Syk Tyrosine Kinases, as Well as Tubulin Polymerization Fanrong Mu, Stephanie L. Coffing, David J. Riese II, Robert L. Geahlen, Pascal Verdier-Pinard, Ernest Hamel, Jill Johnson, and Mark Cushman [Full Article - PDF]

453-467

GnRH Antagonists: A New Generation of Long Acting Analogues Incorporating p-Ureido-phenylalanines at Positions 5 and 6 Guangcheng Jiang, Jacek Stalewski, Robert Galyean, John Dykert, Claudio Schteingart, Pierre Broqua, Audrey Aebi, Michel L. Aubert, Graeme Semple, Peter Robson, Karen Akinsanya, Robert Haigh, Pierre Riviere, Jerzy Trojnar, Jean Louis Junien, and Jean E. Rivier [Full Article - PDF]

BRIEF ARTICLES

468-471

Synthesis by Chemoselective Ligation and Biological Evaluation of Novel Cell-Permeable PKC- Pseudosubstrate Lipopeptides Dominique Bonnet, Kader Thiam, Estelle Loing, Oleg Melnyk, and Hélène Gras-Masse [Full Article - PDF]

472-474

Calculation of the Hydrophobicity of Platinum Drugs James A. Platts, David E. Hibbs, Trevor W. Hambley, and Matthew D. Hall [Full Article - PDF]

BOOK REVIEWS

475-475

Oral Drug Absorption Prediction and Assessment Edited by Jennifer B. Dressman and Hans Lennermäs. Marcel Dekker, Inc., New York. 2000. x + 330 pp. 16 × 23.5 cm. ISBN 0-8247-0272-7. $165.00. Mark Chasin [Full Article - PDF]

475-476

Seafood and Freshwater Toxins: Pharmacology, Physiology, and Detection Edited by L. M. Botana. Marcel Dekker, New York. 2000. xii + 798 pp. 18.5 × 26 cm. ISBN 0-8247-8956-3. $225.00. J. Paul Hieble [Full Article - PDF]