Table of Contents
May 19, 2005
Volume 48, Issue 10
Pages 3449-3661
About the Cover: Interaction of the β-L-enantiomer of a 4'-C-ethynyl-2',3'-dideoxynucleoside analogue (ent-14-TP) at the active site of HIV reverse transcriptase (Siddiqui, M. A.; et al. J. Med. Chem. 2004, 47, 5041-5048).
Perspective
The Next Generation of Phosphodiesterase Inhibitors: Structural Clues to Ligand and Substrate Selectivity of Phosphodiesterases
David T. Manallack, Richard A. Hughes, and Philip E. Thompson
pp 3449–3462Publication Date (Web): April 09, 2005 (Perspective)
DOI: 10.1021/jm040217u
Hi-Res PDF Letters
Structure-Based Virtual Screening for Plant-Based ERβ-Selective Ligands as Potential Preventative Therapy against Age-Related Neurodegenerative Diseases
Liqin Zhao and Roberta D. Brinton
pp 3463–3466Publication Date (Web): April 26, 2005 (Letter)
DOI: 10.1021/jm0490538
Synthesis and Biological Evaluation of Benzodioxanylpiperazine Derivatives as Potent Serotonin 5-HT1A Antagonists: The Discovery of Lecozotan
Wayne E. Childers, Jr., Magid A. Abou-Gharbia, Michael G. Kelly, Terrance H. Andree, Boyd L. Harrison, Douglas M. Ho, Geoffrey Hornby, Donna M. Huryn, Lisa Potestio, Sharon J. Rosenzweig-Lipson, Jean Schmid, Deborah L. Smith, Stacey J. Sukoff, Gan Zhang, and Lee E. Schechter
pp 3467–3470Publication Date (Web): April 16, 2005 (Letter)
DOI: 10.1021/jm049493z
Oxazine 170 Induces DNA:RNA:DNA Triplex Formation
Guangtao Song, Feifei Xing, Xiaogang Qu, Jonathan B. Chaires, and Jinsong Ren
pp 3471–3473Publication Date (Web): April 19, 2005 (Letter)
DOI: 10.1021/jm050131g
Varenicline: An α4β2 Nicotinic Receptor Partial Agonist for Smoking Cessation
Jotham W. Coe, Paige R. Brooks, Michael G. Vetelino, Michael C. Wirtz, Eric P. Arnold, Jianhua Huang, Steven B. Sands, Thomas I. Davis, Lorraine A. Lebel, Carol B. Fox, Alka Shrikhande, James H. Heym, Eric Schaeffer, Hans Rollema, Yi Lu, Robert S. Mansbach, Leslie K. Chambers, Charles C. Rovetti, David W. Schulz, F. David Tingley, III, and Brian T. O'Neill
pp 3474–3477Publication Date (Web): April 23, 2005 (Letter)
DOI: 10.1021/jm050069n
Discovery of the First Potent, Selective 5-Hydroxytryptamine1D Receptor Antagonist
Simon E. Ward, Frank P. Harrington, Laurie J. Gordon, Susanna C. Hopley, Claire M. Scott, and Jeannette M. Watson
pp 3478–3480Publication Date (Web): April 23, 2005 (Letter)
DOI: 10.1021/jm049039v
Articles
Synthesis and Structure−Activity-Relationships of 1H-Imidazo[4,5-c]quinolines That Induce Interferon Production
John F. Gerster, Kyle J. Lindstrom, Richard L. Miller, Mark A. Tomai, Woubalem Birmachu, Shannon N. Bomersine, Shiela J. Gibson, Linda M. Imbertson, Joel R. Jacobson, Roy T. Knafla, Peter V. Maye, Nickolas Nikolaides, Folakemi Y. Oneyemi, Gwen J. Parkhurst, Sharon E. Pecore, Michael J. Reiter, Lisa S. Scribner, Tracy L. Testerman, Natalie J. Thompson, Tammy L. Wagner, Charles E. Weeks, Jean-Denis Andre, Daniel Lagain, Yvon Bastard, and Michel Lupu
pp 3481–3491Publication Date (Web): April 21, 2005 (Article)
DOI: 10.1021/jm049211v
Effect on KATP Channel Activation Properties and Tissue Selectivity of the Nature of the Substituent in the 7- and the 3-Position of 4H-1,2,4-Benzothiadiazine 1,1-Dioxides
Stéphane Boverie, Marie-Hélène Antoine, Fabian Somers, Bénédicte Becker, Sophie Sebille, Raogo Ouedraogo, Stéphane Counerotte, Bernard Pirotte, Philippe Lebrun, and Pascal de Tullio
pp 3492–3503Publication Date (Web): April 22, 2005 (Article)
DOI: 10.1021/jm0311339
Application of Phosphoramidate Pronucleotide Technology to Abacavir Leads to a Significant Enhancement of Antiviral Potency
Christopher McGuigan, Sarah A. Harris, Susan M. Daluge, Kristjan S. Gudmundsson, Ed W. McLean, Thimysta C. Burnette, Harry Marr, Richard Hazen, Lynn D. Condreay, Lance Johnson, Erik De Clercq, and Jan Balzarini
pp 3504–3515Publication Date (Web): April 16, 2005 (Article)
DOI: 10.1021/jm0491400
Novel Synthesis, Cytotoxic Evaluation, and Structure−Activity Relationship Studies of a Series of α-Alkylidene-γ-lactones and Lactams
Tomasz Janecki, Edyta Błaszczyk, Kazimierz Studzian, Anna Janecka, Urszula Krajewska, and Marek Różalski
pp 3516–3521Publication Date (Web): April 16, 2005 (Article)
DOI: 10.1021/jm048970a
Design, Synthesis, and Antipicornavirus Activity of 1-[5-(4-Arylphenoxy)alkyl]-3-pyridin-4-ylimidazolidin-2-one Derivatives
Chih-Shiang Chang, Ying-Ting Lin, Shin-Ru Shih, Chung-Chi Lee, Yen-Chun Lee, Chia-Liang Tai, Sung-Nien Tseng, and Jyh-Haur Chern
pp 3522–3535Publication Date (Web): April 19, 2005 (Article)
DOI: 10.1021/jm050033v
Early Absorption and Distribution Analysis of Antitumor and Anti-AIDS Drugs: Lipid Membrane and Plasma Protein Interactions
Samanta Cimitan, Maria T. Lindgren, Carlo Bertucci, and U. Helena Danielson
pp 3536–3546Publication Date (Web): April 15, 2005 (Article)
DOI: 10.1021/jm049343o
AFMoC Enhances Predictivity of 3D QSAR: A Case Study with DOXP-reductoisomerase
Katrin Silber, Philipp Heidler, Thomas Kurz, and Gerhard Klebe
pp 3547–3563Publication Date (Web): April 16, 2005 (Article)
DOI: 10.1021/jm0491501
Further Studies on the Interaction of the 5-Hydroxytryptamine3 (5-HT3) Receptor with Arylpiperazine Ligands. Development of a New 5-HT3 Receptor Ligand Showing Potent Acetylcholinesterase Inhibitory Properties
Andrea Cappelli, Andrea Gallelli, Monica Manini, Maurizio Anzini, Laura Mennuni, Francesco Makovec, M. Cristina Menziani, Stefano Alcaro, Francesco Ortuso, and Salvatore Vomero
pp 3564–3575Publication Date (Web): April 16, 2005 (Article)
DOI: 10.1021/jm0493461
Structure-Based Design: Synthesis and Biological Evaluation of a Series of Novel Cycloamide-Derived HIV-1 Protease Inhibitors
Arun K. Ghosh, Lisa M. Swanson, Hanna Cho, Sofiya Leshchenko, Khaja Azhar Hussain, Stephanie Kay, D. Eric Walters, Yasuhiro Koh, and Hiroaki Mitsuya
pp 3576–3585Publication Date (Web): April 15, 2005 (Article)
DOI: 10.1021/jm050019i
Synthesis and Structure−Activity Relationships of Novel Selective Factor Xa Inhibitors with a Tetrahydroisoquinoline Ring
Hiroshi Ueno, Katsuyuki Yokota, Jun-ichi Hoshi, Katsutaka Yasue, Mikio Hayashi, Yasunori Hase, Itsuo Uchida, Kazuo Aisaka, Susumu Katoh, and Hidetsura Cho
pp 3586–3604Publication Date (Web): April 21, 2005 (Article)
DOI: 10.1021/jm058160e
Methyl Substitution of 2-Aminobicyclo[3.1.0]hexane 2,6-Dicarboxylate (LY354740) Determines Functional Activity at Metabotropic Glutamate Receptors: Identification of a Subtype Selective mGlu2 Receptor Agonist
Carmen Dominguez, Lourdes Prieto, Matthew J. Valli, Steven M. Massey, Mark Bures, Rebecca A. Wright, Bryan G. Johnson, Sherri L. Andis, Ann Kingston, Darryle D. Schoepp, and James A. Monn
pp 3605–3612Publication Date (Web): April 22, 2005 (Article)
DOI: 10.1021/jm040222y
Stereoselective Binding of Indomethacin Ethanolamide Derivatives to Cyclooxygenase-1
Christopher W. Moth, Jeffrey J. Prusakiewicz, Larry J. Marnett, and Terry P. Lybrand
pp 3613–3620Publication Date (Web): April 23, 2005 (Article)
DOI: 10.1021/jm0494164
Optimization of Amide-Based Inhibitors of Soluble Epoxide Hydrolase with Improved Water Solubility
In-Hae Kim, Fenton R. Heirtzler, Christophe Morisseau, Kosuke Nishi, Hsing-Ju Tsai, and Bruce D. Hammock
pp 3621–3629Publication Date (Web): April 22, 2005 (Article)
DOI: 10.1021/jm0500929
N-Methylsansalvamide A Peptide Analogues. Potent New Antitumor Agents
Shouxin Liu, Wenxin Gu, Denise Lo, Xian-Zhong Ding, Michael Ujiki, Thomas E. Adrian, Gerald A. Soff, and Richard B. Silverman
pp 3630–3638Publication Date (Web): April 22, 2005 (Article)
DOI: 10.1021/jm048952t
Brief Articles
Mono- and Bis-Thiazolium Salts Have Potent Antimalarial Activity
Abdallah Hamzé, Eric Rubi, Pascal Arnal, Michel Boisbrun, Carole Carcel, Xavier Salom-Roig, Marjorie Maynadier, Sharon Wein, Henri Vial, and Michèle Calas
pp 3639–3643Publication Date (Web): April 15, 2005 (Brief Article)
DOI: 10.1021/jm0492608
A New Structural Motif for μ-Opioid Antagonists
Isabelle Van den Eynde, Georges Laus, Peter W. Schiller, Piotr Kosson, Nga N. Chung, Andrzej W. Lipkowski, and Dirk Tourwé
pp 3644–3648Publication Date (Web): April 23, 2005 (Brief Article)
DOI: 10.1021/jm0491795
Are l-Adenosine and Its Derivatives Substrates for S-Adenosyl-l-homocysteine Hydrolase?
Mengmeng Wang, Jinsong Zhang, Daniela Andrei, Krzysztof Kuczera, Ronald T. Borchardt, and Stanislaw F. Wnuk
pp 3649–3653Publication Date (Web): April 21, 2005 (Brief Article)
DOI: 10.1021/jm0490484
Synthesis and Evaluation of New Antimalarial Phenylurenyl Chalcone Derivatives
José N. Domínguez, Caritza León, Juan Rodrigues, Neira Gamboa de Domínguez, Jiri Gut, and Philip J. Rosenthal
pp 3654–3658Publication Date (Web): April 21, 2005 (Brief Article)
DOI: 10.1021/jm058208o
Book Reviews
Science of Synthesis: Houben−Weyl Methods of Molecular Transformation Georg Thieme Verlag, Stuttgart, Germany. 2005. 41627 pp. URL: http://www.science-of-synthesis.com (Electronic Version, 48 Volumes). Price Based on Web Site and Number of Users.
Patrick M. Woster
pp 3659–3660Publication Date (Web): April 16, 2005 (Book Review)
DOI: 10.1021/jm058203r
Chromatography. Concepts and Contrasts. 2nd Edition By James M. Miller. Wiley-Interscience, Hoboken, NJ. 2005. xiv + 490 pp. 16 × 24 cm. ISBN 04714-7207-7. $94.50.
Bruce L. Currie
p 3660Publication Date (Web): April 19, 2005 (Book Review)
DOI: 10.1021/jm0582120
Molecular Diversity and Combinatorial Chemistry. Principles and Applications By Michael C. Pirrung. Elsevier, New York. 2004. xiii + 175 pp. 16.5 × 24 cm. ISBN 0-08-044532-2. $60.00.
Lester A. Mitscher
pp 3660–3661Publication Date (Web): April 26, 2005 (Book Review)
DOI: 10.1021/jm058218p