Table of Contents
August 28, 2003
Volume 46, Issue 18
Pages 3771-3952
About the Cover: Connolly surface map of the X-ray structure of the α-thrombin-cyclopentenedicarboxylic acid derivative complex (yellow) at 1.9 Å resolution superimposed on the X-ray structure of the α-thrombin-PPACK complex (magenta) (Thorstensson, F.; et al. J. Med. Chem. 2003, 46, 1165-1179).
Letters
Structure-Based Design of a Macrocyclic Inhibitor for Peptide Deformylase
Xubo Hu, Kiet T. Nguyen, Christophe L. M. J. Verlinde, Wim G. J. Hol, and Dehua Pei
pp 3771–3774Publication Date (Web): August 05, 2003 (Letter)
DOI: 10.1021/jm034113f
Hi-Res PDFN6-Substituted D-4‘-Thioadenosine-5‘-methyluronamides: Potent and Selective Agonists at the Human A3 Adenosine Receptor
Lak Shin Jeong, Dong Zhe Jin, Hea Ok Kim, Dae Hong Shin, Hyung Ryong Moon, Prashantha Gunaga, Moon Woo Chun, Yong-Chul Kim, Neli Melman, Zhan-Guo Gao, and Kenneth A. Jacobson
pp 3775–3777Publication Date (Web): August 06, 2003 (Letter)
DOI: 10.1021/jm034098e
Fluorine Substitution Can Block CYP3A4 Metabolism-Dependent Inhibition: Identification of (S)-N-[1-(4-Fluoro-3- morpholin-4-ylphenyl)ethyl]-3- (4-fluorophenyl)acrylamide as an Orally Bioavailable KCNQ2 Opener Devoid of CYP3A4 Metabolism-Dependent Inhibition
Yong-Jin Wu, Carl D. Davis, Steven Dworetzky, William C. Fitzpatrick, David Harden, Huan He, Ronald J. Knox, Amy E. Newton, Thomas Philip, Craig Polson, Digavalli V. Sivarao, Li-Qiang Sun, Svetlana Tertyshnikova, David Weaver, Suresh Yeola, Mary Zoeckler, and Michael W. Sinz
pp 3778–3781Publication Date (Web): July 26, 2003 (Letter)
DOI: 10.1021/jm034111v
A Novel Approach of Water-Soluble Paclitaxel Prodrug with No Auxiliary and No Byproduct: Design and Synthesis of Isotaxel
Yoshio Hayashi, Mariusz Skwarczynski, Yoshio Hamada, Youhei Sohma, Tooru Kimura, and Yoshiaki Kiso
pp 3782–3784Publication Date (Web): July 26, 2003 (Letter)
DOI: 10.1021/jm034112n
Articles
Influence of Phenyl Ring Disubstitution on Bisbenzimidazole and Terbenzimidazole Cytotoxicity: Synthesis and Biological Evaluation as Radioprotectors
Urmila Tawar, Akash K. Jain, B. S. Dwarakanath, Ramesh Chandra, Yogendra Singh, N. K. Chaudhury, Divya Khaitan, and Vibha Tandon
pp 3785–3792Publication Date (Web): July 26, 2003 (Article)
DOI: 10.1021/jm030114w
Thalidomide Metabolites and Analogues. 3. Synthesis and Antiangiogenic Activity of the Teratogenic and TNFα-Modulatory Thalidomide Analogue 2-(2,6-Dioxopiperidine-3-yl)phthalimidine1
Frederick A. Luzzio, Alexander V. Mayorov, Sylvia S. W. Ng, Erwin A. Kruger, and William D. Figg
pp 3793–3799Publication Date (Web): July 30, 2003 (Article)
DOI: 10.1021/jm020079d
Novel Pyrone Side Tetracyclic Psoralen Derivatives: Synthesis and Photobiological Evaluation
Lisa Dalla Via, Eugenio Uriarte, Elias Quezada, Alessandro Dolmella, Maria Grazia Ferlin, and Ornella Gia
pp 3800–3810Publication Date (Web): August 06, 2003 (Article)
DOI: 10.1021/jm0210919
3‘-C-Branched-Chain-Substituted Nucleosides and Nucleotides as Potent Inhibitors of Mycobacterium tuberculosis Thymidine Monophosphate Kinase
Veerle Vanheusden, Hélène Munier-Lehmann, Matheus Froeyen, Laurence Dugué, Arne Heyerick, Denis De Keukeleire, Sylvie Pochet, Roger Busson, Piet Herdewijn, and Serge Van Calenbergh
pp 3811–3821Publication Date (Web): August 01, 2003 (Article)
DOI: 10.1021/jm021108n
Synthesis and Pharmacological Evaluation of Potent and Highly Selective D3 Receptor Ligands: Inhibition of Cocaine-Seeking Behavior and the Role of Dopamine D3/D2 Receptors
Giuseppe Campiani, Stefania Butini, Francesco Trotta, Caterina Fattorusso, Bruno Catalanotti, Francesca Aiello, Sandra Gemma, Vito Nacci, Ettore Novellino, Jennifer Ann Stark, Alfredo Cagnotto, Elena Fumagalli, Francesco Carnovali, Luigi Cervo, and Tiziana Mennini
pp 3822–3839Publication Date (Web): July 26, 2003 (Article)
DOI: 10.1021/jm0211220
Stereospecific Synthesis of 5-Substituted 2-Bisarylthiocyclopentane Carboxylic Acids as Specific Matrix Metalloproteinase Inhibitors
Thierry Le Diguarher, Anne-Marie Chollet, Marc Bertrand, Philippe Hennig, Eric Raimbaud, Massimo Sabatini, Nicolas Guilbaud, Alain Pierré, Gordon C. Tucker, and Patrick Casara
pp 3840–3852Publication Date (Web): August 05, 2003 (Article)
DOI: 10.1021/jm0307638
Synthesis, Biological Evaluation, and Receptor Docking Simulations of 2-[(Acylamino)ethyl]-1,4-benzodiazepines as κ-Opioid Receptor Agonists Endowed with Antinociceptive and Antiamnesic Activity
Maurizio Anzini, Laura Canullo, Carlo Braile, Andrea Cappelli, Andrea Gallelli, Salvatore Vomero, M. Cristina Menziani, Pier G. De Benedetti, Milena Rizzo, Simona Collina, Ornella Azzolina, Massimo Sbacchi, Carla Ghelardini, and Nicoletta Galeotti
pp 3853–3864Publication Date (Web): August 06, 2003 (Article)
DOI: 10.1021/jm0307640
Potent, Small-Molecule Inhibitors of Human Mast Cell Tryptase. Antiasthmatic Action of a Dipeptide-Based Transition-State Analogue Containing a Benzothiazole Ketone
Michael J. Costanzo, Stephen C. Yabut, Harold R. Almond, Jr., Patricia Andrade-Gordon, Thomas W. Corcoran, Lawrence de Garavilla, Jack A. Kauffman, William M. Abraham, Rosario Recacha, Debashish Chattopadhyay, and Bruce E. Maryanoff
pp 3865–3876Publication Date (Web): August 05, 2003 (Article)
DOI: 10.1021/jm030050p
Oxindole-Based Compounds Are Selective Inhibitors of Plasmodium falciparum Cyclin Dependent Protein Kinases
Cassandra L. Woodard, Zhiyu Li, April K. Kathcart, James Terrell, Lucia Gerena, Miriam Lopez-Sanchez, Dennis E. Kyle, Apurba K. Bhattacharjee, Daniel A. Nichols, William Ellis, Sean T. Prigge, Jeanne A. Geyer, and Norman C. Waters
pp 3877–3882Publication Date (Web): July 26, 2003 (Article)
DOI: 10.1021/jm0300983
N-(ω-(4-(2-Methoxyphenyl)piperazin-1-yl)alkyl)carboxamides as Dopamine D2 and D3 Receptor Ligands
Anneke Hackling, Robin Ghosh, Sylvie Perachon, André Mann, Hans-Dieter Höltje, Camille G. Wermuth, Jean-Charles Schwartz, Wolfgang Sippl, Pierre Sokoloff, and Holger Stark
pp 3883–3899Publication Date (Web): July 26, 2003 (Article)
DOI: 10.1021/jm030836n
Synthesis and Biological Evaluation of Novel Flavone-8-acetic Acid Derivatives as Reversible Inhibitors of Aminopeptidase N/CD13
Brigitte Bauvois, Marie-Line Puiffe, Jean-Bernard Bongui, Sandrine Paillat, Claude Monneret, and Daniel Dauzonne
pp 3900–3913Publication Date (Web): August 06, 2003 (Article)
DOI: 10.1021/jm021109f
DNA Binding Ligands Targeting Drug-Resistant Bacteria: Structure, Activity, and Pharmacology
Jacob A. Kaizerman, Matthew I. Gross, Yigong Ge, Sarah White, Wenhao Hu, Jian-Xin Duan, Eldon E. Baird, Kirk W. Johnson, Richard D. Tanaka, Heinz E. Moser, and Roland W. Bürli
pp 3914–3929Publication Date (Web): August 06, 2003 (Article)
DOI: 10.1021/jm030097a
Binding of Tetrahydrocarboline Derivatives at Human 5-HT5A Receptors
Nantaka Khorana, Carol Smith, Kathy Herrick-Davis, Anil Purohit, Milt Teitler, Brian Grella, Małgorzata Dukat, and Richard A. Glennon
pp 3930–3937Publication Date (Web): July 26, 2003 (Article)
DOI: 10.1021/jm030080s
A New Class of Diamine-Based Human Histamine H3 Receptor Antagonists: 4-(Aminoalkoxy)benzylamines
Richard Apodaca, Curt A. Dvorak, Wei Xiao, Ann J. Barbier, Jamin D. Boggs, Sandy J. Wilson, Timothy W. Lovenberg, and Nicholas I. Carruthers
pp 3938–3944Publication Date (Web): July 23, 2003 (Article)
DOI: 10.1021/jm030185v
Pyrazole Derivatives as Partial Agonists for the Nicotinic Acid Receptor
T. van Herk, J. Brussee, A. M. C. H. van den Nieuwendijk, P. A. M. van der Klein, A. P. IJzerman, C. Stannek, A. Burmeister, and A. Lorenzen
pp 3945–3951Publication Date (Web): August 01, 2003 (Article)
DOI: 10.1021/jm030888c
Book Reviews
p 3952
Publication Date (Web): August 02, 2003 (Book Review)
DOI: 10.1021/jm0303047