Table of Contents
June 5, 2003
Volume 46, Issue 12
Pages 2261-2550
Perspective
Angiotensin II AT1 Receptor Antagonists. Clinical Implications of Active Metabolites
Boris Schmidt and Bernhard Schieffer
pp 2261–2270Publication Date (Web): May 08, 2003 (Perspective)
DOI: 10.1021/jm0204237
Hi-Res PDF Letters
Isoform-Selective Substrates of Nitric Oxide Synthase
Qiang Jia, Tingwei Cai, Mingchuan Huang, Huiying Li, Ming Xian, Thomas L. Poulos, and Peng G. Wang
pp 2271–2274Publication Date (Web): May 03, 2003 (Letter)
DOI: 10.1021/jm0340703
Design and Synthesis of Highly Potent Benzodiazepine γ-Secretase Inhibitors: Preparation of (2S,3R)-3-(3,4- Difluorophenyl)-2-(4-fluorophenyl)-4- hydroxy-N-((3S)-1-methyl-2-oxo-5- phenyl-2,3-dihydro-1H-benzo[e][1,4]- diazepin-3-yl)butyramide by Use of an Asymmetric Ireland−Claisen Rearrangement
Ian Churcher, Susie Williams, Sonia Kerrad, Timothy Harrison, José L. Castro, Mark S. Shearman, Huw D. Lewis, Earl E. Clarke, Jonathan D. J. Wrigley, Dirk Beher, Yui S. Tang, and Wensheng Liu
pp 2275–2278Publication Date (Web): May 13, 2003 (Letter)
DOI: 10.1021/jm034058a
3-(4-{[Benzyl(methyl)amino]methyl}phenyl)-6,7-dimethoxy-2H-2-chromenone (AP2238) Inhibits Both Acetylcholinesterase and Acetylcholinesterase-Induced β-Amyloid Aggregation: A Dual Function Lead for Alzheimer's Disease Therapy
Lorna Piazzi, Angela Rampa, Alessandra Bisi, Silvia Gobbi, Federica Belluti, Andrea Cavalli, Manuela Bartolini, Vincenza Andrisano, Piero Valenti, and Maurizio Recanatini
pp 2279–2282Publication Date (Web): May 13, 2003 (Letter)
DOI: 10.1021/jm0340602
Letters
A Highly Selective, Non-Hydantoin, Non-Carboxylic Acid Inhibitor of Aldose Reductase with Potent Oral Activity in Diabetic Rat Models: 6-(5-Chloro-3-methylbenzofuran- 2-sulfonyl)-2-H-pyridazin-3-one
Banavara L. Mylari, Sandra J. Armento, David A. Beebe, Edward L. Conn, James B. Coutcher, Michael S. Dina, Melissa T. O'Gorman, Michael C. Linhares, William H. Martin, Peter J. Oates, David A. Tess, Gregory J. Withbroe, and William J. Zembrowski
pp 2283–2286Publication Date (Web): May 10, 2003 (Letter)
DOI: 10.1021/jm034065z
Articles
Comparative Evaluation of 11 Scoring Functions for Molecular Docking
Renxiao Wang, Yipin Lu, and Shaomeng Wang
pp 2287–2303Publication Date (Web): May 08, 2003 (Article)
DOI: 10.1021/jm0203783
Novel Dihydrofolate Reductase Inhibitors. Structure-Based versus Diversity-Based Library Design and High-Throughput Synthesis and Screening
Pierre C. Wyss, Paul Gerber, Peter G. Hartman, Christian Hubschwerlen, Hans Locher, Hans-Peter Marty, and Martin Stahl
pp 2304–2312Publication Date (Web): May 08, 2003 (Article)
DOI: 10.1021/jm020495y
Predicting Drug Metabolism: A Site of Metabolism Prediction Tool Applied to the Cytochrome P450 2C9
Ismael Zamora, Lovisa Afzelius, and Gabriele Cruciani
pp 2313–2324Publication Date (Web): May 10, 2003 (Article)
DOI: 10.1021/jm021104i
Introduction of a Chemical Constraint in a Short Peptide Derived from Human Acidic Fibroblast Growth Factor Elicits Mitogenic Structural Determinants
Sumika Kiyota, Lorella Franzoni, Giuseppe Nicastro, Arianna Benedetti, Sérgio Oyama, Jr., Wládia Viviani, Angelo G. Gambarini, Alberto Spisni, and M. Terêsa M. Miranda
pp 2325–2333Publication Date (Web): May 08, 2003 (Article)
DOI: 10.1021/jm020543e
A Novel Somatostatin Mimic with Broad Somatotropin Release Inhibitory Factor Receptor Binding and Superior Therapeutic Potential
Ian Lewis, Wilfried Bauer, Rainer Albert, Nagarajan Chandramouli, Janos Pless, Gisbert Weckbecker, and Christian Bruns
pp 2334–2344Publication Date (Web): May 13, 2003 (Article)
DOI: 10.1021/jm021093t
Three Dimensional Pharmacophore Modeling of Human CYP17 Inhibitors. Potential Agents for Prostate Cancer Therapy
Omoshile O. Clement, Clive M. Freeman, Rolf W. Hartmann, Venkatesh D. Handratta, Tadas S. Vasaitis, Angela M. H. Brodie, and Vincent C. O. Njar
pp 2345–2351Publication Date (Web): May 10, 2003 (Article)
DOI: 10.1021/jm020576u
Design, Synthesis, and Structure−Activity Relationships of Alkylcarbamic Acid Aryl Esters, a New Class of Fatty Acid Amide Hydrolase Inhibitors
Giorgio Tarzia, Andrea Duranti, Andrea Tontini, Giovanni Piersanti, Marco Mor, Silvia Rivara, Pier Vincenzo Plazzi, Chris Park, Satish Kathuria, and Daniele Piomelli
pp 2352–2360Publication Date (Web): May 10, 2003 (Article)
DOI: 10.1021/jm021119g
Synthesis and Structure−Activity Relationship of α-Sulfonylhydroxamic Acids as Novel, Orally Active Matrix Metalloproteinase Inhibitors for the Treatment of Osteoarthritis
Venkatesan Aranapakam, George T. Grosu, Jamie M. Davis, Baihua Hu, John Ellingboe, Jannie L. Baker, Jerauld S. Skotnicki, Arie Zask, John F. DiJoseph, Amy Sung, Michele A. Sharr, Loran M. Killar, Thomas Walter, Guixian Jin, and Rebecca Cowling
pp 2361–2375Publication Date (Web): May 10, 2003 (Article)
DOI: 10.1021/jm0205548
Synthesis and Structure−Activity Relationship of N-Substituted 4-Arylsulfonylpiperidine-4-hydroxamic Acids as Novel, Orally Active Matrix Metalloproteinase Inhibitors for the Treatment of Osteoarthritis
Venkatesan Aranapakam, Jamie M. Davis, George T. Grosu, Jannie Baker, John Ellingboe, Arie Zask, Jeremy I. Levin, Vincent P. Sandanayaka, Mila Du, Jerauld S. Skotnicki, John F. DiJoseph, Amy Sung, Michele A. Sharr, Loran M. Killar, Thomas Walter, Guixian Jin, Rebecca Cowling, Jeff Tillett, Weiguang Zhao, Joseph McDevitt, and Zhang Bao Xu
pp 2376–2396Publication Date (Web): May 10, 2003 (Article)
DOI: 10.1021/jm0205550
Synthesis of Ethyl 5-Phenyl-6-Oxa-1-Azabicyclo[3.1.0]hexane-2-carboxylate Derivatives and Evaluation of Their Antimalarial Activities
Nongpanga Ningsanont, David St. C. Black, Rachada Chanphen, and Yodhathai Thebtaranonth
pp 2397–2403Publication Date (Web): May 02, 2003 (Article)
DOI: 10.1021/jm020452h
Benzoylalanine-Derived Ketoamides Carrying Vinylbenzyl Amino Residues: Discovery of Potent Water-Soluble Calpain Inhibitors with Oral Bioavailability
Wilfried Lubisch, Edith Beckenbach, Sabina Bopp, Hans-Peter Hofmann, Arzu Kartal, Claudia Kästel, Tanja Lindner, Marion Metz-Garrecht, Jutta Reeb, Ferdinand Regner, Michael Vierling, and Achim Möller
pp 2404–2412Publication Date (Web): May 03, 2003 (Article)
DOI: 10.1021/jm0210717
Optimization of a Tertiary Alcohol Series of Phosphodiesterase-4 (PDE4) Inhibitors: Structure−Activity Relationship Related to PDE4 Inhibition and Human Ether-a-go-go Related Gene Potassium Channel Binding Affinity
Richard W. Friesen, Yves Ducharme, Richard G. Ball, Marc Blouin, Louise Boulet, Bernard Côté, Richard Frenette, Mario Girard, Daniel Guay, Zheng Huang, Thomas R. Jones, France Laliberté, Joseph J. Lynch, Joseph Mancini, Evelyn Martins, Paul Masson, Eric Muise, Douglas J. Pon, Peter K. S. Siegl, Angela Styhler, Nancy N. Tsou, Mervyn J. Turner, Robert N. Young, and Yves Girard
pp 2413–2426Publication Date (Web): May 08, 2003 (Article)
DOI: 10.1021/jm0204542
Modifications to the N-Terminus but Not the C-Terminus of Calcitonin Gene-Related Peptide(8-37) Produce Antagonists with Increased Affinity
D. David Smith, Shankar Saha, Guoyong Fang, Courtney Schaffert, David J. J. Waugh, Wanyun Zeng, Geza Toth, Martin Hulce, and Peter W. Abel
pp 2427–2435Publication Date (Web): May 08, 2003 (Article)
DOI: 10.1021/jm020507f
Synthesis and Biological Activity of Various Derivatives of a Novel Class of Potent, Selective, and Orally Active Prostaglandin D2 Receptor Antagonists. 1. Bicyclo[2.2.1]heptane Derivatives
Susumu Mitsumori, Tatsuo Tsuri, Tsunetoshi Honma, Yoshiharu Hiramatsu, Toshihiko Okada, Hiroshi Hashizume, Masanao Inagaki, Akinori Arimura, Kiyoshi Yasui, Fujio Asanuma, Junji Kishino, and Mitsuaki Ohtani
pp 2436–2445Publication Date (Web): May 10, 2003 (Article)
DOI: 10.1021/jm020517g
Synthesis and Biological Activity of Various Derivatives of a Novel Class of Potent, Selective, and Orally Active Prostaglandin D2 Receptor Antagonists. 2. 6,6-Dimethylbicyclo[3.1.1]heptane Derivatives
Susumu Mitsumori, Tatsuo Tsuri, Tsunetoshi Honma, Yoshiharu Hiramatsu, Toshihiko Okada, Hiroshi Hashizume, Shiro Kida, Masanao Inagaki, Akinori Arimura, Kiyoshi Yasui, Fujio Asanuma, Junji Kishino, and Mitsuaki Ohtani
pp 2446–2455Publication Date (Web): May 10, 2003 (Article)
DOI: 10.1021/jm0205189
Structure−Activity Relationships for 4-Nitrobenzyl Carbamates of 5-Aminobenz[e]indoline Minor Groove Alkylating Agents as Prodrugs for GDEPT in Conjunction with E. coli Nitroreductase
Michael P. Hay, Graham J. Atwell, William R. Wilson, Susan M. Pullen, and William A. Denny
pp 2456–2466Publication Date (Web): May 02, 2003 (Article)
DOI: 10.1021/jm0205191
Discovery and Structure−Activity Relationships of Novel Piperidine Inhibitors of Farnesyltransferase
Shinji Nara, Rieko Tanaka, Jun Eishima, Mitsunobu Hara, Yuichi Takahashi, Shizuo Otaki, Robert J. Foglesong, Philip F. Hughes, Shelley Turkington, and Yutaka Kanda
pp 2467–2473Publication Date (Web): May 02, 2003 (Article)
DOI: 10.1021/jm020522k
Discovery of Substituted N-Phenyl Nicotinamides as Potent Inducers of Apoptosis Using a Cell- and Caspase-Based High Throughput Screening Assay
Sui Xiong Cai, Bao Nguyen, Shaojuan Jia, John Herich, John Guastella, Sanjeeva Reddy, Ben Tseng, John Drewe, and Shailaja Kasibhatla
pp 2474–2481Publication Date (Web): April 29, 2003 (Article)
DOI: 10.1021/jm0205200
Novel Indolyl Aryl Sulfones Active against HIV-1 Carrying NNRTI Resistance Mutations: Synthesis and SAR Studies
Romano Silvestri, Gabriella De Martino, Giuseppe La Regina, Marino Artico, Silvio Massa, Laura Vargiu, Massimo Mura, Anna Giulia Loi, Tiziana Marceddu, and Paolo La Colla
pp 2482–2493Publication Date (Web): May 08, 2003 (Article)
DOI: 10.1021/jm0211063
Design, Synthesis, and Evaluation of Analogues of 3,3,3-Trifluoro-2-Hydroxy-2-Phenyl-Propionamide as Orally Available General Anesthetics
Indrani Choudhury-Mukherjee, Hilary A. Schenck, Sylvia Cechova, Thomas N. Pajewski, Jaideep Kapur, Jeffrey Ellena, David S. Cafiso, and Milton L. Brown
pp 2494–2501Publication Date (Web): May 14, 2003 (Article)
DOI: 10.1021/jm020546r
Neuromuscular Blocking Activity and Therapeutic Potential of Mixed-Tetrahydroisoquinolinium Halofumarates and Halosuccinates in Rhesus Monkeys
Eric E. Boros, Vicente Samano, John A. Ray, James B. Thompson, David K. Jung, Istvan Kaldor, Cecilia S. Koble, Michael T. Martin, Virgil L. Styles, Robert A. Mook, Jr., Paul L. Feldman, John J. Savarese, Matthew R. Belmont, Eric C. Bigham, G. Evan Boswell, Mir A. Hashim, Sanjay S. Patel, James C. Wisowaty, Gary D. Bowers, Caroline L. Moseley, John S. Walsh, Mindy J. Reese, Randy D. Rutkowske, Andrea M. Sefler, and Timothy D. Spitzer
pp 2502–2515Publication Date (Web): May 08, 2003 (Article)
DOI: 10.1021/jm020574+
Full Text HTMLA Short Synthesis and Biological Evaluation of Potent and Nontoxic Antimalarial Bridged Bicyclic β-Sulfonyl-Endoperoxides
Mario D. Bachi, Edward E. Korshin, Roland Hoos, Alex M. Szpilman, Poonsakdi Ploypradith, Suji Xie, Theresa A. Shapiro, and Gary H. Posner
pp 2516–2533Publication Date (Web): May 03, 2003 (Article)
DOI: 10.1021/jm020584a
Synthesis and Antitumor Activity of Novel O-Carbamoylmethyloxime Derivatives of Radicicol
Yoji Ikuina, Nobuyoshi Amishiro, Mayumi Miyata, Hiroaki Narumi, Harumi Ogawa, Tadakazu Akiyama, Yukimasa Shiotsu, Shiro Akinaga, and Chikara Murakata
pp 2534–2541Publication Date (Web): May 10, 2003 (Article)
DOI: 10.1021/jm030110r
Elicitation, a New Window into Plant Chemodiversity and Phytochemical Drug Discovery
Alexander Poulev, Joseph M. O'Neal, Sithes Logendra, Reneta B. Pouleva, Vesa Timeva, Alison S. Garvey, Doloressa Gleba, Ivan S. Jenkins, Barbara T. Halpern, Ralf Kneer, Gordon M. Cragg, and Ilya Raskin
pp 2542–2547Publication Date (Web): May 02, 2003 (Article)
DOI: 10.1021/jm020359t
Brief Articles
Analysis of 6-(2,2-Dichloroacetamido)chrysene Interaction with the Hypoxanthine Phosphoribosyltransferase from Trypanosoma cruzi
Francisco J. Medrano, Mary A. Wenck, Juan C. Engel, and Sydney P. Craig, III
pp 2548–2550Publication Date (Web): May 10, 2003 (Brief Article)
DOI: 10.1021/jm030061i