Table of Contents
September 26, 2002
Volume 45, Issue 20
Pages 4379-4588
About the Cover: Model of the histone deacetylase inhibitor, 3-(4-benzoyl-1-methyl-1H-2-pyrrole)-N-hydroxy-
Letters
6-Aryl-1,4-dihydro-benzo[d][1,3]oxazin- 2-ones: A Novel Class of Potent, Selective, and Orally Active Nonsteroidal Progesterone Receptor Antagonists
Puwen Zhang, Eugene A. Terefenko, Andrew Fensome, Jay Wrobel, Richard Winneker, Scott Lundeen, Keith B. Marschke, and Zhiming Zhang
pp 4379–4382Publication Date (Web): August 27, 2002 (Letter)
DOI: 10.1021/jm025555e
Hi-Res PDFEthyl (3S,4aR,6S,8aR)-6-(4-Ethoxycar- bonylimidazol-1-ylmethyl)decahydroiso- quinoline-3-carboxylic Ester: A Prodrug of a GluR5 Kainate Receptor Antagonist Active in Two Animal Models of Acute Migraine
Sandra A. Filla, Mark A. Winter, Kirk W. Johnson, David Bleakman, Michael G. Bell, Thomas J. Bleisch, Ana M. Castaño, Amy Clemens-Smith, Miriam del Prado, Donna K. Dieckman, Esteban Dominguez, Ana Escribano, Ken H. Ho, Kevin J. Hudziak, Mary A. Katofiasc, Jose A. Martinez-Perez, Ana Mateo, Brian M. Mathes, Edward L. Mattiuz, Ann Marie L. Ogden, Lee A. Phebus, Douglas R. Stack, Robert E. Stratford, and Paul L. Ornstein
pp 4383–4386Publication Date (Web): August 24, 2002 (Letter)
DOI: 10.1021/jm025548q
New Templates for Syntheses of Ring-Fused, C10 β-Turn Peptidomimetics Leading to the First Reported Small-Molecule Mimic of Neurotrophin-3
Mookda Pattarawarapan, Maria Clara Zaccaro, Uri H. Saragovi, and Kevin Burgess
pp 4387–4390Publication Date (Web): August 21, 2002 (Letter)
DOI: 10.1021/jm0255421
A New, Potent Urotensin II Receptor Peptide Agonist Containing a Pen Residue at the Disulfide Bridge
Paolo Grieco, Alfonso Carotenuto, Pietro Campiglia, Enrico Zampelli, Riccardo Patacchini, Carlo A. Maggi, Ettore Novellino, and Paolo Rovero
pp 4391–4394Publication Date (Web): September 04, 2002 (Letter)
DOI: 10.1021/jm025549i
N-[3-(1H-Imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),1 a Novel α1-Adrenoceptor Ligand with an Enhanced in Vitro and in Vivo Profile Relative to Phenylpropanolamine and Midodrine
Robert J. Altenbach, Albert Khilevich, Michael D. Meyer, Steven A. Buckner, Ivan Milicic, Anthony V. Daza, Michael E. Brune, Alyssa B. O'Neill, Donna M. Gauvin, John C. Cain, Masaki Nakane, Mark W. Holladay, Michael Williams, Jorge D. Brioni, and James P. Sullivan
pp 4395–4397Publication Date (Web): August 22, 2002 (Letter)
DOI: 10.1021/jm025550h
A Sorbitol Dehydrogenase Inhibitor of Exceptional in Vivo Potency with a Long Duration of Action: 1-(R)-{4-[4-(4,6-Dimethyl[1,3,5]triazin-2-yl)- 2R,6S-dimethylpiperazin-1-yl]pyrimidin-2- yl}ethanol
Banavara L. Mylari, Peter J. Oates, William J. Zembrowski, David A. Beebe, Edward L. Conn, James B. Coutcher, Melissa T. O'Gorman, Michael C. Linhares, and Gregory J. Withbroe
pp 4398–4401Publication Date (Web): August 30, 2002 (Letter)
DOI: 10.1021/jm020288y
Articles
General Pseudoreceptor Model for Sweet Compounds: A Semiquantitative Prediction of Binding Affinity for Sweet-Tasting Molecules
Angela Bassoli, Michael G. B. Drew, Lucio Merlini, and Gabriella Morini
pp 4402–4409Publication Date (Web): August 24, 2002 (Article)
DOI: 10.1021/jm020833v
Angiotensin II vs Its Type I Antagonists: Conformational Requirements for Receptor Binding Assessed from NMR Spectroscopic and Receptor Docking Experiments
Brian C. Wilkes, Laurent Masaro, Peter W. Schiller, and Katharine A. Carpenter
pp 4410–4418Publication Date (Web): August 22, 2002 (Article)
DOI: 10.1021/jm0103155
Unique Overlap in the Prerequisites for Thrombin Inhibition and Oral Bioavailability Resulting in Potent Oral Antithrombotics
Anton E. P. Adang, Adrianus P. A. de Man, Gerard M. T. Vogel, Peter D. J. Grootenhuis, Martin J. Smit, Co A. M. Peters, Arie Visser, Jos B. M. Rewinkel, Theo van Dinther, Hans Lucas, Jan Kelder, Sjoerd van Aelst, Dick G. Meuleman, and Constant A. A. van Boeckel
pp 4419–4432Publication Date (Web): August 30, 2002 (Article)
DOI: 10.1021/jm011110z
Novel Potent AMPA/Kainate Receptor Antagonists: Synthesis and Anticonvulsant Activity of a Series of 2-[(4-Alkylsemicarbazono)-(4-amino- phenyl)methyl]-4,5-methylenedioxyphenylacetic Acid Alkyl Esters
Nicola Micale, Maria Zappalà, Silvana Grasso, Giulia Puja, Giovambattista De Sarro, Guido Ferreri, Angela De Sarro, Lucio Toma, and Carlo De Micheli
pp 4433–4442Publication Date (Web): August 24, 2002 (Article)
DOI: 10.1021/jm020863y
Discovery and SAR of a Novel Selective and Orally Bioavailable Nonpeptide Classical Competitive Inhibitor Class of Protein-Tyrosine Phosphatase 1B
Henrik Sune Andersen, Ole H. Olsen, Lars F. Iversen, Anette L. P. Sørensen, Steen B. Mortensen, Michael S. Christensen, Sven Branner, Thomas K. Hansen, Jesper F. Lau, Lone Jeppesen, Edmond J. Moran, Jing Su, Farid Bakir, Luke Judge, Manou Shahbaz, Tassie Collins, Todd Vo, Michael J. Newman, William C. Ripka, and Niels Peter H. Møller
pp 4443–4459Publication Date (Web): August 24, 2002 (Article)
DOI: 10.1021/jm0209026
Interaction of Designed Sulfated Flavanoids with Antithrombin: Lessons on the Design of Organic Activators
Gunnar T. Gunnarsson and Umesh R. Desai
pp 4460–4470Publication Date (Web): August 27, 2002 (Article)
DOI: 10.1021/jm020132y
Structural Determinants of A3 Adenosine Receptor Activation: Nucleoside Ligands at the Agonist/Antagonist Boundary
Zhan-Guo Gao, Soo-Kyung Kim, Thibaud Biadatti, Wangzhong Chen, Kyeong Lee, Dov Barak, Seong Gon Kim, Carl R. Johnson, and Kenneth A. Jacobson
pp 4471–4484Publication Date (Web): August 27, 2002 (Article)
DOI: 10.1021/jm020211+
Full Text HTMLAntitumor AHMA Linked to DNA Minor Groove Binding Agents: Synthesis and Biological Evaluation
Kamesh Rastogi, Jang-Yang Chang, Wen-Yu Pan, Ching-Huang Chen, Ting-Chao Chou, Li-Tzong Chen, and Tsann-Long Su
pp 4485–4493Publication Date (Web): August 21, 2002 (Article)
DOI: 10.1021/jm0200714
Antimicrobial Peptides: Synthesis and Antibacterial Activity of Linear and Cyclic Drosocin and Apidaecin 1b Analogues
Marina Gobbo, Laura Biondi, Fernando Filira, Renato Gennaro, Monica Benincasa, Barbara Scolaro, and Raniero Rocchi
pp 4494–4504Publication Date (Web): August 27, 2002 (Article)
DOI: 10.1021/jm020861d
Enhancement of Nucleoside Cytotoxicity through Nucleotide Prodrugs
Jerry D. Rose, William B. Parker, Hitoshi Someya, Sue C. Shaddix, John A. Montgomery, and John A. Secrist III
pp 4505–4512Publication Date (Web): August 24, 2002 (Article)
DOI: 10.1021/jm020107s
Potent and Selective Inhibitors of PDGF Receptor Phosphorylation. 2. Synthesis, Structure Activity Relationship, Improvement of Aqueous Solubility, and Biological Effects of 4-[4-(N-Substituted (thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline Derivatives
Kenji Matsuno, Takao Nakajima, Michio Ichimura, Neill A. Giese, Jin-Chen Yu, Nathalie A. Lokker, Junko Ushiki, Shin-ichi Ide, Shoji Oda, and Yuji Nomoto
pp 4513–4523Publication Date (Web): August 27, 2002 (Article)
DOI: 10.1021/jm0201114
Coupling of a Competitive and an Irreversible Ligand Generates Mixed Type Inhibitors of Trypanosoma cruzi Trypanothione Reductase
Oliver Inhoff, Jonathan M. Richards, Jan Willem Brîet, Gordon Lowe, and R. Luise Krauth-Siegel
pp 4524–4530Publication Date (Web): August 27, 2002 (Article)
DOI: 10.1021/jm020885k
Inactivation and Inhibition of γ-Aminobutyric Acid Aminotransferase by Conformationally Restricted Vigabatrin Analogues
Sun Choi and Richard B. Silverman
pp 4531–4539Publication Date (Web): August 28, 2002 (Article)
DOI: 10.1021/jm020134i
Design, Synthesis, and Immunostimulatory Properties of CpG DNAs Containing Alkyl-Linker Substitutions: Role of Nucleosides in the Flanking Sequences
Dong Yu, Ekambar R. Kandimalla, Yanping Cong, Jimmy Tang, Jin-Yan Tang, Qiuyan Zhao, and Sudhir Agrawal
pp 4540–4548Publication Date (Web): August 06, 2002 (Article)
DOI: 10.1021/jm0201619
Salen−Manganese Complexes as Catalytic Scavengers of Hydrogen Peroxide and Cytoprotective Agents: Structure−Activity Relationship Studies
Susan R. Doctrow, Karl Huffman, Catherine Bucay Marcus, Georges Tocco, Evelyne Malfroy, Christy A. Adinolfi, Henry Kruk, Keith Baker, Natalie Lazarowych, Julius Mascarenhas, and Bernard Malfroy
pp 4549–4558Publication Date (Web): August 28, 2002 (Article)
DOI: 10.1021/jm020207y
4-Substituted d-Glutamic Acid Analogues: The First Potent Inhibitors of Glutamate Racemase (MurI) Enzyme with Antibacterial Activity
Alfonso de Dios, Lourdes Prieto, Jose Alfredo Martín, Almudena Rubio, Jesus Ezquerra, Mark Tebbe, Beatriz López de Uralde, Justina Martín, Ana Sánchez, Deborah L. LeTourneau, James E. McGee, Carole Boylan, Thomas R. Parr, Jr., and Michele C. Smith
pp 4559–4570Publication Date (Web): August 29, 2002 (Article)
DOI: 10.1021/jm020901d
Synthesis of Novel 4,1-Benzoxazepine Derivatives as Squalene Synthase Inhibitors and Their Inhibition of Cholesterol Synthesis
Takashi Miki, Masakuni Kori, Hiroshi Mabuchi, Ryu-ichi Tozawa, Tomoyuki Nishimoto, Yasuo Sugiyama, Koichiro Teshima, and Hidefumi Yukimasa
pp 4571–4580Publication Date (Web): August 30, 2002 (Article)
DOI: 10.1021/jm020234o
Brief Articles
Dicarboxylic Acid bis(l-Prolyl-pyrrolidine) Amides as Prolyl Oligopeptidase Inhibitors
Erik A. A. Wallén, Johannes A. M. Christiaans, Markus M. Forsberg, Jarkko I. Venäläinen, Pekka T. Männistö, and Jukka Gynther
pp 4581–4584Publication Date (Web): August 27, 2002 (Brief Article)
DOI: 10.1021/jm020966g
Book Reviews
Integrated Drug Discovery Technologies Edited by Houng-Yau Mei and Anthony W. Czarnik. Marcel Dekker, Inc., New York. 2002. xii + 577 pp. 16 × 24 cm. ISBN 0-8247-0649-8. $175.
Carl Kaiser
p 4585Publication Date (Web): August 24, 2002 (Book Review)
DOI: 10.1021/jm020304r
Chinese and Related North American Herbs: Phytopharmacology and Therapeutic Values By Thomas S. C. Li. CRC Press, Boca Raton, FL. 2002. iv + 589 pp. 16 × 24 cm. $169.95 ISBN 1-58716-128-1. $169.95.
Chi-Tang Ho
pp 4585–4586Publication Date (Web): August 24, 2002 (Book Review)
DOI: 10.1021/jm0203074
p 4587
Publication Date (Web): August 22, 2002 (Book Review)
DOI: 10.1021/jm020308w
Additions and Corrections
Modification of the Structure of a Metallopeptide: Synthesis and Biological Evaluation of 111In-Labeled DOTA-Conjugated Rhenium-Cyclized α-MSH Analogues.
Zhen Cheng, Jianqing Chen, Yubin Miao, Nellie K. Owen, Thomas P. Quinn, and Silvia S. Jurisson:
p 4588Publication Date (Web): August 21, 2002 (Addition/Correction)
DOI: 10.1021/jm020331h