Table of Contents
March 28, 2002
Volume 45, Issue 7
Pages 1395-1542
Letters
Design, Synthesis, and Evaluation of Opioid Analogues with Non-Peptidic β-Turn Scaffold: Enkephalin and Endomorphin Mimetics
Masakatsu Eguchi, Richard Y. W. Shen, J. Paul Shea, Min S. Lee, and Michael Kahn
pp 1395–1398Publication Date (Web): March 03, 2002 (Letter)
DOI: 10.1021/jm0155897
Hi-Res PDFToward Selective ERβ Agonists for Central Nervous System Disorders: Synthesis and Characterization of Aryl Benzthiophenes
Ulrich Schopfer, Philippe Schoeffter, Serge F. Bischoff, Joachim Nozulak, Dominik Feuerbach, and Philipp Floersheim
pp 1399–1401Publication Date (Web): February 26, 2002 (Letter)
DOI: 10.1021/jm015577l
Articles
Identification of Novel Cyclooxygenase-2 Selective Inhibitors Using Pharmacophore Models
Albert Palomer, Francesc Cabré, Jaume Pascual, Joaquín Campos, María A. Trujillo, Antonio Entrena, Miguel A. Gallo, Lluïsa García, David Mauleón, and Antonio Espinosa
pp 1402–1411Publication Date (Web): February 26, 2002 (Article)
DOI: 10.1021/jm010458r
Molecular Dynamics and Free Energy Analyses of Cathepsin D−Inhibitor Interactions: Insight into Structure-Based Ligand Design
Shuanghong Huo, Junmei Wang, Piotr Cieplak, Peter A. Kollman, and Irwin D. Kuntz
pp 1412–1419Publication Date (Web): March 01, 2002 (Article)
DOI: 10.1021/jm010338j
Studies on the Mechanism of Hypoxic Selectivity in Copper Bis(Thiosemicarbazone) Radiopharmaceuticals
Richard I. Maurer, Philip J. Blower, Jonathan R. Dilworth, Christopher A. Reynolds, Yifan Zheng, and Gregory E. D. Mullen
pp 1420–1431Publication Date (Web): March 21, 2002 (Article)
DOI: 10.1021/jm0104217
Hydroxyethylamine Isostere of an HIV-1 Protease Inhibitor Prefers Its Amine to the Hydroxy Group in Binding to Catalytic Aspartates. A Synchrotron Study of HIV-1 Protease in Complex with a Peptidomimetic Inhibitor
Jan Dohnálek, Jindřich Hašek, Jarmila Dušková, and Hana PetrokováMartin Hradilek, Milan Souček, and Jan KonvalinkaJiří Brynda, Juraj Sedláček, and Milan Fábry
pp 1432–1438Publication Date (Web): February 22, 2002 (Article)
DOI: 10.1021/jm010979e
Structural Basis for the Glucocorticoid Response in a Mutant Human Androgen Receptor (ARccr) Derived from an Androgen-Independent Prostate Cancer
Pedro M. Matias, Maria Arménia Carrondo, Ricardo Coelho, Monica Thomaz, Xiao-Yan Zhao, Anja Wegg, Kerstin Crusius, Ursula Egner, and Peter Donner
pp 1439–1446Publication Date (Web): February 26, 2002 (Article)
DOI: 10.1021/jm011072j
Molecular Interaction of the Antagonist N-(Piperidin-1-yl)-5-(4-chlorophenyl)-1- (2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide with the CB1 Cannabinoid Receptor
Joong-Youn Shim, William J. Welsh, Etienne Cartier, James L. Edwards, and Allyn C. Howlett
pp 1447–1459Publication Date (Web): March 03, 2002 (Article)
DOI: 10.1021/jm010267o
Modeling of Binding Modes and Inhibition Mechanism of Some Natural Ligands of Farnesyl Transferase Using Molecular Docking
Alessandro Pedretti, Luigi Villa, and Giulio Vistoli
pp 1460–1465Publication Date (Web): February 21, 2002 (Article)
DOI: 10.1021/jm011075w
Carbonic Anhydrase Inhibitors. A General Approach for the Preparation of Water-Soluble Sulfonamides Incorporating Polyamino−Polycarboxylate Tails and of Their Metal Complexes Possessing Long-Lasting, Topical Intraocular Pressure-Lowering Properties
Andrea Scozzafava, Luca Menabuoni, Francesco Mincione, and Claudiu T. Supuran
pp 1466–1476Publication Date (Web): February 22, 2002 (Article)
DOI: 10.1021/jm0108202
Toward an Optimal Joint Recognition of the S1‘ Subsites of Endothelin Converting Enzyme-1 (ECE-1), Angiotensin Converting Enzyme (ACE), and Neutral Endopeptidase (NEP)
Nicolas Inguimbert, Pascale Coric, Hervé Poras, Hervé Meudal, Franck Teffot, Marie-Claude Fournié-Zaluski, and Bernard P. Roques
pp 1477–1486Publication Date (Web): February 23, 2002 (Article)
DOI: 10.1021/jm0005454
Synthesis and Structure−Activity Relationships of 3-Aryloxindoles: A New Class of Calcium-Dependent, Large Conductance Potassium (Maxi-K) Channel Openers with Neuroprotective Properties
Piyasena Hewawasam, Matthew Erway, Sandra L. Moon, Jay Knipe, Harvey Weiner, Christopher G. Boissard, Debra J. Post-Munson, Qi Gao, Stella Huang, Valentin K. Gribkoff, and Nicholas A. Meanwell
pp 1487–1499Publication Date (Web): March 03, 2002 (Article)
DOI: 10.1021/jm0101850
1,8-Disubstituted Xanthine Derivatives: Synthesis of Potent A2B-Selective Adenosine Receptor Antagonists
Alaa M. Hayallah, Jesús Sandoval-Ramírez, Ulrike Reith, Ulrike Schobert, Birgit Preiss, Britta Schumacher, John W. Daly, and Christa E. Müller
pp 1500–1510Publication Date (Web): February 14, 2002 (Article)
DOI: 10.1021/jm011049y
4-(4-Cycloalkyl/aryl-oxazol-5-yl)benzenesulfonamides as Selective Cyclooxygenase-2 Inhibitors: Enhancement of the Selectivity by Introduction of a Fluorine Atom and Identification of a Potent, Highly Selective, and Orally Active COX-2 Inhibitor JTE-5221
Hiromasa Hashimoto, Katsuaki Imamura, Jun-ichi Haruta, and Korekiyo Wakitani
pp 1511–1517Publication Date (Web): February 26, 2002 (Article)
DOI: 10.1021/jm010484p
Novel 5-Substituted 2,4-Thiazolidinedione and 2,4-Oxazolidinedione Derivatives as Insulin Sensitizers with Antidiabetic Activities
Yu Momose, Tsuyoshi Maekawa, Tohru Yamano, Mitsuru Kawada, Hiroyuki Odaka, Hitoshi Ikeda, and Takashi Sohda
pp 1518–1534Publication Date (Web): February 27, 2002 (Article)
DOI: 10.1021/jm010490l
Synthesis and Biological Evaluation of Cycloalkylidene Carboxylic Acids as Novel Effectors of Ras/Raf Interaction
Anke Friese, Katja Hell-Momeni, Ilse Zündorf, Thomas Winckler, Theodor Dingermann, and Gerd Dannhardt
pp 1535–1542Publication Date (Web): February 28, 2002 (Article)
DOI: 10.1021/jm011101q