Table of Contents
August 29, 2002
Volume 45, Issue 18
Pages 3813-4056
About the Cover: Model of the histone deacetylase inhibitor, 3-(4-benzoyl-1-methyl-1H-2-pyrrole)-N-hydroxy-
Letters
Arylsulfonamidothiazoles as a New Class of Potential Antidiabetic Drugs. Discovery of Potent and Selective Inhibitors of the 11β-Hydroxysteroid Dehydrogenase Type 1
Tjeerd Barf, Jerk Vallgårda, Rikard Emond, Charlotta Häggström, Guido Kurz, Alf Nygren, Vivienne Larwood, Erifili Mosialou, Kent Axelsson, Rolf Olsson, Lars Engblom, Naimie Edling, Yuko Rönquist-Nii, Birgitta Öhman, Peteris Alberts, and Lars Abrahmsén
pp 3813–3815Publication Date (Web): August 03, 2002 (Letter)
DOI: 10.1021/jm025530f
Hi-Res PDFSAR by MS: A Ligand Based Technique for Drug Lead Discovery Against Structured RNA Targets
Eric E. Swayze, Elizabeth A. Jefferson, Kristin A. Sannes-Lowery, Lawrence B. Blyn, Lisa M. Risen, Satoshi Arakawa, Stephen A. Osgood, Steven A. Hofstadler, and Richard H. Griffey
pp 3816–3819Publication Date (Web): July 27, 2002 (Letter)
DOI: 10.1021/jm0255466
Solid Phase Synthesis and Evaluation of Tyr-Tic-Phe-Phe(p-NHCOCH2Br) ([Phe(p-bromoacetamide)4]TIPP), a Potent Affinity Label for δ Opioid Receptors
Vivek Kumar, Thomas F. Murray, and Jane V. Aldrich
pp 3820–3823Publication Date (Web): August 03, 2002 (Letter)
DOI: 10.1021/jm020290p
Expedited Articles
Orally Active, Water-Soluble Antimalarial 3-Aryltrioxanes: Short Synthesis and Preclinical Efficacy Testing in Rodents
Gary H. Posner, Heung Bae Jeon, Poonsakdi Ploypradith, Ik-Hyeon Paik, Kristina Borstnik, Suji Xie, and Theresa A. Shapiro
pp 3824–3828Publication Date (Web): July 30, 2002 (Expedited Article)
DOI: 10.1021/jm020210h
Discovery of N-Isoxazolyl Biphenylsulfonamides as Potent Dual Angiotensin II and Endothelin A Receptor Antagonists
Natesan Murugesan, John E. Tellew, Zhengxiang Gu, Bridgette L. Kunst, Leena Fadnis, Lyndon A. Cornelius, Rose Ann F. Baska, Yifan Yang, Sophie M. Beyer, Hossain Monshizadegan, Kenneth E. Dickinson, Balkrushna Panchal, Maria T. Valentine, Saeho Chong, Richard A. Morrison, Kenneth E. Carlson, James R. Powell, Suzanne Moreland, Joel C. Barrish, Mark C. Kowala, and John E. Macor
pp 3829–3835Publication Date (Web): August 08, 2002 (Expedited Article)
DOI: 10.1021/jm020138n
Articles
Structural Basis for Understanding Structure−Activity Relationships for the Glutamate Binding Site of the NMDA Receptor
Irina G. Tikhonova, Igor I. Baskin, Vladimir A. Palyulin, Nikolai S. Zefirov, and Sergey O. Bachurin
pp 3836–3843Publication Date (Web): July 27, 2002 (Article)
DOI: 10.1021/jm011091t
Toward a Pharmacophore for Drugs Inducing the Long QT Syndrome: Insights from a CoMFA Study of HERG K+ Channel Blockers
Andrea Cavalli, Elisabetta Poluzzi, Fabrizio De Ponti, and Maurizio Recanatini
pp 3844–3853Publication Date (Web): July 25, 2002 (Article)
DOI: 10.1021/jm0208875
Exploring the Role of Bromine at C(10) of (+)-4-[2-[4-(8-Chloro-3,10-dibromo- 6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11(R)-yl)-1-piperidinyl]-2- oxoethyl]-1-piperidinecarboxamide (Sch-66336): The Discovery of Indolocycloheptapyridine Inhibitors of Farnesyl Protein Transferase
Arthur G. Taveras, Cynthia Aki, Jianping Chao, Ronald J. Doll, Tarik Lalwani, Viyyoor Girijavallabhan, Corey L. Strickland, William T. Windsor, Patricia Weber, Frank Hollinger, Mark Snow, Robert Patton, Paul Kirschmeier, Linda James, Ming Liu, and Amin Nomeir
pp 3854–3864Publication Date (Web): August 06, 2002 (Article)
DOI: 10.1021/jm010463v
Anilinoquinazoline Inhibitors of Fructose 1,6-Bisphosphatase Bind at a Novel Allosteric Site: Synthesis, In Vitro Characterization, and X-ray Crystallography
Stephen W. Wright, Anthony A. Carlo, Maynard D. Carty, Dennis E. Danley, David L. Hageman, George A. Karam, Carolyn B. Levy, Mahmoud N. Mansour, Alan M. Mathiowetz, Lester D. McClure, Nestor B. Nestor, R. Kirk McPherson, Jayvardhan Pandit, Leslie R. Pustilnik, Gayle K. Schulte, Walter C. Soeller, Judith L. Treadway, Ing-Kae Wang, and Paul H. Bauer
pp 3865–3877Publication Date (Web): July 26, 2002 (Article)
DOI: 10.1021/jm010496a
Discovery of Further Pyrrolidine trans-Lactams as Inhibitors of Human Neutrophil Elastase (HNE) with Potential as Development Candidates and the Crystal Structure of HNE Complexed with an Inhibitor (GW475151)
Simon J. F. Macdonald, Michael D. Dowle, Lee A. Harrison, Geoffrey D. E. Clarke, Graham G. A. Inglis, Martin R. Johnson, Pritom Shah, Robin A. Smith, Augustin Amour, Gill Fleetwood, Davina C. Humphreys, Christopher R. Molloy, Mary Dixon, Rosalind E. Godward, Alan J. Wonacott, Onkar M. P. Singh, Simon T. Hodgson, and George W. Hardy
pp 3878–3890Publication Date (Web): August 03, 2002 (Article)
DOI: 10.1021/jm020881f
Chiral N,N-Disubstituted Trifluoro-3-Amino-2-Propanols Are Potent Inhibitors of Cholesteryl Ester Transfer Protein
Richard C. Durley, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Jane L. Wang, Dale P. Spangler, Deborah A. Mischke, Barry L. Parnas, Yvette M. Fobian, Nigam P. Rath, Dorothy D. Honda, Ming Zeng, Daniel T. Connolly, Deborah M. Heuvelman, Bryan J. Witherbee, Michele A. Melton, Kevin C. Glenn, Elaine S. Krul, Mark E. Smith, and James A. Sikorski
pp 3891–3904Publication Date (Web): August 03, 2002 (Article)
DOI: 10.1021/jm020038h
Discovery of Aminothiazole Inhibitors of Cyclin-Dependent Kinase 2: Synthesis, X-ray Crystallographic Analysis, and Biological Activities
Kyoung Soon Kim, S. David Kimball, Raj N. Misra, David B. Rawlins, John T. Hunt, Hai-Yun Xiao, Songfeng Lu, Ligang Qian, Wen-Ching Han, Weifang Shan, Toomas Mitt, Zhen-Wei Cai, Michael A. Poss, Hong Zhu, John S. Sack, John S. Tokarski, Chieh Ying Chang, Nikola Pavletich, Amrita Kamath, William G. Humphreys, Punit Marathe, Isia Bursuker, Kristen A. Kellar, Urvashi Roongta, Roberta Batorsky, Janet G. Mulheron, David Bol, Craig R. Fairchild, Francis Y. Lee, and Kevin R. Webster
pp 3905–3927Publication Date (Web): August 02, 2002 (Article)
DOI: 10.1021/jm0201520
Synthesis and Evaluation of Glyψ(PO2R-N)Pro-Containing Pseudopeptides as Novel Inhibitors of the Human Cyclophilin hCyp-18
Luc Demange, Mireille Moutiez, and Christophe Dugave
pp 3928–3933Publication Date (Web): July 25, 2002 (Article)
DOI: 10.1021/jm020865i
Synthesis of 3‘ ‘-Substituted TSAO Derivatives with Anti-HIV-1 and Anti-HIV-2 Activity through an Efficient Palladium-Catalyzed Cross-Coupling Approach
Esther Lobatón, Fátima Rodríguez-Barrios, Federico Gago, María-Jesús Pérez-Pérez, Erik De Clercq, Jan Balzarini, María-José Camarasa, and Sonsoles Velázquez
pp 3934–3945Publication Date (Web): July 31, 2002 (Article)
DOI: 10.1021/jm020820h
Divalent and Trivalent α-Ketocarboxylic Acids as Inhibitors of Protein Tyrosine Phosphatases
Yen Ting Chen and Christopher T. Seto
pp 3946–3952Publication Date (Web): July 12, 2002 (Article)
DOI: 10.1021/jm020093q
Synthesis of Conformationally Constrained Analogues of Linezolid: Structure−Activity Relationship (SAR) Studies on Selected Novel Tricyclic Oxazolidinones
Natesan Selvakumar, Deekonda Srinivas, Manoj Kumar Khera, Magadi Sitaram Kumar, Rao N. V. S. Mamidi, Hemanth Sarnaik, Chandrashekar Charavaryamath, Bonthu Srinivasa Rao, Mohammed A. Raheem, Jagattaran Das, Javed Iqbal, and Ramanujam Rajagopalan
pp 3953–3962Publication Date (Web): August 03, 2002 (Article)
DOI: 10.1021/jm020092y
Synthesis and Initial Evaluation for In Vivo Chelation of Pu(IV) of a Mixed Octadentate Spermine-Based Ligand Containing 4-Carbamoyl-3-hydroxy-1-methyl-2(1H)-pyridinone and 6-Carbamoyl-1-hydroxy-2(1H)-pyridinone
Jide Xu, Patricia W. Durbin, Birgitta Kullgren, Shirley N. Ebbe, Linda C. Uhlir, and Kenneth N. Raymond
pp 3963–3971Publication Date (Web): July 31, 2002 (Article)
DOI: 10.1021/jm010564t
Design, Synthesis, and SAR of Tachykinin Antagonists: Modulation of Balance in NK1/NK2 Receptor Antagonist Activity
Jeffrey S. Albert, David Aharony, Donald Andisik, Herbert Barthlow, Peter R. Bernstein, Russell A. Bialecki, Robert Dedinas, Bruce T. Dembofsky, Daniel Hill, Karin Kirkland, Gerard M. Koether, Benedict J. Kosmider, Cyrus Ohnmacht, William Palmer, William Potts, William Rumsey, Lihong Shen, Ashok Shenvi, Scott Sherwood, Paul J. Warwick, and Keith Russell
pp 3972–3983Publication Date (Web): August 03, 2002 (Article)
DOI: 10.1021/jm020094i
Design, Synthesis, and Biological Evaluation of Aryloxyethyl Thiocyanate Derivatives against Trypanosoma cruzi
Eleonora Elhalem, Brian N. Bailey, Roberto Docampo, István Ujváry, Sergio H. Szajnman, and Juan B. Rodriguez
pp 3984–3999Publication Date (Web): July 26, 2002 (Article)
DOI: 10.1021/jm0201518
Influence of Bulky Substituents on Histamine H3 Receptor Agonist/Antagonist Properties
Astrid Sasse, Xavier Ligneau, Agnès Rouleau, Sigurd Elz, C. Robin Ganellin, Jean-Michel Arrang, Jean-Charles Schwartz, Walter Schunack, and Holger Stark
pp 4000–4010Publication Date (Web): July 30, 2002 (Article)
DOI: 10.1021/jm020910m
6-Chloropyridazin-3-yl Derivatives Active as Nicotinic Agents: Synthesis, Binding, and Modeling Studies
Lucio Toma, Paolo Quadrelli, William H. Bunnelle, David J. Anderson, Michael D. Meyer, Giorgio Cignarella, Arianna Gelain, and Daniela Barlocco
pp 4011–4017Publication Date (Web): July 27, 2002 (Article)
DOI: 10.1021/jm0208830
Synthesis of a Small Library of 3-(Carboranylalkyl)thymidines and Their Biological Evaluation as Substrates for Human Thymidine Kinases 1 and 2
Ashraf S. Al-Madhoun, Jayaseharan Johnsamuel, Junhua Yan, Weihua Ji, Jianghai Wang, Jin-Cong Zhuo, Anthony J. Lunato, Jeffrey E. Woollard, Andrew E. Hawk, Guirec Y. Cosquer, Thomas E. Blue, Staffan Eriksson, and Werner Tjarks
pp 4018–4028Publication Date (Web): August 02, 2002 (Article)
DOI: 10.1021/jm020047q
Synthesis and Transporter Binding Properties of 3β-[4‘-(Phenylalkyl, -phenylalkenyl, and -phenylalkynl)phenyl]tropane-2β-carboxylic Acid Methyl Esters: Evidence of a Remote Phenyl Binding Domain on the Dopamine Transporter
Bruce E. Blough, Kathryn I. Keverline, Zhe Nie, Hernán Navarro, Michael J. Kuhar, and F. Ivy Carroll
pp 4029–4037Publication Date (Web): August 06, 2002 (Article)
DOI: 10.1021/jm020098n
Ginkgolide Derivatives for Photolabeling Studies: Preparation and Pharmacological Evaluation
Kristian Strømgaard, D. Roland Saito, Hideo Shindou, Satoshi Ishii, Takao Shimizu, and Koji Nakanishi
pp 4038–4046Publication Date (Web): August 03, 2002 (Article)
DOI: 10.1021/jm020147w
Conformationally Constrained Nicotines: Polycyclic, Bridged, and Spiro-Annulated Analogues as Novel Ligands for the Nicotinic Acetylcholine Receptor
Thomas Ullrich, Sylvia Krich, Dieter Binder, Kurt Mereiter, David J. Anderson, Michael D. Meyer, and Michael Pyerin
pp 4047–4054Publication Date (Web): August 07, 2002 (Article)
DOI: 10.1021/jm020916b
Book Reviews
Organic Reactions. Volume 57 Edited by Larry E. Overman. Wiley, New York. 2001. vii + 693 pp. 16 × 23.5 cm. ISBN 0-471-43511-2. $125.00
Bruce L. Currie
p 4055Publication Date (Web): June 27, 2002 (Book Review)
DOI: 10.1021/jm020223v
Additions and Corrections
Design and Synthesis of [(2,3-Dichlorophenyl)piperazin-1-yl]alkylfluorenylcarboxamides as Novel Ligands Selective for the Dopamine D3 Receptor Subtype
Michael J. Robarge, Stephen M. Husbands, Andrzej Kieltyka, Robbin Brodbeck, Andrew Thurkauf, and Amy Hauck Newman*
p 4056Publication Date (Web): July 30, 2002 (Addition/Correction)
DOI: 10.1021/jm020255i
A New Type of Prodrug of Catecholamines: An Opportunity To Improve the Treatment of Parkinson's Disease
Bastiaan J. Venhuis, Nienke Rodenhuis, Håkan V. Wikström,* David Wustrow, Leonard T. Meltzer, Lawrence D. Wise, Stephen J. Johnson, Thomas A. Pugsley, Staffan Sundell, and Durk Dijkstra
p 4056Publication Date (Web): July 18, 2002 (Addition/Correction)
DOI: 10.1021/jm0209634