Table of Contents
January 15, 2004
Volume 47, Issue 2
Pages 281-492
About the Cover: Molecular modeling of overlayed trisubstituted acridine derivatives (mauve and green) complexed with G-quadruplex DNA (Harrison, R. J.; et al. J. Med. Chem. 2003, 46, 4463-4476).
Letters
Discovery of the First N-Substituted 4β-Methyl-5-(3-hydroxyphenyl)morphan To Possess Highly Potent and Selective Opioid δ Receptor Antagonist Activity
F. Ivy Carroll, Li Zhang, S. Wayne Mascarella, Hernán A. Navarro, Richard B. Rothman, Buddy E. Cantrell, Dennis M. Zimmerman, and James B. Thomas
pp 281–284Publication Date (Web): December 11, 2003 (Letter)
DOI: 10.1021/jm030419a
Hi-Res PDFDiscovery of a Bulky 2-tert-Butyl Group Containing Primaquine Analogue That Exhibits Potent Blood-Schizontocidal Antimalarial Activities and Complete Elimination of Methemoglobin Toxicity
Meenakshi Jain, Suryanarayana Vangapandu, Sandeep Sachdeva, Savita Singh, Prati P. Singh, Gopa B. Jena, Kulbhushan Tikoo, Poduri Ramarao, Chaman L. Kaul, and Rahul Jain
pp 285–287Publication Date (Web): December 19, 2003 (Letter)
DOI: 10.1021/jm0304562
Triacylglycerols Based on 2-(N-tert-Butoxycarbonylamino)oleic Acid Are Potent Inhibitors of Pancreatic Lipase
Victoria Magrioti, Robert Verger, and Violetta Constantinou-Kokotou
pp 288–291Publication Date (Web): December 12, 2003 (Letter)
DOI: 10.1021/jm034202s
Enantioselective Synthesis and Biological Activity of (3S,4R)- and (3S,4S)-3-Hydroxy-4-hydroxymethyl- 4-butanolides in Relation to PGE2
Pedro O. Miranda, Francisco Estévez, José Quintana, Candelaria I. García, Ignacio Brouard, Juan I. Padrón, Juan P. Pivel, and Jaime Bermejo
pp 292–295Publication Date (Web): December 16, 2003 (Letter)
DOI: 10.1021/jm034216y
Articles
Synthesis, Monoamine Transporter Binding Properties, and Behavioral Pharmacology of a Series of 3β-(Substituted phenyl)-2β-(3‘-substituted isoxazol-5-yl)tropanes
F. Ivy Carroll, Neil Pawlush, Michael J. Kuhar, Gerald T. Pollard, and James L. Howard
pp 296–302Publication Date (Web): December 09, 2003 (Article)
DOI: 10.1021/jm030453p
Identification of Novel Binding Interactions in the Development of Potent, Selective 2-Naphthamidine Inhibitors of Urokinase. Synthesis, Structural Analysis, and SAR of N-Phenyl Amide 6-Substitution
Michael D. Wendt, Todd W. Rockway, Andrew Geyer, William McClellan, Moshe Weitzberg, Xumiao Zhao, Robert Mantei, Vicki L. Nienaber, Kent Stewart, Vered Klinghofer, and Vincent L. Giranda
pp 303–324Publication Date (Web): December 12, 2003 (Article)
DOI: 10.1021/jm0300072
Evaluation of P1'-Diversified Phosphinic Peptides Leads to the Development of Highly Selective Inhibitors of MMP-11
Magdalini Matziari, Fabrice Beau, Philippe Cuniasse, Vincent Dive, and Athanasios Yiotakis
pp 325–336Publication Date (Web): December 17, 2003 (Article)
DOI: 10.1021/jm0308491
Structural Interaction Fingerprint (SIFt): A Novel Method for Analyzing Three-Dimensional Protein−Ligand Binding Interactions
Zhan Deng, Claudio Chuaqui, and Juswinder Singh
pp 337–344Publication Date (Web): December 12, 2003 (Article)
DOI: 10.1021/jm030331x
Target Guided Synthesis of 5-Benzyl-2,4-diamonopyrimidines: Their Antimalarial Activities and Binding Affinities to Wild Type and Mutant Dihydrofolate Reductases from Plasmodium falciparum
Chawanee Sirichaiwat, Chakapong Intaraudom, Sumalee Kamchonwongpaisan, Jarunee Vanichtanankul, Yodhathai Thebtaranonth, and Yongyuth Yuthavong
pp 345–354Publication Date (Web): December 16, 2003 (Article)
DOI: 10.1021/jm0303352
Diflunisal Analogues Stabilize the Native State of Transthyretin. Potent Inhibition of Amyloidogenesis
Sara L. Adamski-Werner, Satheesh K. Palaninathan, James C. Sacchettini, and Jeffery W. Kelly
pp 355–374Publication Date (Web): December 11, 2003 (Article)
DOI: 10.1021/jm030347n
Quantitative Structure−Activity Relationships for γδ T Cell Activation by Bisphosphonates
John M. Sanders, Subhash Ghosh, Julian M. W. Chan, Gary Meints, Hong Wang, Amy M. Raker, Yongcheng Song, Alison Colantino, Agnieszka Burzynska, Pawel Kafarski, Craig T. Morita, and Eric Oldfield
pp 375–384Publication Date (Web): December 16, 2003 (Article)
DOI: 10.1021/jm0303709
Application of CoMFA and CoMSIA 3D-QSAR and Docking Studies in Optimization of Mercaptobenzenesulfonamides as HIV-1 Integrase Inhibitors
Chih-Ling Kuo, Haregewein Assefa, Shantaram Kamath, Zdzialaw Brzozowski, Jaroslaw Slawinski, Franciszek Saczewski, John K. Buolamwini, and Nouri Neamati
pp 385–399Publication Date (Web): December 11, 2003 (Article)
DOI: 10.1021/jm030378i
Synthesis and Structure−Activity Relationship for a Novel Class of Potent and Selective Carbamoyl-Triazole Based Inhibitors of Hormone Sensitive Lipase
Søren Ebdrup, Lotte Gottlieb Sørensen, Ole Hvilsted Olsen, and Poul Jacobsen
pp 400–410Publication Date (Web): December 12, 2003 (Article)
DOI: 10.1021/jm031004s
Semisynthetic Macrolide Antibacterials Derived from Tylosin. Synthesis and Structure−Activity Relationships of Novel Desmycosin Analogues1
Stjepan Mutak, Nataša Maršić, Miroslava Dominis Kramarić, and Dražen Pavlović
pp 411–431Publication Date (Web): December 16, 2003 (Article)
DOI: 10.1021/jm0308951
Design and Synthesis of Peptidomimetic Protein Farnesyltransferase Inhibitors as Anti-Trypanosoma brucei Agents
Junko Ohkanda, Frederick S. Buckner, Jeffrey W. Lockman, Kohei Yokoyama, Dora Carrico, Richard Eastman, Kate de Luca-Fradley, Wendy Davies, Simon L. Croft, Wesley C. Van Voorhis, Michael H. Gelb, Saïd M. Sebti, and Andrew D. Hamilton
pp 432–445Publication Date (Web): December 12, 2003 (Article)
DOI: 10.1021/jm030236o
Synthesis and Opioid Activity of Side-Chain-to-Side-Chain Cyclic Dynorphin A-(1−11) Amide Analogues Cyclized between Positions 2 and 5. 1. Substitutions in Position 3
Balvinder S. Vig, Thomas F. Murray, and Jane V. Aldrich
pp 446–455Publication Date (Web): December 17, 2003 (Article)
DOI: 10.1021/jm030298e
(2S,1‘S,2‘R,3‘R)-2-(2‘-Carboxy-3‘-hydroxymethylcyclopropyl) Glycine Is a Highly Potent Group 2 and 3 Metabotropic Glutamate Receptor Agonist with Oral Activity
Iván Collado, Concepción Pedregal, Ana Belén Bueno, Alicia Marcos, Rosario González, Jaime Blanco-Urgoiti, Javier Pérez-Castells, Darryle D. Schoepp, Rebecca A. Wright, Bryan G. Johnson, Ann E. Kingston, Eric D. Moher, David W. Hoard, Kelly I. Griffey, and Joseph P. Tizzano
pp 456–466Publication Date (Web): December 09, 2003 (Article)
DOI: 10.1021/jm030967o
Zn2+-Chelating Motif-Tethered Short-Chain Fatty Acids as a Novel Class of Histone Deacetylase Inhibitors
Qiang Lu, Ya-Ting Yang, Chang-Shi Chen, Melanie Davis, John C. Byrd, Mark R. Etherton, Asad Umar, and Ching-Shih Chen
pp 467–474Publication Date (Web): December 11, 2003 (Article)
DOI: 10.1021/jm0303655
DNA-Targeted 1,2,4-Benzotriazine 1,4-Dioxides: Potent Analogues of the Hypoxia-Selective Cytotoxin Tirapazamine
Michael P. Hay, Frederik B. Pruijn, Swarna A. Gamage, H. D. Sarath Liyanage, Mary S. Kovacs, Adam V. Patterson, William R. Wilson, J. Martin Brown, and William A. Denny
pp 475–488Publication Date (Web): December 17, 2003 (Article)
DOI: 10.1021/jm030399c
Brief Articles
Restriction of a Peptide Turn Conformation and Conformational Analysis of Guanidino Group Using Arginine-Proline Fused Amino Acids: Application to Mini Atrial Natriuretic Peptide on Binding to the Receptor
Kenji Sugase, Manabu Horikawa, Masako Sugiyama, and Masaji Ishiguro
pp 489–492Publication Date (Web): December 11, 2003 (Brief Article)
DOI: 10.1021/jm030232j