Table of Contents
August 1, 2002
Volume 45, Issue 16
Pages 3327-3568
About the Cover: Model of the histone deacetylase inhibitor, 3-(4-benzoyl-1-methyl-1H-2-pyrrole)-N-hydroxy-
Letters
Novel Retinoid X Receptor Antagonists: Specific Inhibition of Retinoid Synergism in RXR−RAR Heterodimer Actions
Bitoku Takahashi, Kiminori Ohta, Emiko Kawachi, Hiroshi Fukasawa, Yuichi Hashimoto, and Hiroyuki Kagechika
pp 3327–3330Publication Date (Web): July 09, 2002 (Letter)
DOI: 10.1021/jm0255320
Hi-Res PDF Expedited Articles
Mixed Steroidal 1,2,4,5-Tetraoxanes: Antimalarial and Antimycobacterial Activity
Bogdan A. Šolaja, Nataša Terzić, Gabriella Pocsfalvi, Lucia Gerena, Bernard Tinant, Dejan Opsenica, and Wilbur K. Milhous
pp 3331–3336Publication Date (Web): June 29, 2002 (Expedited Article)
DOI: 10.1021/jm020891g
Articles
Pyrido[2,1-f]purine-2,4-dione Derivatives as a Novel Class of Highly Potent Human A3 Adenosine Receptor Antagonists
Eva-María Priego, Jacobien von Frijtag Drabbe Kuenzel, Ad P. IJzerman, María-José Camarasa, and María-Jesús Pérez-Pérez
pp 3337–3344Publication Date (Web): July 02, 2002 (Article)
DOI: 10.1021/jm0208469
Descriptors, Physical Properties, and Drug-Likeness
Matthias Brüstle, Bernd Beck, Torsten Schindler, William King, Timothy Mitchell, and Timothy Clark
pp 3345–3355Publication Date (Web): July 03, 2002 (Article)
DOI: 10.1021/jm011027b
(4R,5S)/(4S,5R)-4,5-Bis(4-hydroxyphenyl)-2-imidazolines: Ligands for the Estrogen Receptor with a Novel Binding Mode
Ronald Gust, Roland Keilitz, Kathrin Schmidt, and Moriz von Rauch
pp 3356–3365Publication Date (Web): June 29, 2002 (Article)
DOI: 10.1021/jm020809h
2-Ethyl and 2-Ethylidene Analogues of 1α,25-Dihydroxy-19-norvitamin D3: Synthesis, Conformational Analysis, Biological Activities, and Docking to the Modeled rVDR Ligand Binding Domain
Rafal R. Sicinski, Piotr Rotkiewicz, Andrzej Kolinski, Wanda Sicinska, Jean M. Prahl, Connie M. Smith, and Hector F. DeLuca
pp 3366–3380Publication Date (Web): June 28, 2002 (Article)
DOI: 10.1021/jm020007m
Probing the ATP Ribose-Binding Domain of Cyclin-Dependent Kinases 1 and 2 with O6-Substituted Guanine Derivatives
Ashleigh E. Gibson, Christine E. Arris, Johanne Bentley, F. Thomas Boyle, Nicola J. Curtin, Thomas G. Davies, Jane A. Endicott, Bernard T. Golding, Sharon Grant, Roger J. Griffin, Philip Jewsbury, Louise N. Johnson, Veronique Mesguiche, David R. Newell, Martin E. M. Noble, Julie A. Tucker, and Hayley J. Whitfield
pp 3381–3393Publication Date (Web): July 04, 2002 (Article)
DOI: 10.1021/jm020056z
Discovery of 2-Phenylamino-imidazo[4,5-h]isoquinolin-9-ones: A New Class of Inhibitors of Lck Kinase
Roger J. Snow, Mario G. Cardozo, Tina M. Morwick, Carl A. Busacca, Yong Dong, Robert J. Eckner, Stephen Jacober, Scott Jakes, Suresh Kapadia, Susan Lukas, Maret Panzenbeck, Gregory W. Peet, Jeffrey D. Peterson, Anthony S. Prokopowicz, III, Rosemarie Sellati, Robert M. Tolbert, Matt A. Tschantz, and Neil Moss
pp 3394–3405Publication Date (Web): June 27, 2002 (Article)
DOI: 10.1021/jm020113o
Synthesis and Evaluation of 2‘-Substituted 4-(4‘-Carboxy- or 4‘-carboxymethylbenzylidene)-N-acylpiperidines: Highly Potent and in Vivo Active Steroid 5α-Reductase Type 2 Inhibitors
Franck Picard, Stephan Barassin, Armand Mokhtarian, and Rolf W. Hartmann
pp 3406–3417Publication Date (Web): June 29, 2002 (Article)
DOI: 10.1021/jm0208471
Monocyclic Human Tachykinin NK-2 Receptor Antagonists as Evolution of a Potent Bicyclic Antagonist: QSAR and Site-Directed Mutagenesis Studies
Alessandro Giolitti, Maria Altamura, Francesca Bellucci, Danilo Giannotti, Stefania Meini, Riccardo Patacchini, Luigi Rotondaro, Sabrina Zappitelli, and Carlo A. Maggi
pp 3418–3429Publication Date (Web): July 03, 2002 (Article)
DOI: 10.1021/jm011127h
New Inhibitors of Bacterial Protein Synthesis from a Combinatorial Library of Macrocycles
Elizabeth A. Jefferson, Satoshi Arakawa, Lawrence B. Blyn, Alycia Miyaji, Stephen A. Osgood, Raymond Ranken, Lisa M. Risen, and Eric E. Swayze
pp 3430–3439Publication Date (Web): June 27, 2002 (Article)
DOI: 10.1021/jm010437x
Imidazo[2,1-i]purin-5-ones and Related Tricyclic Water-Soluble Purine Derivatives: Potent A2A- and A3-Adenosine Receptor Antagonists
Christa E. Müller, Mark Thorand, Ramatullah Qurishi, Martina Diekmann, Kenneth A. Jacobson, William L. Padgett, and John W. Daly
pp 3440–3450Publication Date (Web): June 28, 2002 (Article)
DOI: 10.1021/jm011093d
Selective α4β7 Integrin Antagonists and Their Potential as Antiinflammatory Agents
Nathan J. P. Dubree, Dean R. Artis, Georgette Castanedo, James Marsters, Daniel Sutherlin, Lisa Caris, Kevin Clark, Susan M. Keating, Maureen H. Beresini, Henry Chiu, Sherman Fong, Henry B. Lowman, Nicholas J. Skelton, and David Y. Jackson
pp 3451–3457Publication Date (Web): June 28, 2002 (Article)
DOI: 10.1021/jm020033k
Synthesis and Biological Evaluation of Novel Macrocyclic Ligands with Pendent Donor Groups as Potential Yttrium Chelators for Radioimmunotherapy with Improved Complex Formation Kinetics
Hyun-soon Chong, Kayhan Garmestani, Dangshe Ma, Diane E. Milenic, Terrish Overstreet, and Martin W. Brechbiel
pp 3458–3464Publication Date (Web): June 18, 2002 (Article)
DOI: 10.1021/jm0200759
The Effect of a Phosphodiester Linking Group on Albumin Binding, Blood Half-Life, and Relaxivity of Intravascular Diethylenetriaminepentaacetato Aquo Gadolinium(III) MRI Contrast Agents
Thomas J. McMurry, David J. Parmelee, Hironao Sajiki, Daniel M. Scott, Hillori S. Ouellet, Richard C. Walovitch, Zoltán Tyeklár, Stéphane Dumas, Paul Bernard, Samuel Nadler, Katarina Midelfort, Matthew Greenfield, Jeffrey Troughton, and Randall B. Lauffer
pp 3465–3474Publication Date (Web): June 27, 2002 (Article)
DOI: 10.1021/jm0102351
Cardiovascular Characterization of [1,4]Thiazino[3,4-c][1,2,4]oxadiazol-1-one Derivatives: Selective Myocardial Calcium Channel Modulators
Roberta Budriesi, Barbara Cosimelli, Pierfranco Ioan, Camilla Zaira Lanza, Domenico Spinelli, and Alberto Chiarini
pp 3475–3481Publication Date (Web): June 29, 2002 (Article)
DOI: 10.1021/jm020815d
Synthesis of Potent Leukotriene A4 Hydrolase Inhibitors. Identification of 3-[Methyl[3-[4-(phenylmethyl)phenoxy]propyl]amino]propanoic Acid
Thomas D. Penning, Mark A. Russell, Barbara B. Chen, Helen Y. Chen, Chi-Dean Liang, Matthew W. Mahoney, James W. Malecha, Julie M. Miyashiro, Stella S. Yu, Leslie J. Askonas, James K. Gierse, Elizabeth I. Harding, Maureen K. Highkin, James F. Kachur, Suzanne H. Kim, Doreen Villani-Price, E. Yvonne Pyla, Nayereh S. Ghoreishi-Haack, and Walter G. Smith
pp 3482–3490Publication Date (Web): June 27, 2002 (Article)
DOI: 10.1021/jm0200916
Synthesis and In Vitro Studies of Novel Pyrimidinyl Peptidomimetics as Potential Antimalarial Therapeutic Agents
Shuren Zhu, Thomas H. Hudson, Dennis E. Kyle, and Ai J. Lin
pp 3491–3496Publication Date (Web): July 09, 2002 (Article)
DOI: 10.1021/jm020104f
Synthesis, Cytotoxicity, and Antiplasmodial and Antitrypanosomal Activity of New Neocryptolepine Derivatives
Tim H. M. Jonckers, Sabine van Miert, Kanyanga Cimanga, Christian Bailly, Pierre Colson, Marie-Claire De Pauw-Gillet, Hilde van den Heuvel, Magda Claeys, Filip Lemière, Eddy L. Esmans, Jef Rozenski, Ludo Quirijnen, Louis Maes, Roger Dommisse, Guy L. F. Lemière, Arnold Vlietinck, and Luc Pieters
pp 3497–3508Publication Date (Web): June 29, 2002 (Article)
DOI: 10.1021/jm011102i
Discovery and Optimization of a Series of Carbazole Ureas as NPY5 Antagonists for the Treatment of Obesity
Michael H. Block, Scott Boyer, Wayne Brailsford, David R. Brittain, Debra Carroll, Steve Chapman, David S. Clarke, Craig S. Donald, Kevin M. Foote, Linda Godfrey, Anthony Ladner, Peter R. Marsham, David J. Masters, Christine D. Mee, Michael R. O'Donovan, J. Elizabeth Pease, Adrian G. Pickup, John W. Rayner, Andrew Roberts, Paul Schofield, Abid Suleman, and Andrew V. Turnbull
pp 3509–3523Publication Date (Web): July 02, 2002 (Article)
DOI: 10.1021/jm011125x
Discovery of an Opioid κ Receptor Selective Pure Antagonist from a Library of N-Substituted 4β-Methyl-5-(3-hydroxyphenyl)morphans
James B. Thomas, Robert N. Atkinson, Nivedita Namdev, Richard B. Rothman, Kenneth M. Gigstad, Scott E. Fix, S. Wayne Mascarella, Jason P. Burgess, N. Ariane Vinson, Heng Xu, Christina M. Dersch, Buddy E. Cantrell, Dennis M. Zimmerman, and F. Ivy Carroll
pp 3524–3530Publication Date (Web): July 04, 2002 (Article)
DOI: 10.1021/jm020084h
Structure−Activity Relationships in 4-Aminoquinoline Antiplasmodials. The Role of the Group at the 7-Position
Catherine H. Kaschula, Timothy J. Egan, Roger Hunter, Nicoletta Basilico, Silvia Parapini, Donatella Taramelli, Erica Pasini, and Diego Monti
pp 3531–3539Publication Date (Web): June 29, 2002 (Article)
DOI: 10.1021/jm020858u
Design, Synthesis, and Biological Evaluation of Indolequinone Phosphoramidate Prodrugs Targeted to DT-diaphorase
Marcy Hernick, Carolee Flader, and Richard F. Borch
pp 3540–3548Publication Date (Web): July 04, 2002 (Article)
DOI: 10.1021/jm020191b
Synthesis of N-Glyoxyl Prolyl and Pipecolyl Amides and Thioesters and Evaluation of Their In Vitro and In Vivo Nerve Regenerative Effects
Gregory S. Hamilton, Yong-Qian Wu, David C. Limburg, Douglas E. Wilkinson, Mark J. Vaal, Jia-He Li, Christine Thomas, Wei Huang, Hansjorg Sauer, Douglas T. Ross, Raj Soni, Yi Chen, Hongshi Guo, Pamela Howorth, Heather Valentine, Shi Liang, Dawn Spicer, Mike Fuller, and Joseph P. Steiner
pp 3549–3557Publication Date (Web): July 09, 2002 (Article)
DOI: 10.1021/jm010556c
Synthesis of Ketone Analogues of Prolyl and Pipecolyl Ester FKBP12 Ligands
Yong-Qian Wu, Douglas E. Wilkinson, David Limburg, Jia-He Li, Hansjorg Sauer, Doug Ross, Shi Liang, Dawn Spicer, Heather Valentine, Mike Fuller, Hong Guo, Pam Howorth, Raj Soni, Yi Chen, Joseph P. Steiner, and Gregory S. Hamilton
pp 3558–3568Publication Date (Web): July 09, 2002 (Article)
DOI: 10.1021/jm0200456