Table of Contents
July 29, 2004
Volume 47, Issue 16
Pages 3897-4110
About the Cover: Ribbon rendered illustration of the nuclear receptor heterodimer RXRα(cyan):PPARRγ (red) ligand binding domains bound with coactivator peptides (magenta) and agonist ligands (space-filling atoms where green is carbon, red is oxygen, and blue is nitrogen) (Haffner, C. D.; et al. J. Med. Chem. 2004, 47, 2010-2029).
Perspective
Current Clinical and Preclinical Photosensitizers for Use in Photodynamic Therapy
Michael R. Detty, Scott L. Gibson, and Stephen J. Wagner
pp 3897–3915Publication Date (Web): June 19, 2004 (Perspective)
DOI: 10.1021/jm040074b
Hi-Res PDF Letters
Phosphorylcholine−Carbohydrate− Protein Conjugates Efficiently Induce Hapten-Specific Antibodies Which Recognize Both Streptococcus pneumoniae and Neisseria meningitidis: A Potential Multitarget Vaccine against Respiratory Infections
Sylvie Bay, Valérie Huteau, Maria-Leticia Zarantonelli, René Pires, Joël Ughetto-Monfrin, Muhamed-Kheir Taha, Patrick England, and Pierre Lafaye
pp 3916–3919Publication Date (Web): July 07, 2004 (Letter)
DOI: 10.1021/jm040783p
Design, Synthesis, and Evaluation of Su- gar Amino Acid Based Inhibitors of Pro- tein Prenyl Transferases PFT and PGGT-1
Farid El Oualid, Brigitte E. A. Burm, Ingrid M. Leroy, Louis H. Cohen, Jacques H. van Boom, Hans van den Elst, Herman S. Overkleeft, Gijs A. van der Marel, and Mark Overhand
pp 3920–3923Publication Date (Web): June 24, 2004 (Letter)
DOI: 10.1021/jm049927q
Imidazole Analogues of Fluoxetine, a Novel Class of Anti-Candida Agents
Romano Silvestri, Marino Artico, Giuseppe La Regina, Alessandra Di Pasquali, Gabriella De Martino, Felicia Diodata D'Auria, Lucia Nencioni, and Anna Teresa Palamara
pp 3924–3926Publication Date (Web): July 02, 2004 (Letter)
DOI: 10.1021/jm049856v
Novel 2-Aminotetralin and 3-AminoChroman Derivatives as Selective Serotonin 5-HT7 Receptor Agonists and Antagonists
Pär Holmberg, Daniel Sohn, Robert Leideborg, Patrizia Caldirola, Pavel Zlatoidsky, Sverker Hanson, Nina Mohell, Susanne Rosqvist, Gunnar Nordvall, Anette M. Johansson, and Rolf Johansson
pp 3927–3930Publication Date (Web): June 29, 2004 (Letter)
DOI: 10.1021/jm0498102
Discovery of a Subnanomolar Helical d-Tridecapeptide Inhibitor of γ-Secretase
Frédéric Bihel, Chittaranjan Das, Michael J. Bowman, and Michael S. Wolfe
pp 3931–3933Publication Date (Web): June 29, 2004 (Letter)
DOI: 10.1021/jm049788c
Substituted 3-Imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino- [6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as Highly Selective and Potent Inhibitors of Glycogen Synthase Kinase-3
Thomas A. Engler, James R. Henry, Sushant Malhotra, Brian Cunningham, Kelly Furness, Joseph Brozinick, Timothy P. Burkholder, Michael P. Clay, Joshua Clayton, Clive Diefenbacher, Eric Hawkins, Philip W. Iversen, Yihong Li, Terry D. Lindstrom, Angela L. Marquart, Johnathan McLean, David Mendel, Elizabeth Misener, Daniel Briere, John C. O'Toole, Warren J. Porter, Steven Queener, Jon K. Reel, Rebecca A. Owens, Richard A. Brier, Thomas E. Eessalu, Jill R. Wagner, Robert M. Campbell, and Renee Vaughn
pp 3934–3937Publication Date (Web): June 23, 2004 (Letter)
DOI: 10.1021/jm049768a
Articles
Spacer-Arm Modulated Gene Delivery Efficacy of Novel Cationic Glycolipids: Design, Synthesis, and in Vitro Transfection Biology
Yenugonda Venkata Mahidhar, Mukthavaram Rajesh, and Arabinda Chaudhuri
pp 3938–3948Publication Date (Web): June 23, 2004 (Article)
DOI: 10.1021/jm030464i
Contribution of Ionization and Lipophilicity to Drug Binding to Albumin: A Preliminary Step toward Biodistribution Prediction
Giuseppe Ermondi, Miriam Lorenti, and Giulia Caron
pp 3949–3961Publication Date (Web): July 02, 2004 (Article)
DOI: 10.1021/jm040760a
A Virtual Screening Approach to Finding Novel and Potent Antagonists at the Melanin-Concentrating Hormone 1 Receptor
David E. Clark, Christopher Higgs, Stephen P. Wren, Hazel J. Dyke, Melanie Wong, Dennis Norman, Peter M. Lockey, and Alan G. Roach
pp 3962–3971Publication Date (Web): July 02, 2004 (Article)
DOI: 10.1021/jm040762v
Design, Synthesis, and Structure−Activity Relationship Studies of 3,4,6-Triphenylpyran-2-ones as Selective Cyclooxygenase-2 Inhibitors
P. N. Praveen Rao, Md. Jashim Uddin, and Edward E. Knaus
pp 3972–3990Publication Date (Web): June 26, 2004 (Article)
DOI: 10.1021/jm049939b
A Computational Study of the Binding of Propidium to the Peripheral Anionic Site of Human Acetylcholinesterase
Andrea Cavalli, Giovanni Bottegoni, Caterina Raco, Marco De Vivo, and Maurizio Recanatini
pp 3991–3999Publication Date (Web): June 19, 2004 (Article)
DOI: 10.1021/jm040787u
Macrocyclic Diacylglycerol-bis-lactones as Conformationally Constrained Analogues of Diacylglycerol-lactones. Interactions with Protein Kinase C
Ji-Hye Kang, Su Yeon Kim, Jeewoo Lee, Victor E. Marquez, Nancy E. Lewin, Larry V. Pearce, and Peter M. Blumberg
pp 4000–4007Publication Date (Web): June 29, 2004 (Article)
DOI: 10.1021/jm0497747
Interaction of Noncompetitive Inhibitors with an Immobilized α3β4 Nicotinic Acetylcholine Receptor Investigated by Affinity Chromatography, Quantitative−Structure Activity Relationship Analysis, and Molecular Docking
Krzysztof Jozwiak, Sarangan Ravichandran, Jack R. Collins, and Irving W. Wainer
pp 4008–4021Publication Date (Web): June 29, 2004 (Article)
DOI: 10.1021/jm0400707
A Physiological Model for the Estimation of the Fraction Dose Absorbed in Humans
Stefan Willmann, Walter Schmitt, Jörg Keldenich, Jörg Lippert, and Jennifer B. Dressman
pp 4022–4031Publication Date (Web): July 02, 2004 (Article)
DOI: 10.1021/jm030999b
Synthesis and Aromatase Inhibitory Activity of Novel Pyridine-Containing Isoflavones
Young-Woo Kim, John C Hackett, and Robert W. Brueggemeier
pp 4032–4040Publication Date (Web): July 02, 2004 (Article)
DOI: 10.1021/jm0306024
Synthesis and Biological Activity of New Potential Agonists for the Human Adenosine A2A Receptor
M. Pilar Bosch, Francisco Campos, Itziar Niubó, Gloria Rosell, J. Luis Díaz, J. Brea, M. Isabel Loza, and Angel Guerrero
pp 4041–4053Publication Date (Web): July 07, 2004 (Article)
DOI: 10.1021/jm031143+
Full Text HTMLDiscovery of the Pyrrolo[2,1-f][1,2,4]triazine Nucleus as a New Kinase Inhibitor Template
John T. Hunt, Toomas Mitt, Robert Borzilleri, Johnni Gullo-Brown, Joseph Fargnoli, Brian Fink, Wen-Ching Han, Steven Mortillo, Gregory Vite, Barri Wautlet, Tai Wong, Chiang Yu, Xiaoping Zheng, and Rajeev Bhide
pp 4054–4059Publication Date (Web): June 23, 2004 (Article)
DOI: 10.1021/jm049892u
Probing the Activity Differences of Simple and Complex Brominated Aryl Compounds against 15-Soybean, 15-Human, and 12-Human Lipoxygenase
Erika N. Segraves, Rachana R. Shah, Nathaniel L. Segraves, Tyler A. Johnson, Stephanie Whitman, Jennifer K. Sui, Victor A. Kenyon, Robert H. Cichewicz, Phillip Crews, and Theodore R. Holman
pp 4060–4065Publication Date (Web): June 30, 2004 (Article)
DOI: 10.1021/jm049872s
Direct Influence of C-Terminally Substituted Amino Acids in the Dmt−Tic Pharmacophore on δ-Opioid Receptor Selectivity and Antagonism
Gianfranco Balboni, Severo Salvadori, Remo Guerrini, Lucia Negri, Elisa Giannini, Sharon D. Bryant, Yunden Jinsmaa, and Lawrence H. Lazarus
pp 4066–4071Publication Date (Web): June 23, 2004 (Article)
DOI: 10.1021/jm040033f
Anti-AIDS Agents. 60. Substituted 3‘R,4‘R-Di-O-(−)-camphanoyl-2‘,2‘-dimethyldihydropyrano[2,3-f]chromone (DCP) Analogues as Potent Anti-HIV Agents
Donglei Yu, Chin-Ho Chen, Arnold Brossi, and Kuo-Hsiung Lee
pp 4072–4082Publication Date (Web): June 29, 2004 (Article)
DOI: 10.1021/jm0400505
Phenylguanidines as Selective Nonpeptide Melanocortin-5 Receptor Antagonists
Chen Chen, Jinghua Yu, Beth A. Fleck, Sam R. J. Hoare, John Saunders, and Alan C. Foster
pp 4083–4088Publication Date (Web): June 23, 2004 (Article)
DOI: 10.1021/jm0400496
Design, Synthesis, and Biological Activity of Potent and Selective Inhibitors of Blood Coagulation Factor Xa
J. Adam Willardsen, Danette A. Dudley, Wayne L. Cody, Liguo Chi, Thomas B. McClanahan, Thomas E. Mertz, Ronald E. Potoczak, Lakshmi S. Narasimhan, Debra R. Holland, Stephen T. Rapundalo, and Jeremy J. Edmunds
pp 4089–4099Publication Date (Web): June 26, 2004 (Article)
DOI: 10.1021/jm0497491
Toward the Development of a Synthetic Group A Streptococcal Vaccine of High Purity and Broad Protective Coverage
Anikó Horváth, Colleen Olive, Levente Karpati, Hsien K. Sun, Michael Good, and Istvan Toth
pp 4100–4104Publication Date (Web): July 07, 2004 (Article)
DOI: 10.1021/jm040041w
Brief Articles
Structural Studies on Bioactive Compounds. 39.1 Biological Consequences of the Structural Modification of DHFR-Inhibitory 2,4-Diamino-6-(4-substituted benzylamino-3-nitrophenyl)-6-ethylpyrimidines (‘benzoprims')
Marianne L. Richardson, Karen A. Croughton, Charles S. Matthews, and Malcolm F. G. Stevens
pp 4105–4108Publication Date (Web): June 29, 2004 (Brief Article)
DOI: 10.1021/jm040785+
Book Reviews
The Practice of Medicinal Chemistry Edited by Camille Georges Wermuth. Academic Press, London. 2003. xv + 768 pp. 22 × 28 cm. ISBN 0-12-744481-5. $179.95.
John W. Ellingboe
p 4109Publication Date (Web): June 15, 2004 (Book Review)
DOI: 10.1021/jm0400956
Fundamentals of Medicinal Chemistry By Gareth Thomas. John Wiley and Sons, Ltd., West Sussex, U.K.. 2003. xv + 285 pp. 19 × 24.5 cm. ISBN 0-4708-4307-1. $30.00.
Patrick M. Woster
p 4109Publication Date (Web): June 18, 2004 (Book Review)
DOI: 10.1021/jm040096y
Additions and Corrections
Unraveling the Active Conformation of Urotensin II.
Alfonso Carotenuto, Paolo Grieco, Pietro Campiglia, Ettore Novellino, and Paolo Rovero:
p 4110Publication Date (Web): July 01, 2004 (Addition/Correction)
DOI: 10.1021/jm040837v