Table of Contents
January 16, 2003
Volume 46, Issue 2
Pages 201-318
Letters
Design, Synthesis, and Biological Evaluation of Fluoroneplanocin A as the Novel Mechanism-Based Inhibitor of S-Adenosylhomocysteine Hydrolase
Lak Shin Jeong, Su Jeong Yoo, Kang Man Lee, Mi Jeong Koo, Won Jun Choi, Hea Ok Kim, Hyung Ryong Moon, Min Young Lee, Jae Gyu Park, Sang Kook Lee, and Moon Woo Chun
pp 201–203Publication Date (Web): December 11, 2002 (Letter)
DOI: 10.1021/jm025557z
Hi-Res PDF3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]- pyridine: A Potent and Highly Selective Metabotropic Glutamate Subtype 5 Receptor Antagonist with Anxiolytic Activity
Nicholas D. P. Cosford, Lida Tehrani, Jeffrey Roppe, Edwin Schweiger, Nicholas D. Smith, Jeffrey Anderson, Linda Bristow, Jesse Brodkin, Xiaohui Jiang, Ian McDonald, Sara Rao, Mark Washburn, and Mark A. Varney
pp 204–206Publication Date (Web): December 12, 2002 (Letter)
DOI: 10.1021/jm025570j
Potential Tumor-Selective Nitroimidazolylmethyluracil Prodrug Derivatives: Inhibitors of the Angiogenic Enzyme Thymidine Phosphorylase
Christian Cole, Philip Reigan, Abdul Gbaj, Philip N. Edwards, Kenneth T. Douglas, Ian J. Stratford, Sally Freeman, and Mohammed Jaffar
pp 207–209Publication Date (Web): December 12, 2002 (Letter)
DOI: 10.1021/jm020964w
Tricyclic Benzimidazoles as Potent Poly(ADP-ribose) Polymerase-1 Inhibitors
Donald J. Skalitzky, Joseph T. Marakovits, Karen A. Maegley, Anne Ekker, Xiao-Hong Yu, Zdenek Hostomsky, Stephen E. Webber, Brian W. Eastman, Robert Almassy, and Jianke LiNicola J. Curtin, David R. Newell, and A. Hilary CalvertRoger J. Griffin and Bernard T. Golding
pp 210–213Publication Date (Web): December 17, 2002 (Letter)
DOI: 10.1021/jm0255769
Articles
Competitive Antagonism of AMPA Receptors by Ligands of Different Classes: Crystal Structure of ATPO Bound to the GluR2 Ligand-Binding Core, in Comparison with DNQX
Anders Hogner, Jeremy R. Greenwood, Tommy Liljefors, Marie-Louise Lunn, Jan Egebjerg, Ingrid K. Larsen, Eric Gouaux, and Jette S. Kastrup
pp 214–221Publication Date (Web): December 12, 2002 (Article)
DOI: 10.1021/jm020989v
Aloisines, a New Family of CDK/GSK-3 Inhibitors. SAR Study, Crystal Structure in Complex with CDK2, Enzyme Selectivity, and Cellular Effects
Yvette Mettey, Marie Gompel, Virginie Thomas, Matthieu Garnier, Maryse Leost, Irène Ceballos-Picot, Martin Noble, Jane Endicott, Jean-michel Vierfond, and Laurent Meijer
pp 222–236Publication Date (Web): December 18, 2002 (Article)
DOI: 10.1021/jm020319p
Structure−Activity Relationship of Imidazo[1,2-a]pyridines as Ligands for Detecting β-Amyloid Plaques in the Brain
Zhi-Ping Zhuang, Mei-Ping Kung, Alan Wilson, Chi-Wan Lee, Karl Plössl, Catherine Hou, David M. Holtzman, and Hank F. Kung
pp 237–243Publication Date (Web): December 18, 2002 (Article)
DOI: 10.1021/jm020351j
Macrocyclization in the Design of Grb2 SH2 Domain-Binding Ligands Exhibiting High Potency in Whole-Cell Systems
Chang-Qing Wei, Yang Gao, Kyeong Lee, Ribo Guo, Bihua Li, Manchao Zhang, Dajun Yang, and Terrence R. Burke, Jr.
pp 244–254Publication Date (Web): December 12, 2002 (Article)
DOI: 10.1021/jm0203635
Novel Hexahydrospiro[piperidine-4,1‘-pyrrolo[3,4-c]pyrroles]: Highly Selective Small-Molecule Nociceptin/Orphanin FQ Receptor Agonists
Sabine Kolczewski, Geo Adam, Andrea M. Cesura, François Jenck, Michael Hennig, Thomas Oberhauser, Sonia M. Poli, Felix Rössler, Stephan Röver, Jürgen Wichmann, and Frank M. Dautzenberg
pp 255–264Publication Date (Web): December 11, 2002 (Article)
DOI: 10.1021/jm0209174
Synthesis and Structure−Affinity Relationship Investigations of 5-Heteroaryl-Substituted Analogues of the Antipsychotic Sertindole. A New Class of Highly Selective α1 Adrenoceptor Antagonists
Thomas Balle, Jens Perregaard, Martha Teresa Ramirez, Anna Kirstine Larsen, Karina Krøjer Søby, Tommy Liljefors, and Kim Andersen
pp 265–283Publication Date (Web): December 11, 2002 (Article)
DOI: 10.1021/jm020938y
Identification of Phenylisoxazolines as Novel and Viable Antibacterial Agents Active against Gram-Positive Pathogens
Michael R. Barbachyn, Gary J. Cleek, Lester A. Dolak, Stuart A. Garmon, Joel Morris, Eric P. Seest, Richard C. Thomas, Dana S. Toops, William Watt, Donn G. Wishka, Charles W. Ford, Gary E. Zurenko, Judith C. Hamel, Ronda D. Schaadt, Douglas Stapert, Betty H. Yagi, Wade J. Adams, Janice M. Friis, J. Gregory Slatter, James P. Sams, Nancee L. Oien, Matthew J. Zaya, Larry C. Wienkers, and Michael A. Wynalda
pp 284–302Publication Date (Web): December 13, 2002 (Article)
DOI: 10.1021/jm020248u
Discovery of a Long-Chain Carbamoyl Aminocarnitine Derivative, a Reversible Carnitine Palmitoyltransferase Inhibitor with Antiketotic and Antidiabetic Activity
Fabio Giannessi, Pompeo Pessotto, Emanuela Tassoni, Piero Chiodi, Roberto Conti, Francesco De Angelis, Natalina Dell'Uomo, Roberto Catini, Roberto Deias, Maria Ornella Tinti, Paolo Carminati, and Arduino Arduini
pp 303–309Publication Date (Web): December 17, 2002 (Article)
DOI: 10.1021/jm020979u
Brief Articles
Synthesis and Benzodiazepine Receptor Affinity of Pyrazolo[1,5-a]pyrimidine Derivatives. 3. New 6-(3-Thienyl) Series as α1 Selective Ligands
Silvia Selleri, Fabrizio Bruni, Camilla Costagli, Annarella Costanzo, Gabriella Guerrini, Giovanna Ciciani, Paola Gratteri, Claudia Bonaccini, Petra Malmberg Aiello, François Besnard, Stephane Renard, Barbara Costa, and Claudia Martini
pp 310–313Publication Date (Web): December 11, 2002 (Brief Article)
DOI: 10.1021/jm020999w
The Role of the Side Chain in Determining Relative δ- and κ-Affinity in C5‘-Substituted Analogues of Naltrindole
Shannon L. Black, Andrew R. Jales, Wolfgang Brandt, John W. Lewis, and Stephen M. Husbands
pp 314–317Publication Date (Web): December 10, 2002 (Brief Article)
DOI: 10.1021/jm020997b
Book Reviews
Drug−Membrane Interactions. Analysis, Drug Distribution, Modeling. Methods and Principles in Medicinal Chemistry, Volume 15 By J. K. Seydel and M. Wiese. Wiley-VCH, Weinheim, Germany. 2002. xix + 349 pp. 17.5 × 24.5 cm. ISBN 3 527 3042 7. $128.00.
David J. Triggle
p 318Publication Date (Web): December 07, 2002 (Book Review)
DOI: 10.1021/jm0204688