Table of Contents
January 3, 2002
Volume 45, Issue 1
Pages 1-249
Articles
Design and Synthesis of Pyrrolidine-5,5-trans-lactams (5-Oxohexahydropyrrolo[3,2-b]pyrroles) as Novel Mechanism-Based Inhibitors of Human Cytomegalovirus Protease. 2. Potency and Chirality
Alan D. Borthwick, Andrew J. Crame, Peter F. Ertl, Anne M. Exall, Terry M. Haley, Graham J. Hart, Andrew M. Mason, Andrew M. K. Pennell, Onkar M. P. Singh, Gordon G. Weingarten, and James M. Woolven
pp 1–18Publication Date (Web): December 05, 2001 (Article)
DOI: 10.1021/jm0102203
Hi-Res PDFNovel 1-Hydroxyazole Bioisosteres of Glutamic Acid. Synthesis, Protolytic Properties, and Pharmacology
Tine B. Stensbøl, Peter Uhlmann, Sandrine Morel, Birgitte L. Eriksen, Jakob Felding, Hasse Kromann, Mette B. Hermit, Jeremy R. Greenwood, Hans Braüner-Osborne, Ulf Madsen, Finn Junager, Povl Krogsgaard-Larsen, Mikael Begtrup, and Per Vedsø
pp 19–31Publication Date (Web): December 04, 2001 (Article)
DOI: 10.1021/jm010303j
α2-Adrenoreceptors Profile Modulation and High Antinociceptive Activity of (S)-(−)-2-[1-(Biphenyl-2-yloxy)ethyl]-4,5-dihydro-1H-imidazole
Francesco Gentili, Pascal Bousquet, Livio Brasili, Mariangela Caretto, Antonio Carrieri, Monique Dontenwill, Mario Giannella, Gabriella Marucci, Marina Perfumi, Alessandro Piergentili, Wilma Quaglia, Carla Rascente, and Maria Pigini
pp 32–40Publication Date (Web): December 04, 2001 (Article)
DOI: 10.1021/jm0110082
Pharmacophore Mapping of a Series of 2,4-Diamino-5-deazapteridine Inhibitors of Mycobacterium avium Complex Dihydrofolate Reductase
Asim Kumar Debnath
pp 41–53Publication Date (Web): December 27, 2001 (Article)
DOI: 10.1021/jm010360c
New Serotonin 5-HT2A, 5-HT2B, and 5-HT2C Receptor Antagonists: Synthesis, Pharmacology, 3D-QSAR, and Molecular Modeling of (Aminoalkyl)benzo and Heterocycloalkanones
José Brea, Jordi Rodrigo, Antonio Carrieri, Ferran Sanz, M. Isabel Cadavid, María J. Enguix, María Villazón, Guadalupe Mengod, Yolanda Caro, Christian F. Masaguer, Enrique Raviña, Nuria B. Centeno, Angelo Carotti, and M. Isabel Loza
pp 54–71Publication Date (Web): December 08, 2001 (Article)
DOI: 10.1021/jm011014y
Hierarchy of Simulation Models in Predicting Structure and Energetics of the Src SH2 Domain Binding to Tyrosyl Phosphopeptides
Gennady M. Verkhivker, Djamal Bouzida, Daniel K. Gehlhaar, Paul A. Rejto, Lana Schaffer, Sandra Arthurs, Anthony B. Colson, Stephan T. Freer, Veda Larson, Brock A. Luty, Tami Marrone, and Peter W. Rose
pp 72–89Publication Date (Web): November 09, 2001 (Article)
DOI: 10.1021/jm0101141
Structure-Based Design and Characterization of Novel Platforms for Ricin and Shiga Toxin Inhibition
Darcie J. Miller, Kabyadi Ravikumar, Huafeng Shen, Jung-Keun Suh, Sean M. Kerwin, and Jon D. Robertus
pp 90–98Publication Date (Web): November 21, 2001 (Article)
DOI: 10.1021/jm010186s
Synthesis of Novel Cationic Lipids: Effect of Structural Modification on the Efficiency of Gene Transfer
James A. Heyes, Dan Niculescu-Duvaz, Robert G. Cooper, and Caroline J. Springer
pp 99–114Publication Date (Web): December 06, 2001 (Article)
DOI: 10.1021/jm010918g
7-Substituted 5-Amino-2-(2-furyl)pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as A2A Adenosine Receptor Antagonists: A Study on the Importance of Modifications at the Side Chain on the Activity and Solubility
Pier Giovanni Baraldi, Barbara Cacciari, Romeo Romagnoli, Giampiero Spalluto, Angela Monopoli, Ennio Ongini, Katia Varani, and Pier Andrea Borea
pp 115–126Publication Date (Web): December 06, 2001 (Article)
DOI: 10.1021/jm010924c
Inotropic Activity of Hydroindene Amidinohydrazones
Luis G. Sevillano, Concepción P. Melero, Esther Caballero, Fernando Tomé, Lionel G. Lelièvre, Käthi Geering, Gilles Crambert, Rosalía Carrón, Manuel Medarde, and Arturo San Feliciano
pp 127–136Publication Date (Web): December 08, 2001 (Article)
DOI: 10.1021/jm0109309
Development of a Virtual Screening Method for Identification of “Frequent Hitters” in Compound Libraries
Olivier Roche, Petra Schneider, Jochen Zuegge, Wolfgang Guba, Manfred Kansy, Alexander Alanine, Konrad Bleicher, Franck Danel, Eva-Maria Gutknecht, Mark Rogers-Evans, Werner Neidhart, Henri Stalder, Michael Dillon, Eric Sjögren, Nader Fotouhi, Paul Gillespie, Robert Goodnow, William Harris, Phil Jones, Mikio Taniguchi, Shinji Tsujii, Wolfgang von der Saal, Gerd Zimmermann, and Gisbert Schneider
pp 137–142Publication Date (Web): December 04, 2001 (Article)
DOI: 10.1021/jm010934d
Anti-Helicobacter pylori Agents. 5. 2-(Substituted guanidino)-4-arylthiazoles and Aryloxazole Analogues
Yousuke Katsura, Shigetaka Nishino, Yoshikazu Inoue, Kazuo Sakane, Yoshimi Matsumoto, Chizu Morinaga, Hirohumi Ishikawa, and Hisashi Takasugi
pp 143–150Publication Date (Web): November 16, 2001 (Article)
DOI: 10.1021/jm010217j
Rational Determination of Transfer Free Energies of Small Drugs across the Water−Oil Interface
Delphine Bas, Delphine Dorison-Duval, Stéphanie Moreau, Pierre Bruneau, and Christophe Chipot
pp 151–159Publication Date (Web): November 27, 2001 (Article)
DOI: 10.1021/jm010289a
Design, Synthesis, and Discovery of Novel trans-Stilbene Analogues as Potent and Selective Human Cytochrome P450 1B1 Inhibitors
Sanghee Kim, Hyojin Ko, Jae Eun Park, Sungkyu Jung, Sang Kwang Lee, and Young-Jin Chun
pp 160–164Publication Date (Web): December 07, 2001 (Article)
DOI: 10.1021/jm010298j
Improvement in the Selectivity and Metabolic Stability of the Serotonin 5-HT1A Ligand, S 15535: A Series of cis- and trans-2-(Arylcycloalkylamine) 1-Indanols
Jean-Louis Peglion, Bertrand Goument, Nicole Despaux, Valérie Charlot, Hélène Giraud, Christian Nisole, Adrian Newman-Tancredi, Anne Dekeyne, Marc Bertrand, Patrick Genissel, and Mark J. Millan
pp 165–176Publication Date (Web): December 05, 2001 (Article)
DOI: 10.1021/jm010975+
Full Text HTMLDesign and Synthesis of Potent Nonpeptidic Farnesyltransferase Inhibitors Based on a Terphenyl Scaffold
Junko Ohkanda, Jeffrey W. Lockman, Mohit A. Kothare, Yimin Qian, Michelle A. Blaskovich, Said M. Sebti, and Andrew D. Hamilton
pp 177–188Publication Date (Web): December 08, 2001 (Article)
DOI: 10.1021/jm0103099
Synthesis and Inotropic Activity of 1-(O-Aminoalkyloximes) of Perhydroindene Derivatives as Simplified Digitalis-like Compounds Acting on the Na+,K+-ATPase
Alberto Cerri, Nicoletta Almirante, Paolo Barassi, Alessandra Benicchio, Sergio De Munari, Giuseppe Marazzi, Isabella Molinari, Fulvio Serra, and Piero Melloni
pp 189–207Publication Date (Web): November 22, 2001 (Article)
DOI: 10.1021/jm011001k
Methanocarba Modification of Uracil and Adenine Nucleotides: High Potency of Northern Ring Conformation at P2Y1, P2Y2, P2Y4, and P2Y11 but Not P2Y6 Receptors
Hak Sung Kim, R. Gnana Ravi, Victor E. Marquez, Savitri Maddileti, Anna-Karin Wihlborg, David Erlinge, Malin Malmsjö, José L. Boyer, T. Kendall Harden, and Kenneth A. Jacobson
pp 208–218Publication Date (Web): November 22, 2001 (Article)
DOI: 10.1021/jm010369e
Phenoxyphenyl Sulfone N-Formylhydroxylamines (Retrohydroxamates) as Potent, Selective, Orally Bioavailable Matrix Metalloproteinase Inhibitors
Carol K. Wada, James H. Holms, Michael L. Curtin, Yujia Dai, Alan S. Florjancic, Robert B. Garland, Yan Guo, H. Robin Heyman, Jamie R. Stacey, Douglas H. Steinman, Daniel H. Albert, Jennifer J. Bouska, Ildiko N. Elmore, Carole L. Goodfellow, Patrick A. Marcotte, Paul Tapang, Douglas W. Morgan, Michael R. Michaelides, and Steven K. Davidsen
pp 219–232Publication Date (Web): December 06, 2001 (Article)
DOI: 10.1021/jm0103920
Inhibition of Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium Dihydrofolate Reductases by 2,4-Diamino-5-[2-methoxy-5-(ω-carboxyalkyloxy)benzyl]pyrimidines: Marked Improvement in Potency Relative to Trimethoprim and Species Selectivity Relative to Piritrexim
Andre Rosowsky, Ronald A. Forsch, and Sherry F. Queener
pp 233–241Publication Date (Web): December 06, 2001 (Article)
DOI: 10.1021/jm010407u
Synthesis of New Dihydroindeno[1,2-c]isoquinoline and Indenoisoquinolinium Chloride Topoisomerase I Inhibitors Having High in Vivo Anticancer Activity in the Hollow Fiber Animal Model
Muthusamy Jayaraman, Brian M. Fox, Melinda Hollingshead, Glenda Kohlhagen, Yves Pommier, and Mark Cushman
pp 242–249Publication Date (Web): December 06, 2001 (Article)
DOI: 10.1021/jm000498f