Table of Contents
April 25, 2002
Volume 45, Issue 9
Pages 1737-1958
Letters
A Computational Ensemble Pharmacophore Model for Identifying Substrates of P-Glycoprotein
Julie E. Penzotti, Michelle L. Lamb, Erik Evensen, and Peter D. J. Grootenhuis
pp 1737–1740Publication Date (Web): March 26, 2002 (Letter)
DOI: 10.1021/jm0255062
Hi-Res PDF Articles
Structure-Based Design and Synthesis of 2-Benzylidene-benzofuran-3-ones as Flavopiridol Mimics
Joseph Schoepfer, Heinz Fretz, Bhabatosh Chaudhuri, Lionel Muller, Egge Seeber, Laurent Meijer, Olivier Lozach, Eric Vangrevelinghe, and Pascal Furet
pp 1741–1747Publication Date (Web): March 26, 2002 (Article)
DOI: 10.1021/jm0108348
Exploration of the Pharmacophore of 3-Alkyl-5-Arylimidazolidinediones as New CB1 Cannabinoid Receptor Ligands and Potential Antagonists: Synthesis, Lipophilicity, Affinity, and Molecular Modeling
Frédéric Ooms, Johan Wouters, Olivier Oscari, Thierry Happaerts, Géraldine Bouchard, Pierre-Alain Carrupt, Bernard Testa, and Didier M. Lambert
pp 1748–1756Publication Date (Web): March 26, 2002 (Article)
DOI: 10.1021/jm010896y
Structure-Based Design of Novel Potent Nonpeptide Thrombin Inhibitors
Norbert H. Hauel, Herbert Nar, Henning Priepke, Uwe Ries, Jean-Marie Stassen, and Wolfgang Wienen
pp 1757–1766Publication Date (Web): March 26, 2002 (Article)
DOI: 10.1021/jm0109513
Vinyl Sulfide Cyclized Analogues of Angiotensin II with High Affinity and Full Agonist Activity at the AT1 Receptor
Petra Johannesson, Gunnar Lindeberg, Anja Johansson, Gregory V. Nikiforovich, Adolf Gogoll, Barbro Synnergren, Madeleine Le Grèves, Fred Nyberg, Anders Karlén, and Anders Hallberg
pp 1767–1777Publication Date (Web): March 30, 2002 (Article)
DOI: 10.1021/jm011063a
Binding Mode Analysis of 3-(4-Benzoyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamide: A New Synthetic Histone Deacetylase Inhibitor Inducing Histone Hyperacetylation, Growth Inhibition, and Terminal Cell Differentiation
Antonello Mai, Silvio Massa, Rino Ragno, Monica Esposito, Gianluca Sbardella, Giuseppina Nocca, Roberto Scatena, Florian Jesacher, Peter Loidl, and Gerald Brosch
pp 1778–1784Publication Date (Web): March 26, 2002 (Article)
DOI: 10.1021/jm011088+
Full Text HTMLInvestigation of Potential Bioisosteric Replacements for the Carboxyl Groups of Peptidomimetic Inhibitors of Protein Tyrosine Phosphatase 1B: Identification of a Tetrazole-Containing Inhibitor with Cellular Activity
Charlotta Liljebris, Scott D. Larsen, Derek Ogg, Barbara J. Palazuk, and John E. Bleasdale
pp 1785–1798Publication Date (Web): March 29, 2002 (Article)
DOI: 10.1021/jm011100y
Identification of Nonpeptidic Urotensin II Receptor Antagonists by Virtual Screening Based on a Pharmacophore Model Derived from Structure−Activity Relationships and Nuclear Magnetic Resonance Studies on Urotensin II
Stefanie Flohr, Michael Kurz, Evi Kostenis, Alexandre Brkovich, Alain Fournier, and Thomas Klabunde
pp 1799–1805Publication Date (Web): March 20, 2002 (Article)
DOI: 10.1021/jm0111043
Cyclodextrin-Derived Host Molecules as Reversal Agents for the Neuromuscular Blocker Rocuronium Bromide: Synthesis and Structure−Activity Relationships
Julia M. Adam, D. Jonathan Bennett, Anton Bom, John K. Clark, Helen Feilden, Edward J. Hutchinson, Ronald Palin, Alan Prosser, David C. Rees, Georgina M. Rosair, Donald Stevenson, Gary J. Tarver, and Ming-Qiang Zhang
pp 1806–1816Publication Date (Web): March 21, 2002 (Article)
DOI: 10.1021/jm011107f
Polysaccharide−Oligoamine Based Conjugates for Gene Delivery
Tony Azzam, Hagit Eliyahu, Libi Shapira, Michal Linial, Yechezkel Barenholz, and Abraham J. Domb
pp 1817–1824Publication Date (Web): March 29, 2002 (Article)
DOI: 10.1021/jm0105528
Rational Design, Synthesis, and Biological Activity of Novel Conformationally Restricted Vitamin D Analogues, (22R)- and (22S)-22-Ethyl-1,25-dihydroxy-23,24-didehydro-24a,24b-dihomo-20-epivitamin D3
Hiroyuki Masuno, Keiko Yamamoto, Xinxiang Wang, Mihwa Choi, Hiroshi Ooizumi, Toshimasa Shinki, and Sachiko Yamada
pp 1825–1834Publication Date (Web): March 27, 2002 (Article)
DOI: 10.1021/jm0105631
Preparation and Characterization of Platinum(II) and (IV) Complexes of 1,3-Diaminepropane and 1,4-Diaminebutane: Circumvention of Cisplatin Resistance and DNA Interstrand Cross-Link Formation in CH1cisR Ovarian Tumor Cells
Amparo Alvarez-Valdés, José Manuel Pérez, Isabel López-Solera, Raúl Lannegrand, José Manuel Continente, Pilar Amo-Ochoa, María José Camazón, Xavier Solans, Mercè Font-Bardía, and Carmen Navarro-Ranninger
pp 1835–1844Publication Date (Web): March 20, 2002 (Article)
DOI: 10.1021/jm010968l
5‘-Deoxy Congeners of 9-(3-Amido-3-deoxy-β-d-xylofuranosyl)-N6-cyclopentyladenine: New Adenosine A1 Receptor Antagonists and Inverse Agonists
Serge Van Calenbergh, Andreas Link, Shelly Fujikawa, Rianne A. F. de Ligt, Veerle Vanheusden, Abolfasl Golisade, Norbert M. Blaton, Jef Rozenski, Adriaan P. IJzerman, and Piet Herdewijn
pp 1845–1852Publication Date (Web): March 16, 2002 (Article)
DOI: 10.1021/jm0110439
Synthesis of Nitroindole Derivatives with High Affinity and Selectivity for Melatoninergic Binding Sites MT3
Véronique Leclerc, Saïd Yous, Philippe Delagrange, Jean A. Boutin, Pierre Renard, and Daniel Lesieur
pp 1853–1859Publication Date (Web): March 27, 2002 (Article)
DOI: 10.1021/jm011053+
Structure−Activity Relationships of Methoctramine-Related Polyamines as Muscular Nicotinic Receptor Noncompetitive Antagonists. 2.1 Role of Polymethylene Chain Lengths Separating Amine Functions and of Substituents on the Terminal Nitrogen Atoms
Michela Rosini, M. Gabriele Bixel, Gabriella Marucci, Roberta Budriesi, Michael Krauss, Maria L. Bolognesi, Anna Minarini, Vincenzo Tumiatti, Ferdinand Hucho, and Carlo Melchiorre
pp 1860–1878Publication Date (Web): March 21, 2002 (Article)
DOI: 10.1021/jm011067f
Halogenated Diazirines as Photolabel Mimics of the Inhaled Haloalkane Anesthetics
Roderic G. Eckenhoff, Frank J. Knoll, Eric P. Greenblatt, and William P. Dailey
pp 1879–1886Publication Date (Web): March 28, 2002 (Article)
DOI: 10.1021/jm0104926
3-Heteroaryl-2-pyridones: Benzodiazepine Site Ligands with Functional Selectivity for α2/α3-Subtypes of Human GABAA Receptor-Ion Channels
Ian Collins, Christopher Moyes, William B. Davey, Michael Rowley, Frances A. Bromidge, Kathleen Quirk, John R. Atack, Ruth M. McKernan, Sally-Ann Thompson, Keith Wafford, Gerard R. Dawson, Andrew Pike, Bindi Sohal, Nancy N. Tsou, Richard G. Ball, and José L. Castro
pp 1887–1900Publication Date (Web): March 29, 2002 (Article)
DOI: 10.1021/jm0110789
Synthesis and Biological Evaluation of Structurally Highly Modified Analogues of the Antimitotic Natural Product Curacin A
Peter Wipf, Jonathan T. Reeves, Raghavan Balachandran, and Billy W. Day
pp 1901–1917Publication Date (Web): March 28, 2002 (Article)
DOI: 10.1021/jm0105171
6-[2-(Phosphonomethoxy)alkoxy]pyrimidines with Antiviral Activity
Antonín Holý, Ivan Votruba, Milena Masojídková, Graciela Andrei, Robert Snoeck, Lieve Naesens, Erik De Clercq, and Jan Balzarini
pp 1918–1929Publication Date (Web): March 27, 2002 (Article)
DOI: 10.1021/jm011095y
Further Studies on Conformationally Constrained Tricyclic Tropane Analogues and Their Uptake Inhibition at Monoamine Transporter Sites: Synthesis of (Z)-9-(Substituted arylmethylene)-7-azatricyclo[4.3.1.03,7]decanes as a Novel Class of Serotonin Transporter Inhibitors
Ao Zhang, Guochun Zhou, Alexander Hoepping, Jayanta Mukhopadhyaya, Kenneth M. Johnson, Mei Zhang, and Alan P. Kozikowski
pp 1930–1941Publication Date (Web): March 27, 2002 (Article)
DOI: 10.1021/jm0105373
Synthesis of N-[4-[1-Ethyl-2-(2,4-diaminofuro[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-l-glutamic Acid as an Antifolate1
Aleem Gangjee, Yibin Zeng, John J. McGuire, and Roy L. Kisliuk
pp 1942–1948Publication Date (Web): March 21, 2002 (Article)
DOI: 10.1021/jm010575m
Studies on the Synthesis and Opioid Agonistic Activities of Mitragynine-Related Indole Alkaloids: Discovery of Opioid Agonists Structurally Different from Other Opioid Ligands
Hiromitsu Takayama, Hayato Ishikawa, Mika Kurihara, Mariko Kitajima, Norio Aimi, Dhavadee Ponglux, Fumi Koyama, Kenjiro Matsumoto, Tomoyuki Moriyama, Leonard T. Yamamoto, Kazuo Watanabe, Toshihiko Murayama, and Syunji Horie
pp 1949–1956Publication Date (Web): March 20, 2002 (Article)
DOI: 10.1021/jm010576e
Additions and Corrections
2,4-Diaminothieno[2,3-d]pyrimidine Lipophilic Antifolates as Inhibitors of Pneumocystis carinii and Toxoplasma gondii Dihydrofolate Reductase.
Andre Rosowsky, Andrew T. Papoulis, and Sherry F. Queener:
p 1957Publication Date (Web): March 14, 2002 (Addition/Correction)
DOI: 10.1021/jm020059b
2,4-Diamino-6,7-dihydro-5H-cyclopenta[d]pyrimidine Analogues of Trimethoprim as Inhibitors of Pneumocystis carinii and Toxoplasma gondii Dihydrofolate Reductase.
Andre Rosowsky, Andrew Papoulis, and Sherry F. Queener:
p 1957Publication Date (Web): March 14, 2002 (Addition/Correction)
DOI: 10.1021/jm020060a
Synthesis and Antiparasitic and Antitumor Activity of 2,4-Diamino-6-(arylmethyl)-5,6,7,8-tetrahydroquinazoline Analogues of Piritrexim.
Andre Rosowsky, Andrew Papoulis, Ronald A. Forsch, and Sherry F. Queener:
pp 1957–1958Publication Date (Web): March 14, 2002 (Addition/Correction)
DOI: 10.1021/jm0200613
Drug Metabolism Databases and High-Throughput Testing During Drug Design and Development.
Rory P. Remmel:
p 1958Publication Date (Web): April 18, 2002 (Addition/Correction)
DOI: 10.1021/jm000383b