Table of Contents
October 10, 2002
Volume 45, Issue 21
Pages 4589-4800
About the Cover: Model of the histone deacetylase inhibitor, 3-(4-benzoyl-1-methyl-1H-2-pyrrole)-N-hydroxy-
Letters
Design and Pharmacology of N-[(3R)-1,2,3,4-Tetrahydroisoquinolinium- 3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)- 2-[4-cyclohexyl-4-(1H-1,2,4-triazol- 1-ylmethyl)piperidin-1-yl]-2-oxoethylamine (1), a Potent, Selective, Melanocortin Subtype-4 Receptor Agonist
Iyassu K. Sebhat, William J. Martin, Zhixiong Ye, Khaled Barakat, Ralph T. Mosley, David B. R. Johnston, Raman Bakshi, Brenda Palucki, David H. Weinberg, Tanya MacNeil, Rubana N. Kalyani, Rui Tang, Ralph A. Stearns, Randy R. Miller, Constantin Tamvakopoulos, Alison M. Strack, Erin McGowan, Doreen E. Cashen, Jennifer E. Drisko, Gary J. Hom, Andrew D. Howard, D. Euan MacIntyre, Lex H. T. van der Ploeg, Arthur A. Patchett, and Ravi P. Nargund
pp 4589–4593Publication Date (Web): September 14, 2002 (Letter)
DOI: 10.1021/jm025539h
Hi-Res PDFInteractive SAR Studies: Rational Discovery of Super-Potent and Highly Selective Dopamine D3 Receptor Antagonists and Partial Agonists
Laura Bettinetti, Karin Schlotter, Harald Hübner, and Peter Gmeiner
pp 4594–4597Publication Date (Web): September 06, 2002 (Letter)
DOI: 10.1021/jm025558r
Articles
Cyclosporins: Structure−Activity Relationships for the Inhibition of the Human MDR1 P-Glycoprotein ABC Transporter
Francis Loor, Françoise Tiberghien, Tom Wenandy, Agnès Didier, and René Traber
pp 4598–4612Publication Date (Web): September 12, 2002 (Article)
DOI: 10.1021/jm0109863
Cyclosporins: Structure−Activity Relationships for the Inhibition of the Human FPR1 Formylpeptide Receptor
Francis Loor, Françoise Tiberghien, Tom Wenandy, Agnès Didier, and Rene Traber
pp 4613–4628Publication Date (Web): September 12, 2002 (Article)
DOI: 10.1021/jm010987v
Development of Novel EDG3 Antagonists Using a 3D Database Search and Their Structure−Activity Relationships
Yuuki Koide, Takeshi Hasegawa, Atsuo Takahashi, Akira Endo, Naoki Mochizuki, Masako Nakagawa, and Atsushi Nishida
pp 4629–4638Publication Date (Web): September 13, 2002 (Article)
DOI: 10.1021/jm020080c
Docking of Flexible Molecules Using Multiscale Ligand Representations
Meir Glick, Guy H. Grant, and W. Graham Richards
pp 4639–4646Publication Date (Web): September 06, 2002 (Article)
DOI: 10.1021/jm020830i
Use of the Kohonen Neural Network for Rapid Screening of Ex Vivo Anti-HIV Activity of Styrylquinolines
Jaroslaw Polanski, Fatima Zouhiri, Laurence Jeanson, Didier Desmaële, Jean d'Angelo, Jean-François Mouscadet, Rafal Gieleciak, Johann Gasteiger, and Marc Le Bret
pp 4647–4654Publication Date (Web): September 13, 2002 (Article)
DOI: 10.1021/jm020845g
Synthesis and Pharmacological Evaluation of 1-[(1,2-Diphenyl-1H-4-imidazolyl)methyl]-4-phenylpiperazines with Clozapine-Like Mixed Activities at Dopamine D2, Serotonin, and GABAA Receptors
Battistina Asproni, Amedeo Pau, Mauro Bitti, Marilena Melosu, Riccardo Cerri, Laura Dazzi, Emanuele Seu, Elisabetta Maciocco, Enrico Sanna, Fabio Busonero, Giuseppe Talani, Luca Pusceddu, Cosimo Altomare, Giuseppe Trapani, and Giovanni Biggio
pp 4655–4668Publication Date (Web): September 17, 2002 (Article)
DOI: 10.1021/jm020848t
Parallel Synthesis of Potent, Pyrazole-Based Inhibitors of Helicobacter pylori Dihydroorotate Dehydrogenase
Tasir S. Haque, Seifu Tadesse, Jovita Marcinkeviciene, M. John Rogers, Christine Sizemore, Lisa M. Kopcho, Karen Amsler, Lisa D. Ecret, Dong Liang Zhan, Frank Hobbs, Andrew Slee, George L. Trainor, Andrew M. Stern, Robert A. Copeland, and Andrew P. Combs
pp 4669–4678Publication Date (Web): September 06, 2002 (Article)
DOI: 10.1021/jm020112w
Design, Synthesis, and Evaluation of New Noncross-Linking Pyrrolobenzodiazepine Dimers with Efficient DNA Binding Ability and Potent Antitumor Activity
Ahmed Kamal, G. Ramesh, N. Laxman, P. Ramulu, O. Srinivas, K. Neelima, Anand K. Kondapi, V. B. Sreenu, and H. A. Nagarajaram
pp 4679–4688Publication Date (Web): September 17, 2002 (Article)
DOI: 10.1021/jm020124h
Synthesis and Antiinflammatory Evaluation of 9-Anilinoacridine and 9-Phenoxyacridine Derivatives
Yeh-Long Chen, Chih-Ming Lu, I-Li Chen, Lo-Ti Tsao, and Jih-Pyang Wang
pp 4689–4694Publication Date (Web): September 10, 2002 (Article)
DOI: 10.1021/jm020102v
Imidazole Inhibitors of Cytokine Release: Probing Substituents in the 2 Position
Stefan A. Laufer, Hans-Günther Striegel, and Gerd K. Wagner
pp 4695–4705Publication Date (Web): September 13, 2002 (Article)
DOI: 10.1021/jm020873z
Design and Synthesis of a Pro-Drug of Vinblastine Targeted at Treatment of Prostate Cancer with Enhanced Efficacy and Reduced Systemic Toxicity
Stephen F. Brady, Joseph M. Pawluczyk, Patricia K. Lumma, Dong-Mei Feng, Jenny M. Wai, Raymond Jones, Deborah DeFeo-Jones, Bradley K. Wong, Cynthia Miller-Stein, Jiunn H. Lin, Allen Oliff, Roger M. Freidinger, and Victor M. Garsky
pp 4706–4715Publication Date (Web): September 05, 2002 (Article)
DOI: 10.1021/jm020139f
New PET Imaging Agent for the Serotonin Transporter: [18F]ACF (2-[(2-Amino-4-chloro-5-fluorophenyl)thio]-N,N-dimethyl-benzenmethanamine)
Shunichi Oya, Seok Rye Choi, Heinz Coenen, and Hank F. Kung
pp 4716–4723Publication Date (Web): September 05, 2002 (Article)
DOI: 10.1021/jm020167y
Homoazanicotine: A Structure-Affinity Study for Nicotinic Acetylcholine (nACh) Receptor Binding
G. Ferretti, M. Dukat, M. Giannella, A. Piergentili, M. Pigini, W. Quaglia, M. I. Damaj, B. R. Martin, and R. A. Glennon
pp 4724–4731Publication Date (Web): September 07, 2002 (Article)
DOI: 10.1021/jm020188s
Antimalarial Activity of Yingzhaosu A Analogues
Hye-Sook Kim, Khurshida Begum, Naoki Ogura, Yusuke Wataya, Takahiro Tokuyasu, Araki Masuyama, Masatomo Nojima, and Kevin J. McCullough
pp 4732–4736Publication Date (Web): September 11, 2002 (Article)
DOI: 10.1021/jm020208q
Potent and Long-Acting Corticotropin Releasing Factor (CRF) Receptor 2 Selective Peptide Competitive Antagonists
J. Rivier, J. Gulyas, D. Kirby, W. Low, M. H. Perrin, K. Kunitake, M. DiGruccio, J. Vaughan, J. C. Reubi, B. Waser, S. C. Koerber, V. Martinez, L. Wang, Y. Taché, and W. Vale
pp 4737–4747Publication Date (Web): September 12, 2002 (Article)
DOI: 10.1021/jm0202122
The Effect of Exchanging Various Substituents at the 2-Position of 2-Methoxyestradiol on Cytotoxicity in Human Cancer Cell Cultures and Inhibition of Tubulin Polymerization
Mark Cushman, Arasambattu K. Mohanakrishnan, Melinda Hollingshead, and Ernest Hamel
pp 4748–4754Publication Date (Web): September 17, 2002 (Article)
DOI: 10.1021/jm020218r
Synthesis, Nicotinic Acetylcholine Receptor Binding, and Antinociceptive Properties of 2-exo-2-(2‘,3‘-Disubstituted 5‘-pyridinyl)-7-azabicyclo[2.2.1]heptanes: Epibatidine Analogues
F. Ivy Carroll, Jeffrey R. Lee, Hernán A. Navarro, Wei Ma, Lawrence E. Brieaddy, Philip Abraham, M. I. Damaj, and Billy R. Martin
pp 4755–4761Publication Date (Web): September 18, 2002 (Article)
DOI: 10.1021/jm0202268
Design and Evaluation of Affinity Labels of Functionalized Amino Acid Anticonvulsants
Arnaud LeTiran, James P. Stables, and Harold Kohn
pp 4762–4773Publication Date (Web): September 06, 2002 (Article)
DOI: 10.1021/jm020225f
Synthesis and Investigation of Conformationally Restricted Analogues of Lavendustin A as Cytotoxic Inhibitors of Tubulin Polymerization
Fanrong Mu, Debbie J. Lee, Donald E. Pryor, Ernest Hamel, and Mark Cushman
pp 4774–4785Publication Date (Web): September 10, 2002 (Article)
DOI: 10.1021/jm0202270
Biosynthesis of Hyperforin in Hypericum perforatum
Petra Adam, Duilio Arigoni, Adelbert Bacher, and Wolfgang Eisenreich
pp 4786–4793Publication Date (Web): September 17, 2002 (Article)
DOI: 10.1021/jm0209782
Brief Articles
Comparison of 3D Structures and AT1 Binding Properties of Pyrazolidine-3,5-diones and Tetrahydropyridazine-3,6-diones with Parent Antihypertensive Drug Irbesartan
Bertrand Le Bourdonnec, Christine Cauvin, Emmanuelle Meulon, Saïd Yous, Jean-François Goossens, François Durant, Raymond Houssin, and Jean-Pierre Hénichart
pp 4794–4798Publication Date (Web): September 12, 2002 (Brief Article)
DOI: 10.1021/jm010457z
Additions and Corrections
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, Didier M. Lambert:
p 4799Publication Date (Web): September 14, 2002 (Addition/Correction)
DOI: 10.1021/jm020995r
Synthesis and Pharmacology of Benzoxazines as Highly Selective Antagonists at M4 Muscarinic Receptors.
Thomas M. Böhme, Corinne E. Augelli-Szafran, Hussein Hallak, Thomas Pugsley, Kevin Serpa, and Roy D. Schwarz:
p 4800Publication Date (Web): September 13, 2002 (Addition/Correction)
DOI: 10.1021/jm020996j