Table of Contents
August 15, 2002
Volume 45, Issue 17
Pages 3569-3812
About the Cover: Model of the histone deacetylase inhibitor, 3-(4-benzoyl-1-methyl-1H-2-pyrrole)-N-hydroxy-
Letters
6α-Ethyl-Chenodeoxycholic Acid (6-ECDCA), a Potent and Selective FXR Agonist Endowed with Anticholestatic Activity
Roberto Pellicciari, Stefano Fiorucci, Emidio Camaioni, Carlo Clerici, Gabriele Costantino, Patrick R. Maloney, Antonio Morelli, Derek J. Parks, and Timothy M. Willson
pp 3569–3572Publication Date (Web): July 20, 2002 (Letter)
DOI: 10.1021/jm025529g
Hi-Res PDFIdentification of a Pharmacophore for Thrombopoietic Activity of Small, Non-Peptidyl Molecules. 1. Discovery and Optimization of Salicylaldehyde Thiosemicarbazone Thrombopoietin Mimics
Kevin J. Duffy, Anthony N. Shaw, Evelyne Delorme, Susan B. Dillon, Connie Erickson-Miller, Leslie Giampa, Yifang Huang, Richard M. Keenan, Peter Lamb, Nannan Liu, Stephen G. Miller, Alan T. Price, Jon Rosen, Heather Smith, Kenneth J. Wiggall, Lihua Zhang, and Juan I. Luengo
pp 3573–3575Publication Date (Web): July 19, 2002 (Letter)
DOI: 10.1021/jm025535c
Identification of a Pharmacophore for Thrombopoietic Activity of Small, Non-Peptidyl Molecules. 2. Rational Design of Naphtho[1,2-d]imidazole Thrombopoietin Mimics
Kevin J. Duffy, Alan T. Price, Evelyne Delorme, Susan B. Dillon, Celine Duquenne, Connie Erickson-Miller, Leslie Giampa, Yifang Huang, Richard M. Keenan, Peter Lamb, Nannan Liu, Stephen G. Miller, Jon Rosen, Anthony N. Shaw, Heather Smith, Kenneth J. Wiggall, Lihua Zhang, and Juan I. Luengo
pp 3576–3578Publication Date (Web): July 19, 2002 (Letter)
DOI: 10.1021/jm0255365
Synthesis, Biological Properties, and Molecular Modeling Investigation of the First Potent, Selective, and Water-Soluble Human A3 Adenosine Receptor Antagonist
Anna Maconi, Giorgia Pastorin, Tatiana Da Ros, Giampiero Spalluto, Zhan-guo Gao, Kenneth A. Jacobson, Pier Giovanni Baraldi, Barbara Cacciari, Katia Varani, Stefano Moro, and Pier Andrea Borea
pp 3579–3582Publication Date (Web): July 16, 2002 (Letter)
DOI: 10.1021/jm020974x
Articles
Nonaromatic Sulfonamide Group as an Ideal Anchor for Potent Human Carbonic Anhydrase Inhibitors: Role of Hydrogen-Bonding Networks in Ligand Binding and Drug Design
Francesco Abbate, Claudiu T. Supuran, Andrea Scozzafava, Pierluigi Orioli, Milton T. Stubbs, and Gerhard Klebe
pp 3583–3587Publication Date (Web): July 12, 2002 (Article)
DOI: 10.1021/jm011131t
Successful Virtual Screening for Novel Inhibitors of Human Carbonic Anhydrase: Strategy and Experimental Confirmation
Sven Grüneberg, Milton T. Stubbs, and Gerhard Klebe
pp 3588–3602Publication Date (Web): July 12, 2002 (Article)
DOI: 10.1021/jm011112j
α1-Adrenoceptor Antagonists. 4.1 Pharmacophore-Based Design, Synthesis, and Biological Evaluation of New Imidazo-, Benzimidazo-, and Indoloarylpiperazine Derivatives
Laura Betti, Maurizio Botta, Federico Corelli, Monia Floridi, Gino Giannaccini, Laura Maccari, Fabrizio Manetti, Giovannella Strappaghetti, Andrea Tafi, and Stefano Corsano
pp 3603–3611Publication Date (Web): July 23, 2002 (Article)
DOI: 10.1021/jm011077g
Arginine-Rich Molecular Transporters for Drug Delivery: Role of Backbone Spacing in Cellular Uptake
Jonathan B. Rothbard, Erik Kreider, Christopher L. VanDeusen, Lee Wright, Bryan L. Wylie, and Paul A. Wender
pp 3612–3618Publication Date (Web): July 11, 2002 (Article)
DOI: 10.1021/jm0105676
(2S,1‘S,2‘S,3‘R)-2-(2‘-Carboxy-3‘-methylcyclopropyl) Glycine Is a Potent and Selective Metabotropic Group 2 Receptor Agonist with Anxiolytic Properties
Iván Collado, Concepción Pedregal, Angel Mazón, Juan Félix Espinosa, Jaime Blanco-Urgoiti, Darryle D. Schoepp, Rebecca A. Wright, Bryan G. Johnson, and Ann E. Kingston
pp 3619–3629Publication Date (Web): July 17, 2002 (Article)
DOI: 10.1021/jm0110486
Design, Synthesis, and Biological Activity of Hybrid Compounds between Uramustine and DNA Minor Groove Binder Distamycin A
Pier Giovanni Baraldi, Romeo Romagnoli, Antonio Entrena Guadix, Maria Josè Pineda de las Infantas, Miguel Angel Gallo, Antonio Espinosa, Alberto Martinez, John P. Bingham, and John A. Hartley
pp 3630–3638Publication Date (Web): July 13, 2002 (Article)
DOI: 10.1021/jm011113b
Design, Synthesis, and Structure−Activity Relationship of 6-Alkynylpyrimidines as Potent Adenosine Kinase Inhibitors
Arthur Gomtsyan, Stanley Didomenico, Chih-Hung Lee, Mark A. Matulenko, Ki Kim, Elizabeth A. Kowaluk, Carol T. Wismer, Joe Mikusa, Haixia Yu, Kathy Kohlhaas, Michael F. Jarvis, and Shripad S. Bhagwat
pp 3639–3648Publication Date (Web): July 09, 2002 (Article)
DOI: 10.1021/jm020049a
Conformational Memories and the Endocannabinoid Binding Site at the Cannabinoid CB1 Receptor
Judy Barnett-Norris, Dow P. Hurst, Diane L. Lynch, Frank Guarnieri, Alex Makriyannis, and Patricia H. Reggio
pp 3649–3659Publication Date (Web): July 13, 2002 (Article)
DOI: 10.1021/jm0200761
(+)-Dinapsoline: An Efficient Synthesis and Pharmacological Profile of a Novel Dopamine Agonist
Sing-Yuen Sit, Kai Xie, Swanee Jacutin-Porte, Matthew T. Taber, Amit G. Gulwadi, Carolyn D. Korpinen, Kevin D. Burris, Thaddeus F. Molski, Elaine Ryan, Cen Xu, Henry Wong, Juliang Zhu, Subramaniam Krishnananthan, Qi Gao, Todd Verdoorn, and Graham Johnson
pp 3660–3668Publication Date (Web): July 20, 2002 (Article)
DOI: 10.1021/jm0101545
Dicaffeoyltartaric Acid Analogues Inhibit Human Immunodeficiency Virus Type 1 (HIV-1) Integrase and HIV-1 Replication at Nontoxic Concentrations
Ryan A. Reinke, Peter J. King, Joseph G. Victoria, Brenda R. McDougall, Guoxiang Ma, Yingqun Mao, Manfred G. Reinecke, and W. Edward Robinson, Jr.
pp 3669–3683Publication Date (Web): July 18, 2002 (Article)
DOI: 10.1021/jm010359d
Anticholinesterase Activity of Compounds Related to Geneserine Tautomers. N-Oxides and 1,2-Oxazines
Qian-sheng Yu, Xiaoxiang Zhu, Harold W. Holloway, Noel F. Whittaker, Arnold Brossi, and Nigel H. Greig
pp 3684–3691Publication Date (Web): July 16, 2002 (Article)
DOI: 10.1021/jm010491d
The Design and Synthesis of Water-Soluble Analogues of CB30865, a Quinazolin-4-one-Based Antitumor Agent
V. Bavetsias, L. A. Skelton, F. Yafai, F. Mitchell, S. C. Wilson, B. Allan, and A. L. Jackman
pp 3692–3702Publication Date (Web): July 13, 2002 (Article)
DOI: 10.1021/jm011081s
1,2,4-Triazolo[5,1-i]purine Derivatives as Highly Potent and Selective Human Adenosine A3 Receptor Ligands
Takashi Okamura, Yasuhisa Kurogi, Hiroshi Nishikawa, Kinji Hashimoto, Hiroshi Fujiwara, and Yoshimitsu Nagao
pp 3703–3708Publication Date (Web): July 16, 2002 (Article)
DOI: 10.1021/jm010570p
Oxygenated Metabolites of Anandamide and 2-Arachidonoylglycerol: Conformational Analysis and Interaction with Cannabinoid Receptors, Membrane Transporter, and Fatty Acid Amide Hydrolase
Mario van der Stelt, J. Albert van Kuik, Monica Bari, Guus van Zadelhoff, Bas R. Leeflang, Gerrit A. Veldink, Alessandro Finazzi-Agrò, Johannes F. G. Vliegenthart, and Mauro Maccarrone
pp 3709–3720Publication Date (Web): July 11, 2002 (Article)
DOI: 10.1021/jm020818q
Highly Potent Geminal Bisphosphonates. From Pamidronate Disodium (Aredia) to Zoledronic Acid (Zometa)
Leo Widler, Knut A. Jaeggi, Markus Glatt, Klaus Müller, Rolf Bachmann, Michael Bisping, Anne-Ruth Born, Reto Cortesi, Gabriela Guiglia, Heidi Jeker, Rémy Klein, Ueli Ramseier, Johann Schmid, Gerard Schreiber, Yves Seltenmeyer, and Jonathan R. Green
pp 3721–3738Publication Date (Web): July 19, 2002 (Article)
DOI: 10.1021/jm020819i
N-Acylvanillamides: Development of an Expeditious Synthesis and Discovery of New Acyl Templates for Powerful Activation of the Vanilloid Receptor
Giovanni Appendino and Alberto MinassiAniello Schiano Morello and Luciano De PetrocellisVincenzo Di Marzo
pp 3739–3745Publication Date (Web): July 09, 2002 (Article)
DOI: 10.1021/jm020844o
Synthesis and Biological Activities of Cyclic Lanthionine Enkephalin Analogues: δ-Opioid Receptor Selective Ligands
Yosup Rew, Shelle Malkmus, Camilla Svensson, Tony L. Yaksh, Nga N. Chung, Peter W. Schiller, Joel A. Cassel, Robert N. DeHaven, and Murray Goodman
pp 3746–3754Publication Date (Web): July 04, 2002 (Article)
DOI: 10.1021/jm020108k
Synthesis and Structure−Activity Relationships of 6,7-Benzomorphan Derivatives as Use-Dependent Sodium Channel Blockers for the Treatment of Stroke
Matthias Grauert, Wolf D. Bechtel, Thomas Weiser, Werner Stransky, Herbert Nar, and Adrian J. Carter
pp 3755–3764Publication Date (Web): July 19, 2002 (Article)
DOI: 10.1021/jm020875j
Synthesis and In Vitro Antitumor Activity of Novel Ring D Analogues of the Marine Pyridoacridine Ascididemin: Structure−Activity Relationship
Evelyne Delfourne, Francis Darro, Philippe Portefaix, Chantal Galaup, Sylvie Bayssade, Anne Bouteillé, Laurent Le Corre, Jean Bastide, Françoise Collignon, Brigitte Lesur, Armand Frydman, and Robert Kiss
pp 3765–3771Publication Date (Web): July 10, 2002 (Article)
DOI: 10.1021/jm0208774
Identification of Orally Active, Potent, and Selective 4-Piperazinylquinazolines as Antagonists of the Platelet-Derived Growth Factor Receptor Tyrosine Kinase Family
Anjali Pandey, Deborah L. Volkots, Joseph M. Seroogy, Jack W. Rose, Jin-Chen Yu, Joseph L. Lambing, Athiwat Hutchaleelaha, Stanley J. Hollenbach, Keith Abe, Neill A. Giese, and Robert M. Scarborough
pp 3772–3793Publication Date (Web): July 23, 2002 (Article)
DOI: 10.1021/jm020143r
Discovery and Structure−Activity Relationship of N-(Ureidoalkyl)-Benzyl-Piperidines As Potent Small Molecule CC Chemokine Receptor-3 (CCR3) Antagonists
George V. De Lucca, Ui T. Kim, Curt Johnson, Brian J. Vargo, Patricia K. Welch, Maryanne Covington, Paul Davies, Kimberly A. Solomon, Robert C. Newton, George L. Trainor, Carl P. Decicco, and Soo S. Ko
pp 3794–3804Publication Date (Web): July 11, 2002 (Article)
DOI: 10.1021/jm0201767
Brief Articles
Characterization of Orally Active Nonpeptide Vasopressin V2 Receptor Agonist. Synthesis and Biological Evaluation of Both the (5R)- and (5S)-Enantioisomers of 2-[1-(2-Chloro-4-pyrrolidin-1-yl-benzoyl)-2,3,4,5-tetrahydro-1H-1-benzazepin- 5-yl]-N-isopropylacetamide
Kazumi Kondo, Keizo Kan, Yoshihisa Tanada, Masahiko Bando, Tomoichi Shinohara, Muneaki Kurimura, Hidenori Ogawa, Shigeki Nakamura, Takahiro Hirano, Yoshitaka Yamamura, Masaru Kido, Toyoki Mori, and Michiaki Tominaga
pp 3805–3808Publication Date (Web): July 16, 2002 (Brief Article)
DOI: 10.1021/jm020133q
Elevation of Ligand Binding to Muscarinic M2 Acetylcholine Receptors by Bis(ammonio)alkane-Type Allosteric Modulators
Alexandra Raasch, Olaf Scharfenstein, Christian Tränkle, Ulrike Holzgrabe, and Klaus Mohr
pp 3809–3812Publication Date (Web): July 11, 2002 (Brief Article)
DOI: 10.1021/jm020871e