Table of Contents
July 4, 2002
Volume 45, Issue 14
Pages 2887-3160
About the Cover: Model of the histone deacetylase inhibitor, 3-(4-benzoyl-1-methyl-1H-2-pyrrole)-N-hydroxy-
Letters
Naphthalene Dicarboxaldehyde as an Electrophilic Fluorogenic Moiety for Affinity Labeling: Application to Opioid Receptor Affinity Labels with Greatly Improved Fluorogenic Properties
Christopher R. McCurdy, Bertrand Le Bourdonnec, Thomas G. Metzger, Rachid El Kouhen, Yan Zhang, Ping Y. Law, and Philip S. Portoghese
pp 2887–2890Publication Date (Web): June 12, 2002 (Letter)
DOI: 10.1021/jm015586u
Hi-Res PDFNovel 2-Oxoamide Inhibitors of Human Group IVA Phospholipase A2
George Kokotos, Stavroula Kotsovolou, David A. Six, Violetta Constantinou-Kokotou, Christopher C. Beltzner, and Edward A. Dennis
pp 2891–2893Publication Date (Web): June 7, 2002 (Letter)
DOI: 10.1021/jm025538p
Articles
An Investigation of Bone Resorption and Dictyostelium discoideum Growth Inhibition by Bisphosphonate Drugs
Christina M. Szabo, Michael B. Martin, and Eric Oldfield
pp 2894–2903Publication Date (Web): June 08, 2002 (Article)
DOI: 10.1021/jm010279+
Full Text HTMLActivity of Bisphosphonates against Trypanosoma brucei rhodesiense
Michael B. Martin, John M. Sanders, Howard Kendrick, Kate de Luca-Fradley, Jared C. Lewis, Joshua S. Grimley, Erin M. Van Brussel, Jeffrey R. Olsen, Gary A. Meints, Agnieszka Burzynska, Pawel Kafarski, Simon L. Croft, and Eric Oldfield
pp 2904–2914Publication Date (Web): June 5, 2002 (Article)
DOI: 10.1021/jm0102809
Principles Governing the Binding of a Class of Non-Peptidic Inhibitors to the SH2 Domain of src Studied by X-ray Analysis
Gudrun Lange, Dominique Lesuisse, Pierre Deprez, Bernard Schoot, Petra Loenze, Didier Bénard, Jean-Pierre Marquette, Pierre Broto, Edoardo Sarubbi, and Eliane Mandine
pp 2915–2922Publication Date (Web): June 4, 2002 (Article)
DOI: 10.1021/jm0110800
Structural Requirements for Inhibition of the Neuronal Nitric Oxide Synthase (NOS-I): 3D-QSAR Analysis of 4-Oxo- and 4-Amino-Pteridine-Based Inhibitors
Hans Matter, Peter Kotsonis, Otmar Klingler, Hartmut Strobel, Lothar G. Fröhlich, Armin Frey, Wolfgang Pfleiderer, and Harald H. H. W. Schmidt
pp 2923–2941Publication Date (Web): May 25, 2002 (Article)
DOI: 10.1021/jm020074g
4,5-Diphenyltriazol-3-ones: Openers of Large-Conductance Ca2+-Activated Potassium (Maxi-K) Channels
Jeffrey L. Romine, Scott W. Martin, Valentin K. Gribkoff, Christopher G. Boissard, Steven I. Dworetzky, Joanne Natale, Yi Li, Qi Gao, Nicholas A. Meanwell, and John E. Starrett, Jr.
pp 2942–2952Publication Date (Web): May 24, 2002 (Article)
DOI: 10.1021/jm010569q
New p-Methylsulfonamido Phenylethylamine Analogues as Class III Antiarrhythmic Agents: Design, Synthesis, Biological Assay, and 3D-QSAR Analysis
Hong Liu, Ming Ji, Xiaomin Luo, Jianhua Shen, Xiaoqin Huang, Weiyi Hua, Hualiang Jiang, and Kaixian Chen
pp 2953–2969Publication Date (Web): June 12, 2002 (Article)
DOI: 10.1021/jm010574u
Prediction of Activity for Nonnucleoside Inhibitors with HIV-1 Reverse Transcriptase Based on Monte Carlo Simulations
Robert C. Rizzo, Marina Udier-Blagović, De-Ping Wang, Edward K. Watkins, Marilyn B. Kroeger Smith, Richard H. Smith, Jr., Julian Tirado-Rives, and William L. Jorgensen
pp 2970–2987Publication Date (Web): June 8, 2002 (Article)
DOI: 10.1021/jm010580q
Identification of Potent and Novel α4β1 Antagonists Using in Silico Screening
Juswinder Singh, Herman van Vlijmen, Yusheng Liao, Wen-Cherng Lee, Mark Cornebise, Mary Harris, I-hsiang Shu, Alan Gill, Julio H. Cuervo, William M. Abraham, and Steven P. Adams
pp 2988–2993Publication Date (Web): June 11, 2002 (Article)
DOI: 10.1021/jm020054e
Pyrazole Urea-Based Inhibitors of p38 MAP Kinase: From Lead Compound to Clinical Candidate
John Regan, Steffen Breitfelder, Pier Cirillo, Thomas Gilmore, Anne G. Graham, Eugene Hickey, Bernhard Klaus, Jeffrey Madwed, Monica Moriak, Neil Moss, Chris Pargellis, Sue Pav, Alfred Proto, Alan Swinamer, Liang Tong, and Carol Torcellini
pp 2994–3008Publication Date (Web): May 25, 2002 (Article)
DOI: 10.1021/jm020057r
Novel, Non-acylguanidine-type Na+/H+ Exchanger Inhibitors: Synthesis and Pharmacology of 5-Tetrahydroquinolinylidene Aminoguanidine Derivatives
Shoji Fukumoto, Eiko Imamiya, Keiji Kusumoto, Shuji Fujiwara, Toshifumi Watanabe, and Mitsuru Shiraishi
pp 3009–3021Publication Date (Web): May 29, 2002 (Article)
DOI: 10.1021/jm0104567
Further Characterization of Structural Requirements for Ligands at the Dopamine D2 and D3 Receptor: Exploring the Thiophene Moiety
Durk Dijkstra, Nienke Rodenhuis, Erik S. Vermeulen, Thomas A. Pugsley, Lawrence D. Wise, and Håkan V. Wikström
pp 3022–3031Publication Date (Web): June 5, 2002 (Article)
DOI: 10.1021/jm001015a
Highly Antibacterial Active Aminoacyl Penicillin Conjugates with Acylated Bis-Catecholate Siderophores Based on Secondary Diamino Acids and Related Compounds
Lothar Heinisch, Steffen Wittmann, Thomas Stoiber, Albrecht Berg, Dorothe Ankel-Fuchs, and Ute Möllmann
pp 3032–3040Publication Date (Web): June 6, 2002 (Article)
DOI: 10.1021/jm010546b
Synthesis and Biological Evaluation at Nicotinic Acetylcholine Receptors of N-Arylalkyl- and N-Aryl-7-Azabicyclo[2.2.1]heptanes
Jie Cheng, Chunming Zhang, Edwin D. Stevens, Sari Izenwasser, Dean Wade, Shaoyi Chen, Dennis Paul, and Mark L. Trudell
pp 3041–3047Publication Date (Web): June 4, 2002 (Article)
DOI: 10.1021/jm0103561
Modification of the Structure of a Metallopeptide: Synthesis and Biological Evaluation of 111In-Labeled DOTA-Conjugated Rhenium-Cyclized α-MSH Analogues
Zhen Cheng, Jianqing Chen, Yubin Miao, Nellie K. Owen, Thomas P. Quinn, and Silvia S. Jurisson
pp 3048–3056Publication Date (Web): June 4, 2002 (Article)
DOI: 10.1021/jm010408m
Potent and Selective Inhibitors of Platelet-Derived Growth Factor Receptor Phosphorylation. 1. Synthesis, Structure−Activity Relationship, and Biological Effects of a New Class of Quinazoline Derivatives
Kenji Matsuno, Michio Ichimura, Takao Nakajima, Keiko Tahara, Shigeki Fujiwara, Hiroshi Kase, Junko Ushiki, Neill A. Giese, Anjali Pandey, Robert M. Scarborough, Nathalie A. Lokker, Jin-Chen Yu, Junko Irie, Eiji Tsukuda, Shin-ichi Ide, Shoji Oda, and Yuji Nomoto
pp 3057–3066Publication Date (Web): June 11, 2002 (Article)
DOI: 10.1021/jm010428o
Lepadins D−F: Antiplasmodial and Antitrypanosomal Decahydroquinoline Derivatives from the Tropical Marine Tunicate Didemnum sp.
Anthony D. Wright, Eva Goclik, Gabriele M. König, and Ronald Kaminsky
pp 3067–3072Publication Date (Web): June 4, 2002 (Article)
DOI: 10.1021/jm0110892
Structure−Activity Relationships of the Melanocortin Tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 at the Mouse Melanocortin Receptors: Part 2 Modifications at the Phe Position
Jerry Ryan Holder, Rayna M. Bauzo, Zhimin Xiang, and Carrie Haskell-Luevano
pp 3073–3081Publication Date (Web): June 4, 2002 (Article)
DOI: 10.1021/jm010524p
Data Analysis of High-Throughput Screening Results: Application of Multidomain Clustering to the NCI Anti-HIV Data Set
Susan Y. Tamura, Patricia A. Bacha, Heather S. Gruver, and Ruth F. Nutt
pp 3082–3093Publication Date (Web): June 7, 2002 (Article)
DOI: 10.1021/jm010535i
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
pp 3094–3102Publication Date (Web): June 4, 2002 (Article)
DOI: 10.1021/jm011116o
Correlations between Cytotoxicity and Topography of Some 2-Arylidenebenzocycloalkanones Determined by X-ray Crystallography
Jonathan R. Dimmock, Gordon A. Zello, Eliud O. Oloo, J. Wilson Quail, Heinz-Bernhard Kraatz, Pál Perjési, Ferenc Aradi, Krisztina Takács-Novák, Theresa M. Allen, Cheryl L. Santos, Jan Balzarini, Erik De Clercq, and James P. Stables
pp 3103–3111Publication Date (Web): June 4, 2002 (Article)
DOI: 10.1021/jm010559p
Potent, Novel in Vitro Inhibitors of the Pseudomonas aeruginosa Deacetylase LpxC
Toni Kline, Niels H. Andersen, Eric A. Harwood, Jason Bowman, Andre Malanda, Stephanie Endsley, Alice L. Erwin, Michael Doyle, Susan Fong, Alex L. Harris, Brian Mendelsohn, Khisimuzi Mdluli, Christian R. H. Raetz, C. Kendall Stover, Pamela R. Witte, Asha Yabannavar, and Shuguang Zhu
pp 3112–3129Publication Date (Web): June 7, 2002 (Article)
DOI: 10.1021/jm010579r
II. Synthesis and Biological Evaluation of Some Bioisosteres and Congeners of the Antitumor Agent, 2-{4-[(7-Chloro-2-quinoxalinyl)oxy]phenoxy}propionic Acid (XK469)
Stuart T. Hazeldine, Lisa Polin, Juiwanna Kushner, Kathryn White, Nicole M. Bouregeois, Brianna Crantz, Eduardo Palomino, Thomas H. Corbett, and Jerome P. Horwitz
pp 3130–3137Publication Date (Web): June 12, 2002 (Article)
DOI: 10.1021/jm0200097
2-Amino-6-arylthio-9-[2-(phosphonomethoxy)ethyl]purine Bis(2,2,2-trifluoroethyl) Esters as Novel HBV-Specific Antiviral Reagents
Kouichi Sekiya, Hideaki Takashima, Naoko Ueda, Naohiro Kamiya, Satoshi Yuasa, Yoshiyuki Fujimura, and Masaru Ubasawa
pp 3138–3142Publication Date (Web): June 4, 2002 (Article)
DOI: 10.1021/jm020036x
Synthesis, SAR, and Biological Evaluation of Oximino-Piperidino-Piperidine Amides. 1. Orally Bioavailable CCR5 Receptor Antagonists with Potent Anti-HIV Activity
Anandan Palani, Sherry Shapiro, Hubert Josien, Thomas Bara, John W. Clader, William J. Greenlee, Kathleen Cox, Julie M. Strizki, and Bahige M. Baroudy
pp 3143–3160Publication Date (Web): June 12, 2002 (Article)
DOI: 10.1021/jm0200815