Table of Contents
May 23, 2002
Volume 45, Issue 11
Pages 2123-2348
Letters
Arylamidrazones as Novel Corticotropin Releasing Factor Receptor Antagonists
Dean M. Wilson, Andreas P. Termin, Long Mao, Michele M. Ramirez-Weinhouse, Valentina Molteni, and Peter D. J. GrootenhuisKeith Miller, Susan Keim, and Gwendolyn Wise
pp 2123–2126Publication Date (Web): April 26, 2002 (Letter)
DOI: 10.1021/jm025512y
Hi-Res PDFDiscovery of N-[2-[2-[[3-Methoxy-4-(5-oxazolyl)phenyl]amino]-5-oxazolyl]phenyl]-N-methyl-4- morpholineacetamide as a Novel and Potent Inhibitor of Inosine Monophosphate Dehydrogenase with Excellent in Vivo Activity
T. G. Murali Dhar, Zhongqi Shen, Junqing Guo, Chunjian Liu, Scott H. Watterson, Henry H. Gu, William J. Pitts, Catherine A. Fleener, Katherine A. Rouleau, N. Z. Sherbina, Kim W. McIntyre, Mark R. Witmer, Jeffrey A. Tredup, Bang-Chi Chen, Rulin Zhao, Mark S. Bednarz, Daniel L. Cheney, John F. MacMaster, Laura M. Miller, Karen K. Berry, Timothy W. Harper, Joel C. Barrish, Diane L. Hollenbaugh, and Edwin J. Iwanowicz
pp 2127–2130Publication Date (Web): April 20, 2002 (Letter)
DOI: 10.1021/jm0105777
Articles
Structure−Activity Relationships at Human and Rat A2B Adenosine Receptors of Xanthine Derivatives Substituted at the 1-, 3-, 7-, and 8-Positions
Soon-Ai Kim, Melissa A. Marshall, Neli Melman, Hak Sung Kim, Christa E. Müller, Joel Linden, and Kenneth A. Jacobson
pp 2131–2138Publication Date (Web): April 25, 2002 (Article)
DOI: 10.1021/jm0104318
5D-QSAR: The Key for Simulating Induced Fit?
Angelo Vedani and Max Dobler
pp 2139–2149Publication Date (Web): April 18, 2002 (Article)
DOI: 10.1021/jm011005p
Rational Design and Evaluation of New Lead Compound Structures for Selective βARK1 Inhibitors
Minoru Iino, Taketoshi Furugori, Tomohiro Mori, Sachiko Moriyama, Akiko Fukuzawa, and Toshiro Shibano
pp 2150–2159Publication Date (Web): April 23, 2002 (Article)
DOI: 10.1021/jm010093a
Nonpeptide Bradykinin B2 Receptor Antagonists: Conversion of Rodent-Selective Bradyzide Analogues into Potent, Orally-Active Human Bradykinin B2 Receptor Antagonists1
Edward K. Dziadulewicz, Timothy J. Ritchie, Allan Hallett, Christopher R. Snell, John W. Davies, Roger Wrigglesworth, Andrew R. Dunstan, Graham C. Bloomfield, Gillian S. Drake, Peter McIntyre, Michael C. Brown, Gillian M. Burgess, Wai Lee, Clare Davis, Mohammed Yaqoob, Steve B. Phagoo, Elsa Phillips, Martin N. Perkins, Elizabeth A. Campbell, Andrew J. Davis, and Humphrey P. Rang
pp 2160–2172Publication Date (Web): April 24, 2002 (Article)
DOI: 10.1021/jm0111088
An Algorithm-Directed Two-Component Library Synthesized Via Solid-Phase Methodology Yielding Potent and Orally Bioavailable p38 MAP Kinase Inhibitors
Jeffrey M. McKenna, Frank Halley, John E. Souness, Iain M. McLay, Stephen D. Pickett, Alan J. Collis, Kenneth Page, and Imtiaz Ahmed
pp 2173–2184Publication Date (Web): April 27, 2002 (Article)
DOI: 10.1021/jm011132l
Inhibition of Geranylgeranyl Diphosphate Synthase by Bisphosphonates and Diphosphates: A Potential Route to New Bone Antiresorption and Antiparasitic Agents
Christina M. Szabo, Yoshihiro Matsumura, Sayaka Fukura, Michael B. Martin, John M. Sanders, Suraj Sengupta, John A. Cieslak, Timothy C. Loftus, Christopher R. Lea, Hyung-Jae Lee, Ali Koohang, Robert M. Coates, Hiroshi Sagami, and Eric Oldfield
pp 2185–2196Publication Date (Web): April 20, 2002 (Article)
DOI: 10.1021/jm010412y
2a-[4-(Tetrahydropyridoindol-2-yl)butyl]tetrahydrobenzindole Derivatives: New Selective Antagonists of the 5-Hydroxytryptamine7 Receptor
Chika Kikuchi, Takashi Ando, Takashi Watanabe, Hiroshi Nagaso, Masayo Okuno, Toyokazu Hiranuma, and Masao Koyama
pp 2197–2206Publication Date (Web): May 01, 2002 (Article)
DOI: 10.1021/jm0104264
Structural Studies of the Resistance of Influenza Virus Neuramindase to Inhibitors
Brian J. Smith, Jennifer L. McKimm-Breshkin, Mandy McDonald, Ross T. Fernley, Joseph N. Varghese, and Peter M. Colman
pp 2207–2212Publication Date (Web): April 30, 2002 (Article)
DOI: 10.1021/jm010528u
Molecular Docking and High-Throughput Screening for Novel Inhibitors of Protein Tyrosine Phosphatase-1B
Thompson N. Doman, Susan L. McGovern, Bryan J. Witherbee, Thomas P. Kasten, Ravi Kurumbail, William C. Stallings, Daniel T. Connolly, and Brian K. Shoichet
pp 2213–2221Publication Date (Web): April 20, 2002 (Article)
DOI: 10.1021/jm010548w
Mode of Action of 4-Hydroxyphenylpyruvate Dioxygenase Inhibition by Triketone-type Inhibitors
Chung-Shieh Wu, Jian-Lin Huang, Yang-Sheng Sun, and Ding-Yah Yang
pp 2222–2228Publication Date (Web): April 27, 2002 (Article)
DOI: 10.1021/jm010568y
2-(Anilinomethyl)imidazolines as α1 Adrenergic Receptor Agonists: the Discovery of α1a Subtype Selective 2‘-Alkylsulfonyl-Substituted Analogues
Stephen J. Hodson, Michael J. Bishop, Jason D. Speake, Frank Navas, III, Deanna T. Garrison, Eric C. Bigham, David L. Saussy, Jr., James A. Liacos, Paul E. Irving, M. Jeffrey Gobel, and Bryan W. Sherman
pp 2229–2239Publication Date (Web): April 26, 2002 (Article)
DOI: 10.1021/jm000542r
Radiolabeled Amino Acids for Tumor Imaging with PET: Radiosynthesis and Biological Evaluation of 2-Amino-3-[18F]fluoro-2-methylpropanoic Acid and 3-[18F]Fluoro-2-methyl-2-(methylamino)propanoic Acid
Jonathan McConathy, Laurent Martarello, Eugene J. Malveaux, Vernon M. Camp, Nicholas E. Simpson, Chiab P. Simpson, Geoffrey D. Bowers, Jeffrey J. Olson, and Mark M. Goodman
pp 2240–2249Publication Date (Web): April 26, 2002 (Article)
DOI: 10.1021/jm010241x
Synthesis of syn- and anti-1-Amino-3-[18F]fluoromethyl-cyclobutane-1-carboxylic Acid (FMACBC), Potential PET Ligands for Tumor Detection
Laurent Martarello, Jonathan McConathy, Vernon M. Camp, Eugene J. Malveaux, Nicholas E. Simpson, Chiab P. Simpson, Jeffrey J. Olson, Geoffrey D. Bowers, and Mark M. Goodman
pp 2250–2259Publication Date (Web): April 26, 2002 (Article)
DOI: 10.1021/jm010242p
Synthesis and in Vitro Pharmacology of Substituted Quinoline-2,4-dicarboxylic Acids as Inhibitors of Vesicular Glutamate Transport
Christina N. Carrigan, Richard D. Bartlett, C. Sean Esslinger, Kimberly A. Cybulski, Pakamas Tongcharoensirikul, Richard J. Bridges, and Charles M. Thompson
pp 2260–2276Publication Date (Web): April 30, 2002 (Article)
DOI: 10.1021/jm010261z
Homodimeric Tacrine Congeners as Acetylcholinesterase Inhibitors
Ming-Kuan Hu, Li-Ju Wu, George Hsiao, and Mao-Hsiung Yen
pp 2277–2282Publication Date (Web): April 26, 2002 (Article)
DOI: 10.1021/jm010308g
Acyl-Protected Hydroxylamines as Spin Label Generators for EPR Brain Imaging
Alexander T. Yordanov, Ken-ichi Yamada, Murali C. Krishna, Angelo Russo, John Yoo, Sean English, James B. Mitchell, and Martin W. Brechbiel
pp 2283–2288Publication Date (Web): May 01, 2002 (Article)
DOI: 10.1021/jm0105169
β-Aryl-Succinic Acid Hydroxamates as Dual Inhibitors of Matrix Metalloproteinases and Tumor Necrosis Factor Alpha Converting Enzyme
Georg Kottirsch, Guido Koch, Roland Feifel, and Ulf Neumann
pp 2289–2293Publication Date (Web): April 27, 2002 (Article)
DOI: 10.1021/jm0110993
Antitumor Agents. 213. Modeling of Epipodophyllotoxin Derivatives Using Variable Selection k Nearest Neighbor QSAR Method
Zhiyan Xiao, Yun-De Xiao, Jun Feng, Alexander Golbraikh, Alexander Tropsha, and Kuo-Hsiung Lee
pp 2294–2309Publication Date (Web): April 24, 2002 (Article)
DOI: 10.1021/jm0105427
Stabilization of the Helical Structure of Y2-Selective Analogues of Neuropeptide Y by Lactam Bridges
Shenggen Yao, Margaret A. Smith-White, Erica K. Potter, and Raymond S. Norton
pp 2310–2318Publication Date (Web): April 24, 2002 (Article)
DOI: 10.1021/jm010543z
Synthesis, Receptor Potency, and Selectivity of Halogenated Diphenylpiperidines as Serotonin 5-HT2A Ligands for PET or SPECT Brain Imaging
Xing Fu, Ping-Zhong Tan, Nora S. Kula, Ross Baldessarini, Gilles Tamagnan, Robert B. Innis, and Ronald M. Baldwin
pp 2319–2324Publication Date (Web): April 30, 2002 (Article)
DOI: 10.1021/jm0200411
Synthesis, Structural Evaluation, and Estrogen Receptor Interaction of 2,3-Diarylpiperazines
Ronald Gust, Roland Keilitz, and Kathrin Schmidt
pp 2325–2337Publication Date (Web): April 25, 2002 (Article)
DOI: 10.1021/jm0208368
Brief Articles
Osteoadsorptive Bisphosphonate Derivatives of Fluoroquinolone Antibacterials
Pál Herczegh, Thomas B. Buxton, James C. McPherson III, Árpád Kovács-Kulyassa, Phyllis D. Brewer, Ferenc Sztaricskai, Gary G. Stroebel, Kent M. Plowman, Dan Farcasiu, and John F. Hartmann
pp 2338–2341Publication Date (Web): April 09, 2002 (Brief Article)
DOI: 10.1021/jm0105326
Pyrazolopyrimidine-2,4-dione Sulfonamides: Novel and Selective Calcitonin Inducers
Adam M. Gilbert, Stephen Caltabiano, Frank E. Koehn, Zhen-jia Chen, Gerardo D. Francisco, John W. Ellingboe, Yogendra Kharode, AnnaMarie Mangine, Rita Francis, Mark TrailSmith, and David Gralnick
pp 2342–2345Publication Date (Web): April 26, 2002 (Brief Article)
DOI: 10.1021/jm010554s
Book Reviews
Textbook of Biochemistry with Clinical Correlations. 5th Edition Edited by Thomas M. Devlin. Wiley-Liss, New York. 2002. xxiv + 1216 pp. 22 × 29 cm. ISBN 0-471-41136-1. $99.94.
D. Eric Walters
p 2346Publication Date (Web): April 26, 2002 (Book Review)
DOI: 10.1021/jm020135a
Additions and Corrections
Synthesis and Evaluation of 3-Trifluoromethyl-7-substituted-1,2,3,4-tetrahydroisoquinolines as Selective Inhibitors of Phenylethanolamine N-Methyltransferase versus the α2-Adrenoceptor.
Gary L. Grunewald, Timothy M. Caldwell, Qifang Li, and Kevin R. Criscione:
p 2347Publication Date (Web): April 20, 2002 (Addition/Correction)
DOI: 10.1021/jm0201161
Synthesis and Biochemical Evaluation of 3-Fluoromethyl-1,2,3,4-tetrahydroisoquinolines as Selective Inhibitors of Phenylethanolamine N-Methyltransferase versus the α2-Adrenoceptor.
Gary L. Grunewald, Timothy M. Caldwell, Qifang Li, Meri Slavica, Kevin R. Criscione, Ronald T. Borchardt, and Wen Wang:
p 2347Publication Date (Web): April 20, 2002 (Addition/Correction)
DOI: 10.1021/jm020117t
Design and Synthesis of Matrix Metalloproteinase Inhibitors Guided by Molecular Modeling. Picking the S1 Pocket Using Conformationally Constrained Inhibitors.
Stephen Hanessian, D. Bruce MacKay, and Nicolas Moitessier:
p 2348Publication Date (Web): April 26, 2002 (Addition/Correction)
DOI: 10.1021/jm020097v
Synthesis and Evaluation of 4-Fluoro-8-substituted-2,3,4,5-tetrahydro-1H-2-benzazapines as Selective Inhibitors of Phenylethanolamine N-Methyltransferase versus the α2-Adrenoceptor.
Gary L. Grunewald, Timothy M. Caldwell, Qifang Li, and Kevin R. Criscione:
p 2348Publication Date (Web): April 20, 2002 (Addition/Correction)
DOI: 10.1021/jm020118l