Table of Contents
March 14, 2002
Volume 45, Issue 6
Pages 1391-1394
Perspectives
Serine−Threonine Protein Phosphatase Inhibitors: Development of Potential Therapeutic Strategies
Adam McCluskey, Alistair T. R. Sim, and Jennette A. Sakoff
pp 1151–1175Publication Date (Web): February 19, 2002 (Perspective)
DOI: 10.1021/jm010066k
Hi-Res PDF6,7-Dihydro-2-benzothiophen-4(5H)-ones: A Novel Class of GABA-A α5 Receptor Inverse Agonists
Mark S. Chambers, John R. Atack, Frances A. Bromidge, Howard B. Broughton, Susan Cook, Gerard R. Dawson, Sarah C. Hobbs, Karen A. Maubach, Austin J. Reeve, Guy R. Seabrook, Keith Wafford, and Angus M. MacLeod
pp 1176–1179Publication Date (Web): February 12, 2002 (Letter)
DOI: 10.1021/jm010471b
3-(1H-Pyrrol-1-yl)-2-oxazolidinones as Reversible, Highly Potent, and Selective Inhibitors of Monoamine Oxidase Type A
Antonello Mai, Marino Artico, Monica Esposito, Gianluca Sbardella, Silvio Massa, Olivia Befani, Paola Turini, Valentina Giovannini, and Bruno Mondovì
pp 1180–1183Publication Date (Web): February 06, 2002 (Letter)
DOI: 10.1021/jm015578d
Articles
Synthesis and X-ray Studies of Chiral Allosteric Modifiers of Hemoglobin
Amal Mamdouh Youssef, Martin K. Safo, Richmond Danso-Danquah, Gajanan S. Joshi, Jean Kister, Michael C. Marden, and Donald J. Abraham
pp 1184–1195Publication Date (Web): February 13, 2002 (Article)
DOI: 10.1021/jm010358l
Ribose-Modified Nucleosides as Ligands for Adenosine Receptors: Synthesis, Conformational Analysis, and Biological Evaluation of 1‘-C-Methyl Adenosine Analogues
Loredana Cappellacci, Grazia Barboni, Micaela Palmieri, Michela Pasqualini, Mario Grifantini, Barbara Costa, Claudia Martini, and Palmarisa Franchetti
pp 1196–1202Publication Date (Web): February 13, 2002 (Article)
DOI: 10.1021/jm0102755
Synthesis and Biological Evaluation of 2-Substituted 3β-Tolyltropane Derivatives at Dopamine, Serotonin, and Norepinephrine Transporters
Lifen Xu, Sari Izenwasser, Jonathan L. Katz, Theresa Kopajtic, Cheryl Klein-Stevens, Naiju Zhu, Stacey A. Lomenzo, Leyte Winfield, and Mark L. Trudell
pp 1203–1210Publication Date (Web): February 06, 2002 (Article)
DOI: 10.1021/jm010453u
A Comprehensive Study of the Active Site Residues of DT-Diaphorase: Rational Design of Benzimidazolediones as DT-Diaphorase Substrates
Ali Suleman and Edward B. Skibo
pp 1211–1220Publication Date (Web): February 09, 2002 (Article)
DOI: 10.1021/jm0104365
PRO_SELECT: Combining Structure-Based Drug Design and Array-Based Chemistry for Rapid Lead Discovery. 2. The Development of a Series of Highly Potent and Selective Factor Xa Inhibitors
John W. Liebeschuetz, Stuart D. Jones, Phillip J. Morgan, Chris W. Murray, Andrew D. Rimmer, Jonathan M. E. Roscoe, Bohdan Waszkowycz, Pauline M. Welsh, William A. Wylie, Stephen C. Young, Harry Martin, Jacqui Mahler, Leo Brady, and Kay Wilkinson
pp 1221–1232Publication Date (Web): February 16, 2002 (Article)
DOI: 10.1021/jm010944e
Designing Small, Nonsugar Activators of Antithrombin Using Hydropathic Interaction Analyses
Gunnar T. Gunnarsson and Umesh R. Desai
pp 1233–1243Publication Date (Web): February 13, 2002 (Article)
DOI: 10.1021/jm020012q
Development of 2,4-Diaminopyrimidines as Antimalarials Based on Inhibition of the S108N and C59R+S108N Mutants of Dihydrofolate Reductase from Pyrimethamine-Resistant Plasmodium falciparum
Bongkoch Tarnchompoo, Chawanee Sirichaiwat, Worrapong Phupong, Chakapong Intaraudom, Worachart Sirawaraporn, Sumalee Kamchonwongpaisan, Jarunee Vanichtanankul, Yodhathai Thebtaranonth, and Yongyuth Yuthavong
pp 1244–1252Publication Date (Web): February 09, 2002 (Article)
DOI: 10.1021/jm010131q
Substituted Diphenyl Sulfides as Selective Serotonin Transporter Ligands: Synthesis and In Vitro Evaluation
Patrick Emond, Johnny Vercouillie, Robert Innis, Sylvie Chalon, Sylvie Mavel, Yves Frangin, Christer Halldin, Jean-Claude Besnard, and Denis Guilloteau
pp 1253–1258Publication Date (Web): February 09, 2002 (Article)
DOI: 10.1021/jm010939a
Substituted Pentacyclic Carbazolones as Novel Muscarinic Allosteric Agents: Synthesis and Structure−Affinity and Cooperativity Relationships
Parviz Gharagozloo, Sebastian Lazareno, Masao Miyauchi, Angela Popham, and Nigel J. M. Birdsall
pp 1259–1274Publication Date (Web): February 19, 2002 (Article)
DOI: 10.1021/jm010946z
Synthesis of New Covalently Bound κ-Carrageenan−AZT Conjugates with Improved Anti-HIV Activities
Patrick Vlieghe, Thierry Clerc, Christophe Pannecouque, Myriam Witvrouw, Erik De Clercq, Jean-Pierre Salles, and Jean-Louis Kraus
pp 1275–1283Publication Date (Web): February 16, 2002 (Article)
DOI: 10.1021/jm010969d
Carbocyclic Dinucleoside Polyphosphonates: Interaction with HIV Reverse Transcriptase and Antiviral Activity
Anastasya L. Khandazhinskaya, Elena A. Shirokova, Yurii S. Skoblov, Lyubov S. Victorova, Ludmila Ye. Goryunova, Robert S. Beabealashvilli, Tatyana R. Pronyaeva, Nina V. Fedyuk, Vladimir V. Zolin, Andrey G. Pokrovsky, and Marina K. Kukhanova
pp 1284–1291Publication Date (Web): February 19, 2002 (Article)
DOI: 10.1021/jm011011l
First Non-ATP Competitive Glycogen Synthase Kinase 3 β (GSK-3β) Inhibitors: Thiadiazolidinones (TDZD) as Potential Drugs for the Treatment of Alzheimer's Disease
Ana Martinez, Mercedes Alonso, Ana Castro, Concepción Pérez, and Francisco J. Moreno
pp 1292–1299Publication Date (Web): February 13, 2002 (Article)
DOI: 10.1021/jm011020u
Novel 4-Anilinoquinazolines with C-7 Basic Side Chains: Design and Structure Activity Relationship of a Series of Potent, Orally Active, VEGF Receptor Tyrosine Kinase Inhibitors
Laurent F. Hennequin, Elaine S. E. Stokes, Andrew P. Thomas, Craig Johnstone, Patrick A. Plé, Donald J. Ogilvie, Michael Dukes, Stephen R. Wedge, Jane Kendrew, and Jon O. Curwen
pp 1300–1312Publication Date (Web): February 19, 2002 (Article)
DOI: 10.1021/jm011022e
Structure−Activity Relationships of 2‘-Fluoro-2‘,3‘-unsaturated d-Nucleosides as Anti-HIV-1 Agents
Kyeong Lee, Yongseok Choi, Giuseppe Gumina, Wen Zhou, Raymond F. Schinazi, and Chung K. Chu
pp 1313–1320Publication Date (Web): February 09, 2002 (Article)
DOI: 10.1021/jm010418n
Development of Long-Acting Dopamine Transporter Ligands as Potential Cocaine-Abuse Therapeutic Agents: Chiral Hydroxyl-Containing Derivatives of 1-[2-[Bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine and 1-[2-(Diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine
Ling-Wei Hsin, Christina M. Dersch, Michael H. Baumann, David Stafford, John R. Glowa, Richard B. Rothman, Arthur E. Jacobson, and Kenner C. Rice
pp 1321–1329Publication Date (Web): February 06, 2002 (Article)
DOI: 10.1021/jm010430f
Syntheses and Antiproliferative Activities of New Rebeccamycin Derivatives with the Sugar Unit Linked to Both Indole Nitrogens
Christelle Marminon, Fabrice Anizon, Pascale Moreau, Stéphane Léonce, Alain Pierré, Bruno Pfeiffer, Pierre Renard, and Michelle Prudhomme
pp 1330–1339Publication Date (Web): February 12, 2002 (Article)
DOI: 10.1021/jm011045t
Synthesis and Mode of Action of Hydrophobic Derivatives of the Glycopeptide Antibiotic Eremomycin and Des-(N-methyl-d-leucyl)eremomycin against Glycopeptide-Sensitive and -Resistant Bacteria
Svetlana S. Printsevskaya, Andrey Y. Pavlov, Evgenia N. Olsufyeva, Elena P. Mirchink, Elena B. Isakova, Marina I. Reznikova, Robert C. Goldman, Arthur A. Branstrom, Eugene R. Baizman, Clifford B. Longley, Ferenc Sztaricskai, Gyula Batta, and Maria N. Preobrazhenskaya
pp 1340–1347Publication Date (Web): February 09, 2002 (Article)
DOI: 10.1021/jm010460i
Design and Synthesis of a Novel and Potent Series of Inhibitors of Cytosolic Phospholipase A2 Based on a 1,3-Disubstituted Propan-2-one Skeleton
Stephen Connolly, Colin Bennion, Sarah Botterell, Pamela J. Croshaw, Catherine Hallam, Kim Hardy, Paul Hartopp, Clive G. Jackson, Sarah J. King, Louise Lawrence, Antonio Mete, David Murray, David H. Robinson, Gillian M. Smith, Linda Stein, Iain Walters, Edward Wells, and W. John Withnall
pp 1348–1362Publication Date (Web): February 08, 2002 (Article)
DOI: 10.1021/jm011050x
Stereochemistry at Phosphorus of the Reaction Catalyzed by myo-Inositol Monophosphatase
Christine M.-J. Fauroux, Michael Lee, Paul M. Cullis, Kenneth T. Douglas, Michael G. Gore, and Sally Freeman
pp 1363–1373Publication Date (Web): February 13, 2002 (Article)
DOI: 10.1021/jm011056m
Synthesis and Notable Antimalarial Activity of Acyclic Peroxides, 1-(Alkyldioxy)-1-(methyldioxy)cyclododecanes
Yoshiaki Hamada, Hidekazu Tokuhara, Araki Masuyama, Masatomo Nojima, Hye-Sook Kim, Kanako Ono, Naoki Ogura, and Yusuke Wataya
pp 1374–1378Publication Date (Web): February 13, 2002 (Article)
DOI: 10.1021/jm010473w
Brief Articles
Design and Synthesis of a Novel L-Dopa−Entacapone Codrug
Jukka Leppänen, Juhani Huuskonen, Tapio Nevalainen, Jukka Gynther, Hannu Taipale, and Tomi Järvinen
pp 1379–1382Publication Date (Web): February 12, 2002 (Brief Article)
DOI: 10.1021/jm010980d
Synthesis and Antimycobacterial Activity of 6-Arylpurines: The Requirements for the N-9 Substituent in Active Antimycobacterial Purines
Lise-Lotte Gundersen, Jon Nissen-Meyer, and Bjørn Spilsberg
pp 1383–1386Publication Date (Web): February 06, 2002 (Brief Article)
DOI: 10.1021/jm0110284
Lipoamino Acid-Based Adjuvant Carrier System: Enhanced Immunogenicity of Group A Streptococcal Peptide Epitopes
Anikó Horváth, Colleen Olive, Allan Wong, Timothy Clair, Penny Yarwood, Michael Good, and Istvan Toth
pp 1387–1390Publication Date (Web): February 12, 2002 (Brief Article)
DOI: 10.1021/jm0110441
Book Reviews
Combinatorial Library Design and Evaluation Edited by Arup K. Ghose and Vellarkad N. Viswanadhan. Marcel Dekker Inc., New York. 2001. xv + 631 pp. 16 × 23.5 cm. ISBN 0-8247-0487-8. $195.00.
Jan W. F. Wasley
p 1391Publication Date (Web): October 23, 2008 (Book Review)
DOI: 10.1021/jm0105732
The Nitro Group in Organic Synthesis By Noboru Ono. Wiley-VCH, New York. 2001. xvi + 372 pp. 16 × 24 cm. ISBN 0-471-31611-3. $130.00.
Bruce L. Currie
pp 1391–1392Publication Date (Web): October 23, 2008 (Book Review)
DOI: 10.1021/jm020011y
Chiral Intermediates Edited by Cynthia A. Challener. Ashgate Publishing, Burlington, VT. 2001. xxiii + 804 pp. 18 × 25 cm. ISBN 0-5660-8412-0. $295.00.
Patrick Dussault
p 1392Publication Date (Web): February 09, 2002 (Book Review)
DOI: 10.1021/jm020013i
Methods in Enzymology. Volume 340. Drug−Nucleic Acid Interactions Edited by Jonathan B. Chaires and Michael J. Waring. Academic Press, New York. 2001. xxxiv + 705 pp. 16 × 23.5 cm. ISBN 0-12-182241-9. $129.95.
D. Eric Walters
p 1392Publication Date (Web): February 13, 2002 (Book Review)
DOI: 10.1021/jm0200254
Goodman and Gilman's The Pharmacological Basis of Therapeutics. 10th Edition Edited by J. G. Hardman, L. E. Limbird, and A. G. Gilman. McGraw Hill, New York. 2001. xxvii + 2148 pp. 21 × 26 cm. ISBN 0-07-1354469-7. $125.00.
Kennerly S. Patrick
pp 1392–1393Publication Date (Web): February 14, 2002 (Book Review)
DOI: 10.1021/jm020026w
Books of Interest
p 1394Publication Date (Web): February 12, 2002 (Book Review)
DOI: 10.1021/jm020032s