Table of Contents
February 27, 2003
Volume 46, Issue 5
Pages 655-882
Perspectives
Immobilized Artificial Membrane HPLC in Drug Research
Agnes Taillardat-Bertschinger, Pierre-Alain Carrupt, Francesco Barbato, and Bernard Testa
pp 655–665Publication Date (Web): January 30, 2003 (Perspective)
DOI: 10.1021/jm020265j
Hi-Res PDFDesign and Synthesis of the Potent, Orally Available, Brain-Penetrable Arylpyrazole Class of Neuropeptide Y5 Receptor Antagonists
Nagaaki Sato, Toshiyuki Takahashi, Takunobu Shibata, Yuji Haga, Aya Sakuraba, Masaaki Hirose, Miki Sato, Katsumasa Nonoshita, Yuko Koike, Hidefumi Kitazawa, Naoko Fujino, Yasuyuki Ishii, Akane Ishihara, Akio Kanatani, and Takehiro Fukami
pp 666–669Publication Date (Web): January 24, 2003 (Letter)
DOI: 10.1021/jm025513q
In Vitro and in Vivo Characterization of 3-{2-[6-(2-tert-Butoxyethoxy)pyridin-3-yl]-1H-imidazol-4-yl}benzonitrile Hydrochloride Salt, a Potent and Selective NPY5 Receptor Antagonist
Richard L. Elliott, Robert M. Oliver, Marlys Hammond, Terrell A. Patterson, Li She, Diane M. Hargrove, Kelly A. Martin, Tristan S. Maurer, J. Cory Kalvass, Bradley P. Morgan, Paul A. DaSilva-Jardine, Ralph W. Stevenson, Christine M. Mack, and James V. Cassella
pp 670–673Publication Date (Web): February 04, 2003 (Letter)
DOI: 10.1021/jm025584p
Synthesis and Biological Evaluation of Novel Cyclosporin A Analogues: Potential Soft Drugs for the Treatment of Autoimmune Diseases
Tsvetelina Lazarova, Jason S. Chen, Blake Hamann, Jane M. Kang, Daniela Homuth-Trombino, Feng Han, Ethan Hoffmann, Christopher McClure, Jens Eckstein, and Yat Sun Or
pp 674–676Publication Date (Web): January 29, 2003 (Letter)
DOI: 10.1021/jm025595i
2,6-Dimethyltyrosine Analogues of a Stereodiversified Ligand Library: Highly Potent, Selective, Non-Peptidic μ Opioid Receptor Agonists
Bryce A. Harrison, Gavril W. Pasternak, and Gregory L. Verdine
pp 677–680Publication Date (Web): January 29, 2003 (Letter)
DOI: 10.1021/jm025608s
Discovery of an Orally Efficacious Inhibitor of Coagulation Factor Xa Which Incorporates a Neutral P1 Ligand
Yong Mi Choi-Sledeski, Robert Kearney, Gregory Poli, Henry Pauls, Charles Gardner, Yong Gong, Michael Becker, Roderick Davis, Alfred Spada, Guyan Liang, Valeria Chu, Karen Brown, Dennis Collussi, Robert Leadley, Jr., Sam Rebello, Phillip Moxey, Suzanne Morgan, Ross Bentley, Charles Kasiewski, Sebastien Maignan, Jean-Pierre Guilloteau, and Vincent Mikol
pp 681–684Publication Date (Web): February 04, 2003 (Letter)
DOI: 10.1021/jm020384z
Articles
Molecular Structures of Human Factor Xa Complexed with Ketopiperazine Inhibitors: Preference for a Neutral Group in the S1 Pocket
Sébastien Maignan, Jean-Pierre Guilloteau, Yong Mi Choi-Sledeski, Michael R. Becker, William R. Ewing, Henry W. Pauls, Alfred P. Spada, and Vincent Mikol
pp 685–690Publication Date (Web): February 01, 2003 (Article)
DOI: 10.1021/jm0203837
Tricyclic Indole-2-carboxylic Acids: Highly in Vivo Active and Selective Antagonists for the Glycine Binding Site of the NMDA Receptor
Seiji Katayama, Nobuyuki Ae, Toru Kodo, Shuji Masumoto, Shinji Hourai, Chika Tamamura, Hiroyasu Tanaka, and Ryu Nagata
pp 691–701Publication Date (Web): January 24, 2003 (Article)
DOI: 10.1021/jm020239l
Synthesis and Structure−Affinity Relationships of Novel N-(1-Ethyl-4-methylhexahydro-1,4-diazepin-6-yl)pyridine-3-carboxamides with Potent Serotonin 5-HT3 and Dopamine D2 Receptor Antagonistic Activity
Yoshimi Hirokawa, Iwao Fujiwara, Kenji Suzuki, Hiroshi Harada, Takashi Yoshikawa, Naoyuki Yoshida, and Shiro Kato
pp 702–715Publication Date (Web): February 01, 2003 (Article)
DOI: 10.1021/jm020270n
Non-Peptide Angiotensin II Receptor Antagonists: Chemical Feature Based Pharmacophore Identification
Eva M. Krovat and Thierry Langer
pp 716–726Publication Date (Web): February 01, 2003 (Article)
DOI: 10.1021/jm021032v
Synthesis and Dopamine Receptor Modulating Activity of 3-Substituted γ-Lactam Peptidomimetics of l-Prolyl-l-leucyl-glycinamide
Kristine Dolbeare, Giuseppe F. Pontoriero, Suresh K. Gupta, Ram K. Mishra, and Rodney L. Johnson
pp 727–733Publication Date (Web): January 18, 2003 (Article)
DOI: 10.1021/jm020441o
Design and Synthesis of Plasmepsin I and Plasmepsin II Inhibitors with Activity in Plasmodium falciparum-Infected Cultured Human Erythrocytes
Daniel Nöteberg, Elizabeth Hamelink, Johan Hultén, Mats Wahlgren, Lotta Vrang, Bertil Samuelsson, and Anders Hallberg
pp 734–746Publication Date (Web): January 22, 2003 (Article)
DOI: 10.1021/jm020951i
Antiinflammatory, Gastrosparing, and Antiplatelet Properties of New NO-Donor Esters of Aspirin
Clara Cena, Marco L. Lolli, Loretta Lazzarato, Elena Guaita, Giuseppina Morini, Gabriella Coruzzi, Stuart P. McElroy, Ian L. Megson, Roberta Fruttero, and Alberto Gasco
pp 747–754Publication Date (Web): February 01, 2003 (Article)
DOI: 10.1021/jm020969t
Antileishmanial Ring-Substituted Ether Phospholipids
Nikos Avlonitis, Eleni Lekka, Anastasia Detsi, Maria Koufaki, Theodora Calogeropoulou, Efi Scoulica, Eleni Siapi, Ioanna Kyrikou, Thomas Mavromoustakos, Andrew Tsotinis, Simona Golic Grdadolnik, and Alexandros Makriyannis
pp 755–767Publication Date (Web): February 04, 2003 (Article)
DOI: 10.1021/jm020972c
Design, Synthesis, SAR, and Molecular Modeling Studies of Acylthiocarbamates: A Novel Series of Potent Non-nucleoside HIV-1 Reverse Transcriptase Inhibitors Structurally Related to Phenethylthiazolylthiourea Derivatives
Angelo Ranise, Andrea Spallarossa, Silvia Schenone, Olga Bruno, Francesco Bondavalli, Laura Vargiu, Tiziana Marceddu, Massimo Mura, Paolo La Colla, and Alessandra Pani
pp 768–781Publication Date (Web): February 04, 2003 (Article)
DOI: 10.1021/jm0209984
S-Acyl-2-Thioethyl Aryl Phosphotriester Derivatives of AZT: Synthesis, Antiviral Activity, and Stability Study
Suzanne Peyrottes, Gaëlle Coussot, Isabelle Lefebvre, Jean-Louis Imbach, Gilles Gosselin, Anne-Marie Aubertin, and Christian Périgaud
pp 782–793Publication Date (Web): February 01, 2003 (Article)
DOI: 10.1021/jm021016y
Synthesis and Biological Effects of Novel 2-Amino-3-naphthoylthiophenes as Allosteric Enhancers of the A1 Adenosine Receptor
Pier Giovanni Baraldi, Romeo Romagnoli, Maria Giovanna Pavani, Maria del Carmen Nuñez, Mojgan Aghazadeh Tabrizi, John C. Shryock, Edward Leung, Allan R. Moorman, Canan Uluoglu, Valeria Iannotta, Stefania Merighi, and Pier Andrea Borea
pp 794–809Publication Date (Web): January 28, 2003 (Article)
DOI: 10.1021/jm0210212
Design of Novel Chimeric Melanotropin−Deltorphin Analogues. Discovery of the First Potent Human Melanocortin 1 Receptor Antagonist
G. Han, J. M. Quillan, K. Carlson, W. Sadée, and V. J. Hruby
pp 810–819Publication Date (Web): January 30, 2003 (Article)
DOI: 10.1021/jm020355o
Development of Potential Antitumor Agents. Synthesis and Biological Evaluation of a New Set of Sulfonamide Derivatives as Histone Deacetylase Inhibitors
Giliane Bouchain, Silvana Leit, Sylvie Frechette, Elie Abou Khalil, Rico Lavoie, Oscar Moradei, Soon Hyung Woo, Marielle Fournel, Pu T. Yan, Ann Kalita, Marie-Claude Trachy-Bourget, Carole Beaulieu, Zuomei Li, Marie-France Robert, A. Robert MacLeod, Jeffrey M. Besterman, and Daniel Delorme
pp 820–830Publication Date (Web): January 30, 2003 (Article)
DOI: 10.1021/jm020377a
Synthesis and Flow Cytometric Evaluation of Novel 1,2,3,4-Tetrahydroisoquinoline Conformationally Constrained Analogues of Nitrobenzylmercaptopurine Riboside (NBMPR) Designed for Probing Its Conformation When Bound to the es Nucleoside Transporter
Zhengxiang Zhu, John Furr, and John K. Buolamwini
pp 831–837Publication Date (Web): January 24, 2003 (Article)
DOI: 10.1021/jm020405p
Syntheses and Opioid Receptor Binding Affinities of 8-Amino-2,6-methano-3-benzazocines
Mark P. Wentland, Yingchun Ye, Christopher L. Cioffi, Rongliang Lou, Qun Zhou, Guoyou Xu, Wenhu Duan, Christoph M. Dehnhardt, Xufeng Sun, Dana J. Cohen, and Jean M. Bidlack
pp 838–849Publication Date (Web): February 01, 2003 (Article)
DOI: 10.1021/jm020429w
Novel α-Melanocyte Stimulating Hormone Peptide Analogues with High Candidacidal Activity
Paolo Grieco, Claudia Rossi, Gualtiero Colombo, Stefano Gatti, Ettore Novellino, James M. Lipton, and Anna Catania
pp 850–855Publication Date (Web): January 30, 2003 (Article)
DOI: 10.1021/jm0204338
Structure−Activity Relationships of Dimethindene Derivatives as New M2-Selective Muscarinic Receptor Antagonists
Thomas M. Böhme, Christine Keim, Kai Kreutzmann, Matthias Linder, Theo Dingermann, Gerd Dannhardt, Ernst Mutschler, and Günter Lambrecht
pp 856–867Publication Date (Web): January 30, 2003 (Article)
DOI: 10.1021/jm020895l
Brief Articles
Structure−Activity Relationship Study and Drug Profile of N-(4-Fluorophenylsulfonyl)-l-valyl-l-leucinal (SJA6017) as a Potent Calpain Inhibitor
Jun Inoue, Masayuki Nakamura, Ying-She Cui, Yusuke Sakai, Osamu Sakai, Jeanette R. Hill, Kevin K. W. Wang, and Po-Wai Yuen
pp 868–871Publication Date (Web): February 01, 2003 (Brief Article)
DOI: 10.1021/jm0201924
Three-Dimensional Structure of the Ligand-Binding Core of GluR2 in Complex with the Agonist (S)-ATPA: Implications for Receptor Subunit Selectivity
Marie-Louise Lunn, Anders Hogner, Tine B. Stensbøl, Eric Gouaux, Jan Egebjerg, and Jette S. Kastrup
pp 872–875Publication Date (Web): January 30, 2003 (Brief Article)
DOI: 10.1021/jm021020+
Full Text HTMLEvaluation of the First Cytostatically Active 1-Aza-9-oxafluorenes as Novel Selective CDK1 Inhibitors with P-Glycoprotein Modulating Properties
Kristin Brachwitz, Burkhardt Voigt, Laurent Meijer, Olivier Lozach, Christoph Schächtele, Josef Molnár, and Andreas Hilgeroth
pp 876–879Publication Date (Web): February 01, 2003 (Brief Article)
DOI: 10.1021/jm021090g
Book Reviews
Software Program Title: Molecular Conceptor Drug Design Courseware. Version 1.02 By Claude Cohen. Synergix Ltd., Jerusalem, Israel. August, 2002. CD-ROM (plus HASP key, table of contents, and installation guide). ISBN 965-90508-0-1. $4900 (commercial), $2900 (academic).
Peter Gund
pp 880–881Publication Date (Web): January 25, 2003 (Book Review)
DOI: 10.1021/jm020551v
Alkaloids. Nature's Curse or Blessing? By Manfred Hesse. Wiley-VCH, Weinheim, Germany. 2002. xii + 413 pp. 22 × 23.5 cm. ISBN 3906390241. $115.00.
Joseph G. Cannon
p 881Publication Date (Web): January 29, 2003 (Book Review)
DOI: 10.1021/jm0205503
Additions and Corrections
Design and Synthesis of Dipeptide Nitriles as Reversible and Potent Cathepsin S Inhibitors.
Yancey D. Ward, David S. Thomson, Leah L. Frye, Charles L. Cywin, Tina Morwick, Michel J. Emmanuel, Renée Zindell, Daniel McNeil, Younes Bekkali, Marc Girardot, Matt Hrapchak, Molly DeTuri, Kathy Crane, Della White, Susan Pav, Yong Wang, Ming-Hong Hao, Christine A. Grygon, Mark E. Labadia, Dorothy M. Freeman, Walter Davidson, Jerry L. Hopkins, Maryanne L. Brown, and Denice M. Spero:
p 882Publication Date (Web): January 24, 2003 (Addition/Correction)
DOI: 10.1021/jm030013y