Table of Contents
January 31, 2002
Volume 45, Issue 3
Pages 541-752
Perspectives
Designing Non-Peptide Peptidomimetics in the 21st Century: Inhibitors Targeting Conformational Ensembles
Matthew G. Bursavich and Daniel H. Rich
pp 541–558Publication Date (Web): January 24, 2002 (Perspective)
DOI: 10.1021/jm010425b
Hi-Res PDF Letters
Design, Synthesis and Activity of Ascorbic Acid Prodrugs of Nipecotic, Kynurenic and Diclophenamic Acids, Liable to Increase Neurotropic Activity
Stefano Manfredini, Barbara Pavan, Silvia Vertuani, Martina Scaglianti, Donatello Compagnone, Carla Biondi, Angelo Scatturin, Sergio Tanganelli, Luca Ferraro, Puttur Prasad, and Alessandro Dalpiaz
pp 559–562Publication Date (Web): December 21, 2001 (Letter)
DOI: 10.1021/jm015556r
Discovery of a 3-Amino-6-phenyl-pyridazine Derivative as a New Synthetic Antineuroinflammatory Compound
Salida Mirzoeva, Anu Sawkar, Magdalena Zasadzki, Ling Guo, Anastasia V. Velentza, Vincent Dunlap, Jean-Jacques Bourguignon, Helena Ramstrom, Jacques Haiech, Linda J. Van Eldik, and D. Martin Watterson
pp 563–566Publication Date (Web): December 28, 2001 (Letter)
DOI: 10.1021/jm015573g
Articles
Synthesis and Evaluation of Potent and Selective β3 Adrenergic Receptor Agonists Containing Acylsulfonamide, Sulfonylsulfonamide, and Sulfonylurea Carboxylic Acid Isosteres
David E. Uehling, Kelly H. Donaldson, David N. Deaton, Clifton E. Hyman, Elizabeth E. Sugg, David G. Barrett, Robert G. Hughes, Barbara Reitter, Kim K. Adkison, Mary E. Lancaster, Frank Lee, Robert Hart, Mark A. Paulik, Bryan W. Sherman, Timothy True, and Conrad Cowan
pp 567–583Publication Date (Web): December 29, 2001 (Article)
DOI: 10.1021/jm0101500
Identification of a Second Binding Site in the Estrogen Receptor
Willem P. van Hoorn
pp 584–589Publication Date (Web): December 19, 2001 (Article)
DOI: 10.1021/jm0109661
Antitumor Polycyclic Acridines. 8.1 Synthesis and Telomerase-Inhibitory Activity of Methylated Pentacyclic Acridinium Salts
Robert A. Heald, Chetna Modi, Jenny C. Cookson, Ian Hutchinson, Charles A. Laughton, Sharon M. Gowan, Lloyd R. Kelland, and Malcolm F. G. Stevens
pp 590–597Publication Date (Web): December 21, 2001 (Article)
DOI: 10.1021/jm011015q
Synthesis and Biological Activity of a Novel Class of Small Molecular Weight Peptidomimetic Competitive Inhibitors of Protein Tyrosine Phosphatase 1B
Scott D. Larsen, Tjeerd Barf, Charlotta Liljebris, Paul D. May, Derek Ogg, Theresa J. O'Sullivan, Barbara J. Palazuk, Heinrich J. Schostarez, F. Craig Stevens, and John E. Bleasdale
pp 598–622Publication Date (Web): December 29, 2001 (Article)
DOI: 10.1021/jm010393s
Synthesis and Preliminary Characterization of a Novel Antiarrhythmic Compound (KB130015) with an Improved Toxicity Profile Compared with Amiodarone
Bo Carlsson, B. N. Singh, Marcel Temciuc, Stefan Nilsson, Yi-Lin Li, Charlotta Mellin, and Johan Malm
pp 623–630Publication Date (Web): January 03, 2002 (Article)
DOI: 10.1021/jm001126+
Full Text HTMLDesign, Synthesis, and Evaluation of Novel 2-Substituted 3-Hydroxypyridin-4-ones: Structure−Activity Investigation of Metalloenzyme Inhibition by Iron Chelators
Zu D. Liu, Reem Kayyali, Robert C. Hider, John B. Porter, and Anthony E. Theobald
pp 631–639Publication Date (Web): January 5, 2002 (Article)
DOI: 10.1021/jm010817i
Synthesis and Optimization of a New Family of Type 3 17β-Hydroxysteroid Dehydrogenase Inhibitors by Parallel Liquid-Phase Chemistry
René Maltais, Van Luu-The, and Donald Poirier
pp 640–653Publication Date (Web): December 27, 2001 (Article)
DOI: 10.1021/jm010286y
Expansion of Structure−Activity Studies of Piperidine Analogues of 1-[2-(Diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine (GBR 12935) Compounds by Altering Substitutions in the N-Benzyl Moiety and Behavioral Pharmacology of Selected Molecules
Aloke K. Dutta, Matthew C. Davis, Xiang-Shu Fei, Patrick M. Beardsley, Charles D. Cook, and Maarten. E. A. Reith
pp 654–662Publication Date (Web): December 21, 2001 (Article)
DOI: 10.1021/jm010316x
Correlation of the Antibacterial Activities of Cationic Peptide Antibiotics and Cationic Steroid Antibiotics1
Bangwei Ding, Qunying Guan, Joshua P. Walsh, J. Scott Boswell, Tim W. Winter, Erica S. Winter, Stephanie S. Boyd, Chunhong Li, and Paul B. Savage
pp 663–669Publication Date (Web): December 22, 2001 (Article)
DOI: 10.1021/jm0105070
Design and Synthesis of Motilin Antagonists Derived from the [1−4] Fragment of Porcine Motilin
Masayuki Haramura, Akira Okamachi, Kouichi Tsuzuki, Kenji Yogo, Makoto Ikuta, Toshiro Kozono, Hisanori Takanashi, and Eigoro Murayama
pp 670–675Publication Date (Web): January 8, 2002 (Article)
DOI: 10.1021/jm010332u
Identification of Potent and Selective Mechanism-Based Inhibitors of the Cysteine Protease Cruzain Using Solid-Phase Parallel Synthesis
Lily Huang, Alice Lee, and Jonathan A. Ellman
pp 676–684Publication Date (Web): December 29, 2001 (Article)
DOI: 10.1021/jm010333m
Synthesis of 1-(3,4-Dihydroxy-5-nitrophenyl)-2-phenyl-ethanone and Derivatives as Potent and Long-Acting Peripheral Inhibitors of Catechol-O-methyltransferase
David A. Learmonth, Maria A. Vieira-Coelho, Jan Benes, Paula C. Alves, Nuno Borges, Ana P. Freitas, and Patrício Soares-da-Silva
pp 685–695Publication Date (Web): December 22, 2001 (Article)
DOI: 10.1021/jm0109964
2,6-Di(ω-aminoalkyl)-2,5,6,7-tetrahydropyrazolo[3,4,5-mn]pyrimido[5,6,1-de]acridine-5,7-diones: Novel, Potent, Cytotoxic, and DNA-Binding Agents
Ippolito Antonini, Paolo Polucci, Amelia Magnano, Barbara Gatto, Manlio Palumbo, Ernesto Menta, Nicoletta Pescalli, and Sante Martelli
pp 696–702Publication Date (Web): December 21, 2001 (Article)
DOI: 10.1021/jm011004x
Novel Mycophenolic Adenine Bis(phosphonate) Analogues As Potential Differentiation Agents against Human Leukemia1
Krzysztof W. Pankiewicz, Krystyna B. Lesiak-Watanabe, Kyoichi A. Watanabe, Steven E. Patterson, Hiremagalur N. Jayaram, Joel A. Yalowitz, Michael D. Miller, Michael Seidman, Alokes Majumdar, Gerd Prehna, and Barry M. Goldstein
pp 703–712Publication Date (Web): January 8, 2002 (Article)
DOI: 10.1021/jm0104116
Evaluation of the Dmt−Tic Pharmacophore: Conversion of a Potent δ-Opioid Receptor Antagonist into a Potent δ Agonist and Ligands with Mixed Properties
Gianfranco Balboni, Remo Guerrini, Severo Salvadori, Clementina Bianchi, Daniela Rizzi, Sharon D. Bryant, and Lawrence H. Lazarus
pp 713–720Publication Date (Web): January 5, 2002 (Article)
DOI: 10.1021/jm010449i
Novel Angular Benzophenazines: Dual Topoisomerase I and Topoisomerase II Inhibitors as Potential Anticancer Agents
Nigel Vicker, Luke Burgess, Irina S. Chuckowree, Rory Dodd, Adrian J. Folkes, David J. Hardick, Timothy C. Hancox, Warren Miller, John Milton, Sukhjit Sohal, Shouming Wang, Stephen P. Wren, Peter A. Charlton, Wendy Dangerfield, Chris Liddle, Prakash Mistry, Alistair J. Stewart, and William A. Denny
pp 721–739Publication Date (Web): January 8, 2002 (Article)
DOI: 10.1021/jm010329a
Brief Articles
Structure−Activity Relationships for Pyrido-, Imidazo-, Pyrazolo-, Pyrazino-, and Pyrrolophenazinecarboxamides as Topoisomerase-Targeted Anticancer Agents
Swarna A. Gamage, Julie A. Spicer, Gordon W. Rewcastle, John Milton, Sukhjit Sohal, Wendy Dangerfield, Prakash Mistry, Nigel Vicker, Peter A. Charlton, and William A. Denny
pp 740–743Publication Date (Web): January 8, 2002 (Brief Article)
DOI: 10.1021/jm010330+
Antitumor Benzothiazoles. 16.1 Synthesis and Pharmaceutical Properties of Antitumor 2-(4-Aminophenyl)benzothiazole Amino Acid Prodrugs
Ian Hutchinson, Sharon A. Jennings, B. Rao Vishnuvajjala, Andrew D. Westwell, and Malcolm F. G. Stevens
pp 744–747Publication Date (Web): December 20, 2001 (Brief Article)
DOI: 10.1021/jm011025r
New Neplanocin Analogues. 12. Alternative Synthesis and Antimalarial Effect of (6‘R)-6‘-C-Methylneplanocin A, a Potent AdoHcy Hydrolase Inhibitor1
Satoshi Shuto, Noriaki Minakawa, Satoshi Niizuma, Hye-Sook Kim, Yusuke Wataya, and Akira Matsuda
pp 748–751Publication Date (Web): January 5, 2002 (Brief Article)
DOI: 10.1021/jm010374i
Additions and Corrections
Synthesis and Comparative Molecular Field Analysis (CoMFA) of Symmetric and Nonsymmetric Cyclic Sulfamide HIV-1 Protease Inhibitors.
Wesley Schaal, Anna Karlsson, Göran Ahlsén, Jimmy Lindberg, Hans O. Andersson, U. Helena Danielson, Björn Classon, Torsten Unge, Bertil Samuelsson, Johan Hultén, Anders Hallberg, and Anders Karlén:
p 752Publication Date (Web): January 8, 2002 (Addition/Correction)
DOI: 10.1021/jm011105v