Journal of Medicinal Chemistry
Volume 43, Issue 25 (December 14, 2000)
Copyright © 2000 American Chemical Society

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EDITORIAL

4725-4725

Web Submission of Letters To Replace Communications Philip S. Portoghese Editor-in-Chief [Full Article - PDF]

ARTICLES

4726-4737

Synthesis and Structure-Activity Relationships of Chiral Allosteric Modifiers of Hemoglobin Melissa Phelps Grella, Richmond Danso-Danquah, Martin K. Safo, Gajanan S. Joshi, Jean Kister, Michael Marden, Stephen J. Hoffman, and Donald J. Abraham [Full Article - PDF]

4738-4746

Ethylene Glycol and Amino Acid Derivatives of 5-Aminolevulinic Acid as New Photosensitizing Precursors of Protoporphyrin IX in Cells Yann Berger, Alain Greppi, Olivier Siri, Reinhard Neier, and Lucienne Juillerat-Jeanneret [Full Article - PDF]

4747-4758

Inhibition of Monoamine Oxidases by Functionalized Coumarin Derivatives: Biological Activities, QSARs, and 3D-QSARs Carmela Gnerre, Marco Catto, Francesco Leonetti, Peter Weber, Pierre-Alain Carrupt, Cosimo Altomare, Angelo Carotti, and Bernard Testa [Full Article - PDF]

4759-4767

Protein-Based Virtual Screening of Chemical Databases. 1. Evaluation of Different Docking/Scoring Combinations Caterina Bissantz, Gerd Folkers, and Didier Rognan [Full Article - PDF]

4768-4780

Pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine Derivatives as Highly Potent and Selective Human A3 Adenosine Receptor Antagonists: Influence of the Chain at the N8 Pyrazole Nitrogen Pier Giovanni Baraldi, Barbara Cacciari, Romeo Romagnoli, Giampiero Spalluto, Stefano Moro, Karl-Norbert Klotz, Edward Leung, Katia Varani, Stefania Gessi, Stefania Merighi, and Pier Andrea Borea [Full Article - PDF]

4781-4786

Design of Adenosine Kinase Inhibitors from the NMR-Based Screening of Fragments Philip J. Hajduk, Arthur Gomtsyan, Stanley Didomenico, Marlon Cowart, Erol K. Bayburt, Larry Solomon, Jean Severin, Richard Smith, Karl Walter, Thomas F. Holzman, Andrew Stewart, Steve McGaraughty, Michael F. Jarvis, Elizabeth A. Kowaluk, and Stephen W. Fesik [Full Article - PDF]

4787-4792

Chemical Syntheses and Biological Activities of Lactam Analogues of -Conotoxin SI Balazs Hargittai, Núria A. Solé, Duncan R. Groebe, Stewart N. Abramson, and George Barany [Full Article - PDF]

4793-4800

Semisynthesis of Antitumoral Acetogenins: SAR of Functionalized Alkyl-Chain Bis-Tetrahydrofuranic Acetogenins, Specific Inhibitors of Mitochondrial Complex I Teresa Gallardo, M. Carmen Zafra-Polo, José R. Tormo, M. Carmen González, Xavier Franck, Ernesto Estornell, and Diego Cortes [Full Article - PDF]

4801-4805

N4-(-Aminoalkyl)-1-[(-aminoalkyl)amino]-4-acridinecarboxamides: Novel, Potent, Cytotoxic, and DNA-Binding Agents Ippolito Antonini, Paolo Polucci, Lloyd R. Kelland, Silvano Spinelli, Nicoletta Pescalli, and Sante Martelli [Full Article - PDF]

4806-4811

Synthesis and Antitumor Activities of Novel Pyrimidine Derivatives of 2,3-O,O-Dibenzyl-6-deoxy-L-ascorbic Acid and 4,5-Didehydro-5,6- dideoxy-L-ascorbic Acid Silvana Rai-Mali, Draenka Svedrui, Tatjana Gazivoda, Andreja Marunovi, Antonija Hergold-Brundi, Ante Nagl, Jan Balzarini, Erik De Clercq, and Mladen Mintas [Full Article - PDF]

4812-4821

(2,2':6',2' '-Terpyridine)platinum(II) Complexes Are Irreversible Inhibitors of Trypanosoma cruzi Trypanothione Reductase But Not of Human Glutathione Reductase Susanne Bonse, Jonathan M. Richards, Steven A. Ross, Gordon Lowe, and R. Luise Krauth-Siegel [Full Article - PDF]

4822-4833

Non-depolarizing Neuromuscular Blocking Activity of Bisquaternary Amino Di- and Tripeptide Derivatives Leo H. D. J. Booij, Leon A. G. M. van der Broek, Wilson Caulfield, Brigitte M. G. Dommerholt-Caris, John K. Clark, Jan van Egmond, Ross McGuire, Alan W. Muir, Harry C. J. Ottenheijm, and David C. Rees [Full Article - PDF]

4834-4839

Synthesis and Evaluation of Pharmacological and Pharmacokinetic Properties of 11H-[1,2,4]Triazolo[4,5-c][2,3]benzodiazepin-3(2H)-ones Maria Zappalà, Rosaria Gitto, Francesca Bevacqua, Silvana Quartarone, Alba Chimirri, Milena Rizzo, Giovambattista De Sarro, and Angela De Sarro [Full Article - PDF]

4840-4849

Synthesis and Transporter Binding Properties of Bridged Piperazine Analogues of 1-{2-[Bis(4-fluorophenyl)methoxy]ethyl}-4-(3-phenylpropyl)piperazine (GBR 12909) Ying Zhang, Richard B. Rothman, Christina M. Dersch, Brian R. de Costa, Arthur E. Jacobson, and Kenner C. Rice [Full Article - PDF]

4850-4867

Synthesis, Structure-Activity Relationships, and Pharmacological Profile of 9-Amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro[1,4]diazepino[6,7,1-hi]indoles: Discovery of Potent, Selective Phosphodiesterase Type 4 Inhibitors Catherine Burnouf, Eric Auclair, Nadine Avenel, Bernadette Bertin, Christèle Bigot, Alain Calvet, Kam Chan, Corinne Durand, Veronique Fasquelle, Frédéric Féru, Richard Gilbertsen, Henry Jacobelli, Adel Kebsi, Emmanuelle Lallier, Jacquie Maignel, Brigitte Martin, Stéphane Milano, Malika Ouagued, Yves Pascal, Marie-Pierre Pruniaux, Jocelyne Puaud, Marie-Noëlle Rocher, Christophe Terrasse, Roger Wrigglesworth, and Annette M. Doherty [Full Article - PDF]

4868-4876

Design, Synthesis, and Monoamine Transporter Binding Site Affinities of Methoxy Derivatives of Indatraline Xiao-Hui Gu, Han Yu, Arthur E. Jacobson, Richard B. Rothman, Christina M. Dersch, Clifford George, Judith L. Flippen-Anderson, and Kenner C. Rice [Full Article - PDF]

4877-4883

Synthesis and Antitumor Activity of Thieno-Separated Tricyclic Purines Katherine L. Seley, Piotr Januszczyk, Asmerom Hagos, and Liang Zhang , Daniel T. Dransfield [Full Article - PDF]

4884-4892

Carbonic Anhydrase Inhibitors: Water-Soluble 4-Sulfamoylphenylthioureas as Topical Intraocular Pressure-Lowering Agents with Long-Lasting Effects Angela Casini, Andrea Scozzafava, Francesco Mincione, Luca Menabuoni, Marc A. Ilies, and Claudiu T. Supuran [Full Article - PDF]

4893-4909

Synthesis, SARs, and Pharmacological Characterization of 2-Amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic Acid Derivatives as Potent, Selective, and Orally Active Group II Metabotropic Glutamate Receptor Agonists Atsuro Nakazato, Toshihito Kumagai, Kazunari Sakagami, Ryoko Yoshikawa, Yoshiko Suzuki, Shigeyuki Chaki, Hisanaka Ito, Takeo Taguchi, Shigetada Nakanishi, and Shigeru Okuyama [Full Article - PDF]

4910-4918

Structural Determinants of AMPA Agonist Activity in Analogues of 2-Amino-3-(3-carboxy-5-methyl-4-isoxazolyl)propionic Acid: Synthesis and Pharmacology Benny Bang-Andersen, Haleh Ahmadian, Sibylle M. Lenz, Tine B. Stensbl, Ulf Madsen, Klaus P. Bges, and Povl Krogsgaard-Larsen [Full Article - PDF]

BRIEF ARTICLES

4919-4922

Synthesis of Apicidin-Derived Quinolone Derivatives: Parasite-Selective Histone Deacetylase Inhibitors and Antiproliferative Agents Peter T. Meinke, Steven L. Colletti, George Doss, Robert W. Myers, Anne M. Gurnett, Paula M. Dulski, Sandra J. Darkin-Rattray, John J. Allocco, Stefan Galuska, Dennis M. Schmatz, Matthew J. Wyvratt, and Michael H. Fisher [Full Article - PDF]