Journal of Medicinal Chemistry
Volume 43, Issue 11 (June 1, 2000)
Copyright © 2000 American Chemical Society

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COMMUNICATIONS

2083-2086

SPR Biosensor Studies of the Direct Interaction between 27 Drugs and a Liposome Surface: Correlation with Fraction Absorbed in Humans Ernest Danelian, Anders Karlén, Robert Karlsson, Susanne Winiwarter, Anna Hansson, Stefan Löfås, Hans Lennernäs, and Markku D. Hämäläinen [Full Article - PDF]

2087-2092

Non-Amidine-Containing 1,2-Dibenzamidobenzene Inhibitors of Human Factor Xa with Potent Anticoagulant and Antithrombotic Activity John J. Masters, Jeffry B. Franciskovich, Jennifer M. Tinsley, Charles Campbell, Jack B. Campbell, Trelia J. Craft, Larry L. Froelich, Donetta S. Gifford-Moore, Lynne A. Hay, David K. Herron, Valentine J. Klimkowski, Kenneth D. Kurz, James T. Metz, Andrew M. Ratz, Robert T. Shuman, Gerald F. Smith, Tommy Smith, Richard D. Towner, Michael R. Wiley, Alex Wilson, and Ying K. Yee [Full Article - PDF]

ARTICLES

2093-2099

Mapping the Active Site of Angiotensin-Converting Enzyme by Transferred NOE Spectroscopy Moriz Mayer and Bernd Meyer [Full Article - PDF]

2100-2114

Developing a Dynamic Pharmacophore Model for HIV-1 Integrase Heather A. Carlson, Kevin M. Masukawa, Kathleen Rubins, Fredric D. Bushman, William L. Jorgensen, Roberto D. Lins, James M. Briggs, and J. Andrew McCammon [Full Article - PDF]

2115-2123

Synthesis, Molecular Modeling, and Opioid Receptor Affinity of 9,10-Diazatricyclo[4.2.1.12,5]decanes and 2,7-Diazatricyclo[4.4.0.03,8]decanes Structurally Related to 3,8-Diazabicyclo[3.2.1]octanes Paola Vianello, Alberto Albinati, Gerardo A. Pinna, Antonio Lavecchia, Luciana Marinelli, Pier Andrea Borea, Stefania Gessi, Paola Fadda, Silvia Tronci, and Giorgio Cignarella [Full Article - PDF]

2124-2134

Modeling of -Opioid Receptor/Agonists Interactions Using Pharmacophore-Based and Docking Simulations Antonio Lavecchia, Giovanni Greco, Ettore Novellino, Franco Vittorio, and Giuseppe Ronsisvalle [Full Article - PDF]

2135-2148

Peptide and Peptide Mimetic Inhibitors of Antigen Presentation by HLA-DR Class II MHC Molecules. Design, Structure-Activity Relationships, and X-ray Crystal Structures David R. Bolin, Amy L. Swain, Ramakanth Sarabu, Steven J. Berthel, Paul Gillespie, Nicholas J. S. Huby, Raymond Makofske, Lucja Orzechowski, Agostino Perrotta, Katherine Toth, Joel P. Cooper, Nan Jiang, Fiorenza Falcioni, Robert Campbell, Donald Cox, Diana Gaizband, Charles J. Belunis, Damir Vidovic, Kouichi Ito, Robert Crowther, Ursula Kammlott, Xiaolei Zhang, Robert Palermo, David Weber, Jeanmarie Guenot, Zoltan Nagy, and Gary L. Olson [Full Article - PDF]

2149-2154

Structure-Activity Relationships in Platelet-Activating Factor (PAF). 10. From PAF Antagonism to Inhibition of HIV-1 Replication Nawal Serradji, Okkacha Bensaid, Marc Martin, Erwan Kan, Nathalie Dereuddre-Bosquet, Catherine Redeuilh, Jack Huet, Françoise Heymans, Aazdine Lamouri, Pascal Clayette, Chang Zhi Dong, Dominique Dormont, and Jean-Jacques Godfroid [Full Article - PDF]

2155-2164

Structure-Activity Relationships in a Series of Bisquaternary Bisphthalimidine Derivatives Modulating the Muscarinic M2-Receptor Allosterically Hector M. Botero Cid, Christian Tränkle, Knut Baumann, Rainer Pick, Elisabeth Mies-Klomfass, Evi Kostenis, Klaus Mohr, and Ulrike Holzgrabe [Full Article - PDF]

2165-2175

Synthesis, Structure, and Neuroprotective Properties of Novel Imidazolyl Nitrones Alain Dhainaut, André Tizot, Eric Raimbaud, Brian Lockhart, Pierre Lestage, and Solo Goldstein [Full Article - PDF]

2176-2182

Population, Acid-Base, and Redox Properties of N-Acetylcysteine Conformers Béla Noszál, Dóra Visky, and Márta Kraszni [Full Article - PDF]

2183-2195

Design, Synthesis, and Structure-Activity Relationships of Phthalimide-Phenylpiperazines: A Novel Series of Potent and Selective 1a-Adrenergic Receptor Antagonists Gee-Hong Kuo, Catherine Prouty, William V. Murray, Virginia Pulito, Linda Jolliffe, Peter Cheung, Sally Varga, Mary Evangelisto, and Jian Wang [Full Article - PDF]

2196-2203

Methanocarba Analogues of Purine Nucleosides as Potent and Selective Adenosine Receptor Agonists Kenneth A. Jacobson, Xiao-duo Ji, An-Hu Li, Neli Melman, Maqbool A. Siddiqui, Kye-Jung Shin, Victor E. Marquez, and R. Gnana Ravi [Full Article - PDF]

2204-2216

Predicting Blood-Brain Barrier Permeation from Three-Dimensional Molecular Structure Patrizia Crivori, Gabriele Cruciani, Pierre-Alain Carrupt, and Bernard Testa [Full Article - PDF]

2217-2226

Novel Potent Ligands for the Central Nicotinic Acetylcholine Receptor: Synthesis, Receptor Binding, and 3D-QSAR Analysis Simon Feldbæk Nielsen, Elsebet Østergaard Nielsen, Gunnar M. Olsen, Tommy Liljefors, and Dan Peters [Full Article - PDF]

2227-2238

Isoquinoline and Quinazoline Urea Analogues as Antagonists for the Human Adenosine A3 Receptor Jacqueline E. van Muijlwijk-Koezen, Henk Timmerman, Henk van der Goot, Wiro M. P. B. Menge, Jacobien Frijtag von Drabbe Künzel, Miriam de Groote, and Adriaan P. IJzerman [Full Article - PDF]

2239-2247

Novel Inhibitors of Nucleoside Triphosphate Diphosphohydrolases: Chemical Synthesis and Biochemical and Pharmacological Characterizations Fernand-Pierre Gendron, Efrat Halbfinger, Bilha Fischer, Martine Duval, Pédro D'Orléans-Juste, and Adrien R. Beaudoin [Full Article - PDF]

2248-2257

Anilides of (R)-Trifluoro-2-hydroxy-2-methylpropionic Acid as Inhibitors of Pyruvate Dehydrogenase Kinase Gregory R. Bebernitz,,1 Thomas D. Aicher,,1,2 James L. Stanton, Jiaping Gao,3 Suraj S. Shetty,3 Douglas C. Knorr,1 Robert J. Strohschein,1 Jennifer Tan,1 Leonard J. Brand,1 Charles Liu,1 Wei H. Wang,1 Christine C. Vinluan,4 Emma L. Kaplan,4 Carol J. Dragland,4 Dominick DelGrande,3 Amin Islam,3 Robert J. Lozito,3 Xilin Liu,3 Wieslawa M. Maniara, and William R. Mann4 [Full Article - PDF]

2258-2265

Synthesis and Evaluation of Nitroheterocyclic Phosphoramidates as Hypoxia-Selective Alkylating Agents Richard F. Borch, Jiwen Liu, James P. Schmidt, Joseph T. Marakovits, Carolyn Joswig, Jerry J. Gipp, and R. Timothy Mulcahy [Full Article - PDF]

2266-2274

Synthesis, in Vitro Anti-Breast Cancer Activity, and Intracellular Decomposition of Amino Acid Methyl Ester and Alkyl Amide Phosphoramidate Monoesters of 3'-Azido-3'-deoxythymidine (AZT) Vidhya V. Iyer, George W. Griesgraber, Matthew R. Radmer, Edward J. McIntee, and Carston R. Wagner [Full Article - PDF]

BRIEF ARTICLES

2275-2279

Quinolones: Novel Probes in Antifilarial Chemotheraphy Sanjay K. Srivastava, Prem M. S. Chauhan, Amiya P. Bhaduri, Nigar Fatima, and Ranjit K. Chatterjee [Full Article - PDF]

2280-2284

Modeling Cyclooxygenase Inhibition. Implication of Active Site Hydration on the Selectivity of Ketoprofen Analogues Albert Palomer, Juan J. Pérez, Susana Navea, Oriol Llorens, Jaume Pascual, Lluïsa García, and David Mauleón [Full Article - PDF]

2285-2289

Topoisomerase I-Mediated Antiproliferative Activity of Enantiomerically Pure Fluorinated Homocamptothecins Olivier Lavergne, Danièle Demarquay, Christian Bailly, Christophe Lanco, Alain Rolland, Marion Huchet, Helène Coulomb, Nicole Muller, Nicole Baroggi, José Camara, Christine Le Breton, Eric Manginot, Jean-Bernard Cazaux, and Dennis C. H. Bigg [Full Article - PDF]

BOOK REVIEWS

2290-2291

Reviews in Computational Chemistry. Volume 13 Edited by Kenny B. Lipkowitz and Donald B. Boyd. Wiley-VCH, New York. 1999. xxxiii + 426 pp. 16 × 24 cm. ISBN 0471-33135-X. $135.00. Peter A. Kollman [Full Article - PDF]

2291-2291

Second Supplements to the Second Edition of Rodd's Chemitry of Carbon Compounds. Volume IV: Heterocyclic Compounds. Part I. Six-membered Heterocyclic Compounds with Two Hetero-Atoms from Group V of the Periodic Table: the Pyridazine and Pyrimidine Groups. Part J. Six-membered Heterocyclic Compounds with Two Hetero-Atoms from Group V of the Periodic Table: the Pyrazine Group, Phenoxazine, Phenothiazine, Phenazine and Sulphur Dyes. Six-membered Heterocyclic Compounds with Three or More Hetero-Atoms Edited by M. Sainsbury. Elsevier, Amsterdam. 2000. xiv + 299 pp. 15 × 23 cm. ISBN-0-444-82980-6. $183.50. Arnold Martin [Full Article - PDF]

2291-2292

Potassium Ion Channels: Molecular Structure, Function and Diseases Edited by Yoshihisa Kurachi, Lily Yeh Jan, and Michel Lazdunzki. Academic Press, San Diego, CA. 1999. xxiv + 492 pp. 15 × 22 cm. ISBN 0-12-153346-8. $99.95. Murali Gopalakrishnan [Full Article - PDF]