Journal of Medicinal Chemistry
Volume 43, Issue 23 (November 16, 2000)
Copyright © 2000 American Chemical Society

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PERSPECTIVES

4333-4353

Therapeutic Opportunities for Muscarinic Receptors in the Central Nervous System Christian C. Felder, Frank P. Bymaster, John Ward, and Neil DeLapp [Full Article - PDF]

4354-4358

Biarylpropylsulfonamides as Novel, Potent Potentiators of 2-Amino-3- (5-methyl-3-hydroxyisoxazol-4-yl)- propanoic Acid (AMPA) Receptors Paul L. Ornstein, Dennis M. Zimmerman, M. Brian Arnold, Thomas J. Bleisch, Buddy Cantrell, Richard Simon, Hamideh Zarrinmayeh, S. Richard Baker, Mary Gates, Joseph P. Tizzano, and David Bleakman , Allan Mandelzys, Kieth R. Jarvie, Ken Ho, Michelle Deverill, and Rajender K. Kamboj [Full Article - PDF]

4359-4362

Design, Radiosynthesis, and Biodistribution of a New Potent and Selective Ligand for in Vivo Imaging of the Adenosine A2A Receptor System Using Positron Emission Tomography Sergio Todde, Rosa Maria Moresco, Pasquale Simonelli, Pier Giovanni Baraldi, Barbara Cacciari, Giampiero Spalluto, Katia Varani, Angela Monopoli, Mario Matarrese, Assunta Carpinelli, Fulvio Magni, Marzia Galli Kienle, and Ferruccio Fazio [Full Article - PDF]

4363-4366

5-[1'-(2'-N-Arylsulfonyl-1',2',3',4'-tetrahydroisoquinolyl)]-4,5-dihydro-2(3H)-furanones: Positive Allosteric Modulators of the GABAA Receptor with a New Mode of Action Rodolphe Razet, Urs Thomet, Roman Furtmüller, Angèle Chiaroni, Erwin Sigel, Werner Sieghart, and Robert H. Dodd [Full Article - PDF]

4367-4369

Increased DNA Binding Specificity for Antitumor Ecteinascidin 743 through Protein-DNA Interactions? Raquel García-Nieto, Ignacio Manzanares, Carmen Cuevas, and Federico Gago [Full Article - PDF]

EXPEDITED ARTICLES

4370-4376

Structure-Function Studies on the New Growth Hormone-Releasing Peptide, Ghrelin: Minimal Sequence of Ghrelin Necessary for Activation of Growth Hormone Secretagogue Receptor 1a Maria A. Bednarek, Scott D. Feighner, Sheng-Shung Pong, Karen Kulju McKee, Donna L. Hreniuk, Maria V. Silva, Vivien A. Warren, Andrew D. Howard, Lex H. Y. Van der Ploeg, and James V. Heck [Full Article - PDF]

4377-4387

Reduction-Sensitive Lipopolyamines as a Novel Nonviral Gene Delivery System for Modulated Release of DNA with Improved Transgene Expression Gerardo Byk, Barbara Wetzer, Marc Frederic, Catherine Dubertret, Bruno Pitard, Gabrielle Jaslin, and Daniel Scherman [Full Article - PDF]

ARTICLES

4388-4397

Novel Design of Nonpeptide AVP V2 Receptor Agonists: Structural Requirements for an Agonist Having 1-(4-Aminobenzoyl)-2,3,4,5-tetrahydro-1H-1-benzazepine as a Template Kazumi Kondo, Hidenori Ogawa, Tomoichi Shinohara, Muneaki Kurimura, Yoshihisa Tanada, Keizo Kan, Hiroshi Yamashita, Shigeki Nakamura, Takahiro Hirano, Yoshitaka Yamamura, Toyoki Mori, Michiaki Tominaga, and Akiko Itai [Full Article - PDF]

4398-4415

Design, Synthesis, and Biological Evaluation of Potent and Selective Amidino Bicyclic Factor Xa Inhibitors Qi Han, Celia Dominguez, Pieter F. W. Stouten, Jeongsook M. Park, Daniel E. Duffy, Robert A. Galemmo, Jr., Karen A. Rossi, Richard S. Alexander, Angela M. Smallwood, Pancras C. Wong, Matthew M. Wright, Joseph M. Luettgen, Robert M. Knabb, and Ruth R. Wexler [Full Article - PDF]

4416-4427

Multiple-Conformation and Protonation-State Representation in 4D-QSAR: The Neurokinin-1 Receptor System Angelo Vedani, Hans Briem, Max Dobler, Horst Dollinger, and Daniel R. McMasters [Full Article - PDF]

4428-4436

Chiral Resolution, Pharmacological Characterization, and Receptor Docking of the Noncompetitive mGlu1 Receptor Antagonist (±)-2-Hydroxyimino- 1a,2-dihydro-1H-7-oxacyclopropa[b]naphthalene-7a-carboxylic Acid Ethyl Ester David Ott, Philipp Floersheim, Werner Inderbitzin, Natacha Stoehr, Eric Francotte, Gabrielle Lecis, Paul Richert, Grety Rihs, Peter Josef Flor, Rainer Kuhn, and Fabrizio Gasparini [Full Article - PDF]

4437-4445

Synthesis and Evaluation of 17-Aliphatic Heterocycle-Substituted Steroidal Inhibitors of 17-Hydroxylase/C17-20-Lyase (P450 17) Rolf W. Hartmann, Markus Hector, Bertil G. Wachall, Anja Palusczak, Martina Palzer, Volker Huch, and Michael Veith [Full Article - PDF]

4446-4451

Computational Studies on HIV-1 Protease Inhibitors: Influence of Calculated Inhibitor-Enzyme Binding Affinities on the Statistical Quality of 3D-QSAR CoMFA Models Philippa R. N. Jayatilleke, Anil C. Nair, Randy Zauhar, and William J. Welsh [Full Article - PDF]

4452-4464

Design and Synthesis of Pyrrolidine-5,5-trans-lactams (5-Oxo-hexahydro-pyrrolo[3,2-b]pyrroles) as Novel Mechanism-Based Inhibitors of Human Cytomegalovirus Protease. 1. The -Methyl-trans-lactam Template Alan D. Borthwick, S. Jane Angier, Andrew J. Crame, Anne M. Exall, Terry M. Haley, Graham J. Hart, Andrew M. Mason, Andrew M. K. Pennell, and Gordon G. Weingarten [Full Article - PDF]

4465-4478

Structure-Activity Relationships of 17-Derivatives of Estradiol as Inhibitors of Steroid Sulfatase Roch P. Boivin, Van Luu-The, Roger Lachance, Fernand Labrie, and Donald Poirier [Full Article - PDF]

4479-4487

6-Alkylamino- and 2,3-Dihydro-3'-methoxy-2-phenyl-4-quinazolinones and Related Compounds: Their Synthesis, Cytotoxicity, and Inhibition of Tubulin Polymerization Mann-Jen Hour, Li-Jiau Huang, Sheng-Chu Kuo, Yi Xia, Kenneth Bastow, Yuka Nakanishi, Ernest Hamel, and Kuo-Hsiung Lee [Full Article - PDF]

4488-4498

A Selenopyrylium Photosensitizer for Photodynamic Therapy Related in Structure to the Antitumor Agent AA1 with Potent in Vivo Activity and No Long-Term Skin Photosensitization Kristi A. Leonard, Jonathan P. Hall, Marina I. Nelen, Sherry R. Davies, Sandra O. Gollnick, Sue Camacho, Allan R. Oseroff, Scott L. Gibson, Russell Hilf, and Michael R. Detty [Full Article - PDF]

4499-4507

Molecular Simplification of 1,4-Diazabicyclo[4.3.0]nonan-9-ones Gives Piperazine Derivatives That Maintain High Nootropic Activity Dina Manetti, Carla Ghelardini, Alessandro Bartolini, Silvia Dei, Nicoletta Galeotti, Fulvio Gualtieri, Maria Novella Romanelli, and Elisabetta Teodori [Full Article - PDF]

4508-4515

Exploring the Structural Basis of Neurotoxicity in C17-Polyacetylenes Isolated from Water Hemlock Koji Uwai, Katsuyo Ohashi, Yoshiaki Takaya, Tomihisa Ohta, Takeshi Tadano, Kensuke Kisara, Koichi Shibusawa, Ryoji Sakakibara, and Yoshiteru Oshima [Full Article - PDF]

4516-4525

Syntheses of 4'-C-Ethynyl--D-arabino- and 4'-C-Ethynyl-2'-deoxy--D-ribo-pentofuranosylpyrimidines and -purines and Evaluation of Their Anti-HIV Activity Hiroshi Ohrui, Satoru Kohgo, Kenji Kitano, Shinji Sakata, Eiichi Kodama, Kazuhisa Yoshimura, Masao Matsuoka, Shiro Shigeta, and Hiroaki Mitsuya [Full Article - PDF]

4526-4533

Solid-Phase Synthesis and Biological Evaluation of a Combinatorial Library of Philanthotoxin Analogues Kristian Strmgaard, Tim J. Brier, Kim Andersen, Ian R. Mellor, Alex Saghyan, Denis Tikhonov, Peter N. R. Usherwood, Povl Krogsgaard-Larsen, and Jerzy W. Jaroszewski [Full Article - PDF]

4534-4541

Classification of Multidrug-Resistance Reversal Agents Using Structure-Based Descriptors and Linear Discriminant Analysis Gregory A. Bakken and Peter C. Jurs [Full Article - PDF]

4542-4551

Carbonic Anhydrase Inhibitors: Perfluoroalkyl/Aryl-Substituted Derivatives of Aromatic/Heterocyclic Sulfonamides as Topical Intraocular Pressure-Lowering Agents with Prolonged Duration of Action Andrea Scozzafava, Luca Menabuoni, Francesco Mincione, Fabrizio Briganti, Giovanna Mincione, and Claudiu T. Supuran [Full Article - PDF]

4552-4562

Synthesis, 18F-Labeling, and Biological Evaluation of Piperidyl and Pyrrolidyl Benzilates as in Vivo Ligands for Muscarinic Acetylcholine Receptors Marc B. Skaddan, Michael R. Kilbourn, Scott E. Snyder, Phil S. Sherman, Tim J. Desmond, and Kirk A. Frey [Full Article - PDF]

BRIEF ARTICLES

4563-4569

Cyanoindole Derivatives as Highly Selective Dopamine D4 Receptor Partial Agonists: Solid-Phase Synthesis, Binding Assays, and Functional Experiments Harald Hübner, Johannes Kraxner, and Peter Gmeiner [Full Article - PDF]

4570-4574

S-Acyl-2-thioethyl Aryl Phosphotriester Derivatives as Mononucleotide Prodrugs Nathalie Schlienger, Suzanne Peyrottes, Tarek Kassem, Jean-Louis Imbach, Gilles Gosselin, Anne-Marie Aubertin, and Christian Périgaud [Full Article - PDF]