Journal of Medicinal Chemistry
Volume 42, Issue 12 (June 17, 1999)
Copyright © 1999 American Chemical Society

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2063-2063

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ANNOUNCEMENTS

ARTICLES

2064-2086

Structure-Antiviral Activity Relationship in the Series of Pyrimidine and Purine N-[2-(2-Phosphonomethoxy)ethyl] Nucleotide Analogues. 1. Derivatives Substituted at the Carbon Atoms of the Base Antonín Hol, Jaroslav Günter, Hana Dvoáková, Milena Masojídková, Graciela Andrei, Robert Snoeck, Jan Balzarini, and Erik De Clercq [Full Article - PDF]

2087-2104

Fluorination of 3-(3-(Piperidin-1-yl)propyl)indoles and 3-(3-(Piperazin-1-yl)propyl)indoles Gives Selective Human 5-HT1D Receptor Ligands with Improved Pharmacokinetic Profiles Monique B. van Niel, Ian Collins, Margaret S. Beer, Howard B. Broughton, Susan K. F. Cheng, Simon C. Goodacre, Anne Heald, Karen L. Locker, Angus M. MacLeod, Denise Morrison, Christopher R. Moyes, Desmond O'Connor, Andrew Pike, Michael Rowley, Michael G. N. Russell, Balbinder Sohal, Josephine A. Stanton, Steven Thomas, Hugh Verrier, Alan P. Watt, and José L. Castro [Full Article - PDF]

2105-2111

A Peptide Agonist Acts by Occupation of a Monomeric G Protein-Coupled Receptor: Dual Sites of Covalent Attachment to Domains Near TM1 and TM7 of the Same Molecule Make Biologically Significant Domain-Swapped Dimerization Unlikely Elizabeth M. Hadac, Zongshi Ji, Delia I. Pinon, Randal M. Henne, Terry P. Lybrand, and Laurence J. Miller [Full Article - PDF]

2112-2124

Phthalein Derivatives as a New Tool for Selectivity in Thymidylate Synthase Inhibition Paola M. Costi, Marcella Rinaldi, Donatella Tondi, Piergiorgio Pecorari, Daniela Barlocco, Stefano Ghelli, Robert M. Stroud, Daniel V. Santi, Thomas J. Stout, Chiara Musiu, Elena M. Marangiu, Alessandra Pani, Donatella Congiu, Giulia A. Loi, and Paolo La Colla [Full Article - PDF]

2125-2135

Tricyclic Farnesyl Protein Transferase Inhibitors: Crystallographic and Calorimetric Studies of Structure-Activity Relationships Corey L. Strickland, Patricia C. Weber, William T. Windsor, Zhen Wu, Hung V. Le, Margaret M. Albanese, Carmen S. Alvarez, David Cesarz, Joycelyn del Rosario, Jeffrey Deskus, Alan K. Mallams, F. George Njoroge, John J. Piwinski, Stacy Remiszewski, Randall R. Rossman, Arthur G. Taveras, Bancha Vibulbhan, Ronald J. Doll, Viyyoor M. Girijavallabhan, and Ashit K. Ganguly [Full Article - PDF]

2136-2144

Design and Synthesis of Modified Quinolones as Antitumoral Acridones Oriana Tabarrini, Violetta Cecchetti, Arnaldo Fravolini, Giuseppe Nocentini, A. Barzi, Stefano Sabatini, Hua Miao, and Claudia Sissi [Full Article - PDF]

2145-2161

Novel Multidrug Resistance Reversal Agents Dan Berger, Ron Citarella, Minu Dutia, Lee Greenberger, William Hallett, Rolf Paul, and Dennis Powell [Full Article - PDF]

2162-2168

Butenolide Endothelin Antagonists with Improved Aqueous Solubility William C. Patt, Xue-Min Cheng, Joseph T. Repine, Chet Lee, Bill R. Reisdorph, Mark A. Massa, Annette M. Doherty, Kathleen M. Welch, John W. Bryant, Michael A. Flynn, Donnelle M. Walker, Richard L. Schroeder, Stephen J. Haleen, and Joan A. Keiser [Full Article - PDF]

2169-2179

Prediction of Ligand-Receptor Binding Thermodynamics by Free Energy Force Field Three-Dimensional Quantitative Structure-Activity Relationship Analysis: Applications to a Set of Glucose Analogue Inhibitors of Glycogen Phosphorylase Prabha Venkatarangan and Anton J. Hopfinger [Full Article - PDF]

2180-2190

Design and Synthesis of Potent, Selective, and Orally Bioavailable Tetrasubstituted Imidazole Inhibitors of p38 Mitogen-Activated Protein Kinase Nigel J. Liverton, John W. Butcher, Christopher F. Claiborne, David A. Claremon, Brian E. Libby, Kevin T. Nguyen, Steven M. Pitzenberger, Harold G. Selnick, Garry R. Smith, Andrew Tebben, Joseph P. Vacca, Sandor L. Varga, Lily Agarwal, Kim Dancheck, Amy J. Forsyth, Daniel S. Fletcher, Betsy Frantz, William A. Hanlon, Coral F. Harper, Scott J. Hofsess, Matthew Kostura, Jiunn Lin, Sylvie Luell, Edward A. O'Neill, Chad J. Orevillo, Margaret Pang, Janey Parsons, Anna Rolando, Yousif Sahly, Denise M. Visco, and Stephen J. O'Keefe [Full Article - PDF]

2191-2203

Synthesis of 9-O-Substituted Derivatives of 9-Hydroxy-5,6-dimethyl-6H- pyrido[4,3-b]carbazole-1-carboxylic Acid (2-(Dimethylamino)ethyl)amide and Their 10- and 11-Methyl Analogues with Improved Antitumor Activity Claude Guillonneau, Alain Pierré, Yves Charton, Nicolas Guilbaud, Laurence Kraus-Berthier, Stéphane Léonce, André Michel, Emile Bisagni, and Ghanem Atassi [Full Article - PDF]

2204-2211

Stereoselective Characterization of the 1,4-Dihydropyridine Binding Site at L-Type Calcium Channels in the Resting State and the Opened/Inactivated State Klaus-Jürgen Schleifer [Full Article - PDF]

2212-2217

Structure-Activity Relationships of L-Dioxolane Uracil Nucleosides as Anti-Epstein Barr Virus Agents Ju-Sheng Lin, Toshihiko Kira, Elizabeth Gullen, Yongseok Choi, Fucheng Qu, Chung K. Chu, and Yung-Chi Cheng [Full Article - PDF]

2218-2226

Benzodiazepine Receptor Ligands. 4. Synthesis and Pharmacological Evaluation of 3-Heteroaryl-8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-Oxides Annarella Costanzo, Gabriella Guerrini, Giovanna Ciciani, Fabrizio Bruni, Silvia Selleri, Barbara Costa, Claudia Martini, Antonio Lucacchini, Petra Malmberg Aiello, and Alessandra Ipponi [Full Article - PDF]

2227-2234

Novel and Potent 6-Chloro-3-pyridinyl Ligands for the 42 Neuronal Nicotinic Acetylcholine Receptor Bachir Latli, Kevin D'Amour, and John E. Casida [Full Article - PDF]

2235-2244

New (Sulfonyloxy)piperazinyldibenzazepines as Potential Atypical Antipsychotics: Chemistry and Pharmacological Evaluation Yi Liao, Bastiaan J. Venhuis, Nienke Rodenhuis, Wia Timmerman, and Håkan Wikström , Eddie Meier , Gerd D. Bartoszyk, Henning Böttcher, and Christoph A. Seyfried , Staffan Sundell [Full Article - PDF]

2245-2250

Cross-Linking and Sequence-Specific Alkylation of DNA by Aziridinylquinones. 3. Effects of Alkyl Substituents Robert H. J. Hargreaves, C. Caroline O'Hare, John A. Hartley, David Ross, and John Butler [Full Article - PDF]

2251-2259

Synthesis and Nicotinic Acetylcholine Receptor in Vivo Binding Properties of 2-Fluoro-3-[2(S)-2-azetidinylmethoxy]pyridine: A New Positron Emission Tomography Ligand for Nicotinic Receptors Frédéric Dollé, Lilian Dolci, Héric Valette, Françoise Hinnen, Françoise Vaufrey, Ilonka Guenther, Chantal Fuseau, Christine Coulon, Michel Bottlaender, and Christian Crouzel [Full Article - PDF]

2260-2265

2,4-Diphenyl Furan Diamidines as Novel Anti-Pneumocystis carinii Pneumonia Agents Iris Francesconi, W. David Wilson, Farial A. Tanious, James E. Hall, Brendan C. Bender, Richard R. Tidwell, Donald McCurdy, and David W. Boykin [Full Article - PDF]

BRIEF ARTICLES

2266-2271

Design and Synthesis of Novel Quinoxaline-2,3-dione AMPA/GlyN Receptor Antagonists: Amino Acid Derivatives Sham S. Nikam, John J. Cordon, Daniel F. Ortwine, Tycho H. Heimbach, Anthony C. Blackburn, Mark G. Vartanian, Carrie B. Nelson, Roy D. Schwarz, Peter A. Boxer, and Michael F. Rafferty [Full Article - PDF]

2272-2279

Synthesis of Classical and a Nonclassical 2-Amino-4-oxo-6-methyl-5-substituted Pyrrolo[2,3-d]pyrimidine Antifolate Inhibitors of Thymidylate Synthase Aleem Gangjee,, Farahnaz Mavandadi,, Roy L. Kisliuk, and Sherry F. Queener [Full Article - PDF]

2280-2286

Potent Inhibition of Steroid Sulfatase Activity by 3-O-Sulfamate 17-Benzyl(or 4'-tert-butylbenzyl)estra-1,3,5(10)-trienes: Combination of Two Substituents at Positions C3 and C17 of Estradiol Liviu C. Ciobanu, Roch P. Boivin, Van Luu-The, Fernand Labrie, and Donald Poirier [Full Article - PDF]

2287-2294

2-Amino-4-benzyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridines: Novel Selective 3-Adrenoceptor Agonists Weiping Zheng, Victor I. Nikulin, Anish A. Konkar, Sandeep S. Vansal, Gamal Shams, Dennis R. Feller, and Duane D. Miller [Full Article - PDF]