Journal of Medicinal Chemistry
Volume 42, Issue 7 (April 8, 1999)
Copyright © 1999 American Chemical Society

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ARTICLES

1115-1122

Characterization of the Binding Site of the Histamine H3 Receptor. 1. Various Approaches to the Synthesis of 2-(1H-Imidazol-4-yl)cyclopropylamine and Histaminergic Activity of (1R,2R)- and (1S,2S)-2-(1H-Imidazol-4-yl)- cyclopropylamine Iwan J. P. De Esch, Roeland C. Vollinga, Kees Goubitz, Henk Schenk, Ulf Appelberg, Uli Hacksell, Sylvia Lemstra, Obbe P. Zuiderveld, Marcel Hoffmann, Rob Leurs, Wiro M. P. B. Menge, and Henk Timmerman [Full Article - PDF]

1123-1144

Piperazine Imidazo[1,5-a]quinoxaline Ureas as High-Affinity GABAA Ligands of Dual Functionality E. Jon Jacobsen, Lindsay S. Stelzer, Ruth E. TenBrink, Kenneth L. Belonga, Donald B. Carter, Haesook K. Im, Wha Bin Im, Vimala H. Sethy, Andy H. Tang, Philip F. VonVoigtlander, James D. Petke, Wei-Zhu Zhong, and John W. Mickelson [Full Article - PDF]

1145-1150

Novel Potential Agents for Human Cytomegalovirus Infection: Synthesis and Antiviral Activity Evaluation of Benzothiadiazine Dioxide Acyclonucleosides Ana Martinez, Ana I. Esteban, Ana Castro, Carmen Gil, Santiago Conde, Graciela Andrei, Robert Snoeck, Jan Balzarini, and Erik De Clercq [Full Article - PDF]

1151-1160

Synthesis, Structure-Activity Relationships, and in Vivo Evaluations of Substituted Di-tert-butylphenols as a Novel Class of Potent, Selective, and Orally Active Cyclooxygenase-2 Inhibitors. 1. Thiazolone and Oxazolone Series Yuntao Song, David T. Connor, Robert Doubleday, Roderick J. Sorenson, Anthony D. Sercel, Paul C. Unangst, Bruce D. Roth, Richard B. Gilbertsen, Kam Chan, Denis J. Schrier, Antonio Guglietta, Dirk A. Bornemeier, and Richard D. Dyer [Full Article - PDF]

1161-1169

Synthesis, Structure-Activity Relationships, and in Vivo Evaluations of Substituted Di-tert-butylphenols as a Novel Class of Potent, Selective, and Orally Active Cyclooxygenase-2 Inhibitors. 2. 1,3,4- and 1,2,4-Thiadiazole Series Yuntao Song, David T. Connor, Anthony D. Sercel, Roderick J. Sorenson, Robert Doubleday, Paul C. Unangst, Bruce D. Roth, Vlad G. Beylin, Richard B. Gilbertsen, Kam Chan, Denis J. Schrier, Antonio Guglietta, Dirk A. Bornemeier, and Richard D. Dyer [Full Article - PDF]

1170-1177

Design and Synthesis of a Potent Cyclic Analogue of the Myelin Basic Protein Epitope MBP72-85: Importance of the Ala81 Carboxyl Group and of a Cyclic Conformation for Induction of Experimental Allergic Encephalomyelitis Theodore Tselios, Lesley Probert, Ioanna Daliani, Elizabeth Matsoukas, Anastasios Troganis, Ioannis P. Gerothanassis, Thomas Mavromoustakos, Graham J. Moore, and John M. Matsoukas [Full Article - PDF]

1178-1192

Orally Active Isoxazoline Glycoprotein IIb/IIIa Antagonists with Extended Duration of Action Richard E. Olson, Thais M. Sielecki, John Wityak, Donald J. Pinto, Douglas G. Batt, William E. Frietze, Jie Liu, A. Ewa Tobin, Michael J. Orwat, Susan V. Di Meo, Gregory C. Houghton, George K. Lalka, Shaker A. Mousa, Adrienne L. Racanelli, Elizabeth A. Hausner, Ram P. Kapil, Shelley R. Rabel, Martin J. Thoolen, Thomas M. Reilly, Paul S. Anderson, and Ruth R. Wexler [Full Article - PDF]

1193-1202

Synthesis and in Vitro Pharmacology of a Series of New Chiral Histamine H3-Receptor Ligands: 2-(R and S)-Amino-3-(1H-imidazol-4(5)-yl)propyl Ether Derivatives Jari T. Kovalainen, Johannes A. M. Christiaans, Sanna Kotisaari, Jarmo T. Laitinen, Pekka T. Männistö, Leena Tuomisto, and Jukka Gynther [Full Article - PDF]

1203-1212

Structure-Based Design, Synthesis, and Biological Evaluation of Irreversible Human Rhinovirus 3C Protease Inhibitors. 3. Structure-Activity Studies of Ketomethylene-Containing Peptidomimetics Peter S. Dragovich, Thomas J. Prins, Ru Zhou, Shella A. Fuhrman, Amy K. Patick, David A. Matthews, Clifford E. Ford, James W. Meador III, Rose Ann Ferre, and Stephen T. Worland [Full Article - PDF]

1213-1224

Structure-Based Design, Synthesis, and Biological Evaluation of Irreversible Human Rhinovirus 3C Protease Inhibitors. 4. Incorporation of P1 Lactam Moieties as L-Glutamine Replacements Peter S. Dragovich, Thomas J. Prins, Ru Zhou, Stephen E. Webber, Joseph T. Marakovits, Shella A. Fuhrman, Amy K. Patick, David A. Matthews, Caroline A. Lee, Clifford E. Ford, Benjamin J. Burke, Paul A. Rejto, Thomas F. Hendrickson, Tove Tuntland, Edward L. Brown, James W. Meador III, Rose Ann Ferre, James E. V. Harr, Maha B. Kosa, and Stephen T. Worland [Full Article - PDF]

1225-1234

Binding Preferences of Hydroxamate Inhibitors of the Matrix Metalloproteinase Human Fibroblast Collagenase Samuel Toba, K. V. Damodaran, and Kenneth M. Merz, Jr. [Full Article - PDF]

1235-1249

Guanidine Derivatives as Combined Thromboxane A2 Receptor Antagonists and Synthase Inhibitors Rainer Soyka, Brian D. Guth, Hans M. Weisenberger, Peter Luger, and Thomas H. Müller [Full Article - PDF]

1250-1261

Docking of Cationic Antibiotics to Negatively Charged Pockets in RNA Folds Thomas Hermann and Eric Westhof [Full Article - PDF]

1262-1273

Enzyme-Assisted Total Synthesis of the Optical Antipodes D-myo-Inositol 3,4,5-Trisphosphate and D-myo-Inositol 1,5,6-Trisphosphate: Aspects of Their Structure-Activity Relationship to Biologically Active Inositol Phosphates Stephan Adelt, Oliver Plettenburg, Rolf Stricker, Georg Reiser, Hans-Josef Altenbach, and Günter Vogel [Full Article - PDF]

1274-1281

2,3-Diarylcyclopentenones as Orally Active, Highly Selective Cyclooxygenase-2 Inhibitors W. Cameron Black, Christine Brideau, Chi-Chung Chan, Stella Charleson, Nathalie Chauret, David Claveau, Diane Ethier, Robert Gordon, Gillian Greig, Jocelyne Guay, Gregory Hughes, Paule Jolicoeur, Yves Leblanc, Deborah Nicoll-Griffith, Nathalie Ouimet, Denis Riendeau, Denise Visco, Zhaoyin Wang, Lijing Xu, and Petpiboon Prasit [Full Article - PDF]

1282-1292

Synthesis and Biological Evaluation of Boron-Containing Polyamines as Potential Agents for Neutron Capture Therapy of Brain Tumors Jin-Cong Zhuo, Jianping Cai, Albert H. Soloway, Rolf F. Barth, Dianne M. Adams, Weihua Ji, and Werner Tjarks [Full Article - PDF]

1293-1305

1-Arylnaphthalene Lignan: A Novel Scaffold for Type 5 Phosphodiesterase Inhibitor Tatsuzo Ukita, Yoshinori Nakamura, Akira Kubo, Yasuo Yamamoto, Masami Takahashi, Jun Kotera, and Tomohiro Ikeo [Full Article - PDF]

1306-1311

Quinuclidine Inhibitors of 2,3-Oxidosqualene Cyclase-Lanosterol Synthase: Optimization from Lipid Profiles George R. Brown, David M. Hollinshead, Elaine S. E. Stokes, David S. Clarke, M. Allan Eakin, Alan J. Foubister, Steven C. Glossop, David Griffiths, Michael C. Johnson, Fergus McTaggart, Donald J. Mirrlees, Graham J. Smith, and Robin Wood [Full Article - PDF]

1312-1319

Fluorescent Pseudo-Peptide Linear Vasopressin Antagonists: Design, Synthesis, and Applications Thierry Durroux, Marion Peter, Gerardo Turcatti, André Chollet, Marie-Noëlle Balestre, Claude Barberis, and René Seyer [Full Article - PDF]

1320-1328

Synthesis and Anti-HIV and Anti-HBV Activities of 2'-Fluoro-2',3'-unsaturated L-Nucleosides Kyeong Lee, Yongseok Choi, Elizabeth Gullen, Susan Schlueter-Wirtz, Raymond F. Schinazi, Yung-Chi Cheng, and Chung K. Chu [Full Article - PDF]