Journal of Medicinal Chemistry
Volume 40, Issue 22 (October 24, 1997)
Copyright © 1997 American Chemical Society

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3489-3493

Dibasic Benzo[b]thiophene Derivatives as a Novel Class of Active Site-Directed Thrombin Inhibitors. 1. Determination of the Serine Protease Selectivity, Structure-Activity Relationships, and Binding Orientation Daniel J. Sall, Jolie A. Bastian, Stephen L. Briggs, John A. Buben, Nickolay Y. Chirgadze, David K. Clawson, Michael L. Denney, Deborah D. Giera, Donetta S. Gifford-Moore, Richard W. Harper, Kenneth L. Hauser, Valentine J. Klimkowski, Todd J. Kohn, Ho-Shen Lin, Jefferson R. McCowan, Alan D. Palkowitz, Gerald F. Smith, Kumiko Takeuchi, Kenneth J. Thrasher, Jennifer M. Tinsley, Barbara G. Utterback, Sau-Chi B. Yan, and Minsheng Zhang [Full Article - PDF]

3494-3496

6-Chloro-5-methyl-1-[[2-[(2-methyl-3- pyridyl)oxy]-5-pyridyl]carbamoyl]indoline (SB-242084): The First Selective and Brain Penetrant 5-HT2C Receptor Antagonist Steven M. Bromidge, Malcolm Duckworth, Ian T. Forbes, Peter Ham, Frank D. King, Kevin M. Thewlis, Frank E. Blaney, Christopher B. Naylor, Thomas P. Blackburn, Guy A. Kennett, Martyn D. Wood, and Stephen E. Clarke [Full Article - PDF]

3497-3500

3-[2-(Pyrrolidin-1-yl)ethyl]indoles and 3-[3-(Piperidin-1-yl)propyl]indoles: Agonists for the h5-HT1D Receptor with High Selectivity over the h5-HT1B Subtype José L. Castro, Leslie J. Street, Alexander R. Guiblin, Richard A. Jelley, Michael G. N. Russell, Francine Sternfeld, Margaret S. Beer, Josephine A. Stanton, and Victor G. Matassa [Full Article - PDF]

3501-3503

Selective, Orally Active 5-HT1D Receptor Agonists as Potential Antimigraine Agents Angus M. MacLeod, Leslie J. Street, Austin J. Reeve, Richard A. Jelley, Francine Sternfeld, Margaret S. Beer, Josephine A. Stanton, Alan P. Watt, Denise Rathbone, and Victor G. Matassa [Full Article - PDF]

3504-3507

Bicyclo[2.2.1]heptane and 6,6-Dimethylbicyclo[3.1.1]heptane Derivatives: Orally Active, Potent, and Selective Prostaglandin D2 Receptor Antagonists Tatsuo Tsuri, Tsunetoshi Honma, Yoshiharu Hiramatsu, Toshihiko Okada, Hiroshi Hashizume, Susumu Mitsumori, Masanao Inagaki, Akinori Arimura, Kiyoshi Yasui, Fujio Asanuma, Junji Kishino, and Mitsuaki Ohtani [Full Article - PDF]

3508-3515

Preparation, Characterization, DNA Binding, and in Vitro Cytotoxicity of the Enantiomers of the Platinum(II) Complexes N-Methyl-, N-Ethyl- and N,N-Dimethyl-(R)- and -(S)-3-aminohexahydroazepinedichloroplatinum(II) Evonne M. Rezler, Ronald R. Fenton, Warren J. Esdale, Mark J. McKeage, Pamela J. Russell, and Trevor W. Hambley [Full Article - PDF]

3516-3523

Novel Tacrine Analogues for Potential Use against Alzheimer's Disease: Potent and Selective Acetylcholinesterase Inhibitors and 5-HT Uptake Inhibitors Maureen T. McKenna, George R. Proctor, Louise C. Young, and Alan L. Harvey [Full Article - PDF]

3524-3533

Inhibition of Tubulin Polymerization by 5,6-Dihydroindolo[2,1-a]isoquinoline Derivatives Michael Goldbrunner, Günther Loidl, Thomas Polossek, Albrecht Mannschreck, and Erwin von Angerer [Full Article - PDF]

3534-3541

Studies on Selectin Blockers. 5. Design, Synthesis, and Biological Profile of Sialyl Lewis x Mimetics Based on Modified Serine-Glutamic Acid Dipeptides Takahiro Tsukida, Yasuyuki Hiramatsu, Hideki Tsujishita, Takao Kiyoi, Masahiro Yoshida, Kiriko Kurokawa, Hideki Moriyama, Hiroshi Ohmoto, Yukihisa Wada, Tadayuki Saito, and Hirosato Kondo [Full Article - PDF]

3542-3550

Differentiation between Partial Agonists and Neutral 5-HT1B Antagonists by Chemical Modulation of 3-[3-(N,N-Dimethylamino)propyl]-4-hydroxy- N-[4-(pyridin-4-yl)phenyl]benzamide (GR-55562) Marie Lamothe, Petrus J. Pauwels, Karine Belliard, Philippe Schambel, and Serge Halazy [Full Article - PDF]

3551-3556

Discovery of 3-Aminobenzyloxycarbonyl as an N-Terminal Group Conferring High Affinity to the Minimal Phosphopeptide Sequence Recognized by the Grb2-SH2 Domain Pascal Furet, Brigitte Gay, Carlos García-Echeverría, Joseph Rahuel, Heinz Fretz, Joseph Schoepfer, and Giorgio Caravatti [Full Article - PDF]

3557-3566

Antimalarial Activity of Molecules Interfering with Plasmodium falciparum Phospholipid Metabolism. Structure-Activity Relationship Analysis Michèle Calas, Gérard Cordina, Jacques Bompart, Mohamed Ben Bari, Taïb Jei, Marie L. Ancelin, and Henri Vial [Full Article - PDF]

3567-3583

Biologically Active Heteroarotinoids Exhibiting Anticancer Activity and Decreased Toxicity Doris M. Benbrook, Matora M. Madler, Lyle W. Spruce, Paul J. Birckbichler, Eldon C. Nelson, Shankar Subramanian, G. Mahika Weerasekare, Jonathan B. Gale, Manford K. Patterson, Jr., Binghe Wang, Wei Wang, Shennan Lu, Tami C. Rowland, Paul DiSivestro, Charles Lindamood III, Donald L. Hill, and K. Darrell Berlin [Full Article - PDF]

3584-3593

Novel Fluoroquinolone Antibacterial Agents Containing Oxime-Substituted (Aminomethyl)pyrrolidines: Synthesis and Antibacterial Activity of 7-(4-(Aminomethyl)-3-(methoxyimino)pyrrolidin-1-yl)-1-cyclopropyl-6-fluoro- 4-oxo-1,4-dihydro[1,8]naphthyridine-3-carboxylic Acid (LB20304),1 Chang Yong Hong, Young Kwan Kim, Jay Hyok Chang, Se Ho Kim, Hoon Choi, Do Hyun Nam, Yong Zu Kim, and Jin Hwan Kwak [Full Article - PDF]

3594-3600

Design, Synthesis, and Dopamine Receptor Modulating Activity of Diketopiperazine Peptidomimetics of L-Prolyl-L-leucylglycinamide Paul W. Baures, William H. Ojala, Willard J. Costain, Michael C. Ott, Ashish Pradhan, William B. Gleason, Ram K. Mishra, and Rodney L. Johnson [Full Article - PDF]

3601-3616

Use of a Pharmacophore Model for the Design of EGF-R Tyrosine Kinase Inhibitors: 4-(Phenylamino)pyrazolo[3,4-d]pyrimidines Peter Traxler, Guido Bold, Joerg Frei, Marc Lang, Nicholas Lydon, Helmut Mett, Elisabeth Buchdunger, Thomas Meyer, Marcel Mueller, and Pascal Furet [Full Article - PDF]

3617-3625

Potent Anandamide Analogs: The Effect of Changing the Length and Branching of the End Pentyl Chain William J. Ryan, W. Kenneth Banner, Jenny L. Wiley, Billy R. Martin, and Raj K. Razdan [Full Article - PDF]

3626-3634

Synthesis and Pharmacological Comparison of Dimethylheptyl and Pentyl Analogs of Anandamide Herbert H. Seltzman, Denise N. Fleming, Brian F. Thomas, Anne F. Gilliam, Deirdre S. McCallion, Roger G. Pertwee, David R. Compton, and Billy R. Martin [Full Article - PDF]

3635-3644

Structure-Activity Relationships of 2'-Deoxy-2',2'-difluoro-L-erythro-pentofuranosyl Nucleosides Lakshmi P. Kotra, Yuejun Xiang, M. Gary Newton, Raymond F. Schinazi, Yung-C. Cheng, and Chung K. Chu [Full Article - PDF]

3645-3650

Synthesis of Willardiine and 6-Azawillardiine Analogs: Pharmacological Characterization on Cloned Homomeric Human AMPA and Kainate Receptor Subtypes David E. Jane, Ken Hoo, Raj Kamboj, Michele Deverill, David Bleakman, and Allan Mandelzys [Full Article - PDF]

3651-3658

Constrained Corticotropin-Releasing Factor Antagonists with i-(i + 3) Glu-Lys Bridges Antonio Miranda, Sabine L. Lahrichi, Jozsef Gulyas, Steven C. Koerber, Anthony G. Craig, Anne Corrigan, Catherine Rivier, Wylie Vale, and Jean Rivier [Full Article - PDF]

3659-3669

Induction of the Estrogen Specific Mitogenic Response of MCF-7 Cells by Selected Analogues of Estradiol-17: A 3D QSAR Study Thomas E. Wiese, Lisa A. Polin, Eduardo Palomino, and S. C. Brooks [Full Article - PDF]

3670-3678

Novel and Highly Potent 5-HT3 Receptor Agonists Based on a Pyrroloquinoxaline Structure Giuseppe Campiani, Andrea Cappelli, Vito Nacci, Maurizio Anzini, Salvatore Vomero, Michel Hamon, Alfredo Cagnotto, Claudia Fracasso, Chiara Uboldi, Silvio Caccia, Silvana Consolo, and Tiziana Mennini [Full Article - PDF]

3679-3686

5-(N-Oxyaza)-7-substituted-1,4-dihydroquinoxaline-2,3-diones: Novel, Systemically Active and Broad Spectrum Antagonists for NMDA/glycine, AMPA, and Kainate Receptors Sui Xiong Cai, Jin-Cheng Huang, Stephen A. Espitia, Minhtam Tran, Victor I. Ilyin, Jon E. Hawkinson, Richard M. Woodward, Eckard Weber, and John F. W. Keana [Full Article - PDF]

3687-3693

Synthesis of a Series of Potent and Orally Bioavailable Thrombin Inhibitors That Utilize 3,3-Disubstituted Propionic Acid Derivatives in the P3 Position Thomas J. Tucker, William C. Lumma, S. Dale Lewis, Stephen J. Gardell, Bobby J. Lucas, Jack T. Sisko, Joseph J. Lynch, Elizabeth A. Lyle, Elizabeth P. Baskin, Richard F. Woltmann, Sandra D. Appleby, I-Wu Chen, Kimberley B. Dancheck, Adel M. Naylor-Olsen, Julie A. Krueger, Carolyn M. Cooper, and Joseph P. Vacca [Full Article - PDF]

3694-3699

2,4-Diaminothieno[2,3-d]pyrimidine Lipophilic Antifolates as Inhibitors of Pneumocystis carinii and Toxoplasma gondii Dihydrofolate Reductase Andre Rosowsky, Andrew T. Papoulis, and Sherry F. Queener [Full Article - PDF]

3700-3705

(S)-Homo-AMPA, a Specific Agonist at the mGlu6 Subtype of Metabotropic Glutamic Acid Receptors Haleh Ahmadian, Birgitte Nielsen, Hans Bräuner-Osborne, Tommy N. Johansen, Tine B. Stensbl, Frank A. Slk, Naohiro Sekiyama, Shigetada Nakanishi, Povl Krogsgaard-Larsen, and Ulf Madsen [Full Article - PDF]

3706-3706

Synthesis and Bioevaluation of 7-5-Desaturase Inhibitors, an Enzyme Late in the Biosynthesis of the Fungal Sterol Ergosterol Alex S. Goldstein and Leah L. Frye [Full Article - PDF]