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 -
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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 -
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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 -
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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 -
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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 -
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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 -
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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 -
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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 -
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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 -
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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 -
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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 -
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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 -
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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 -
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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] |