4169-4194
| Neuronal Nicotinic Acetylcholine Receptors as Targets for Drug Discovery
Mark W. Holladay,
Michael J. Dart, and
John K. Lynch
[Full Article -
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4195-4198
| Development of a High-Affinity Ligand That Binds Irreversibly to Mel1b Melatonin Receptors
Paula A. Witt-Enderby,
Guo-Hua Chu,
Megan L. Gillen, and
Pui-Kai Li
[Full Article -
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4199-4207
| Synthesis and Biological Activity of Novel Nonnucleoside Inhibitors of HIV-1 Reverse Transcriptase. 2-Aryl-Substituted Benzimidazoles
Thomas Roth,
Marshall L. Morningstar,
Paul L. Boyer,
Stephen H. Hughes,
Robert W. Buckheit, Jr., and
Christopher J. Michejda
[Full Article -
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4208-4221
| Monoaryl- and Bisaryldihydroxytropolones as Potent Inhibitors of Inositol Monophosphatase
Serge R. Piettre,
Catherine André,
Marie-Christine Chanal,
Jean-Bernard Ducep,
Brigitte Lesur,
François Piriou,
Pierre Raboisson,
Jean-Michel Rondeau,
Charles Schelcher,
Pascale Zimmermann, and
Axel J. Ganzhorn
[Full Article -
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4222-4234
| Regulation of Retinoidal Actions by Diazepinylbenzoic Acids. Retinoid Synergists Which Activate the RXR-RAR Heterodimers
Hiroki Umemiya,
Hiroshi Fukasawa,
Masayuki Ebisawa,
Laurence Eyrolles,
Emiko Kawachi,
Ghislaine Eisenmann,
Hinrich Gronemeyer,
Yuichi Hashimoto,
Koichi Shudo, and
Hiroyuki Kagechika
[Full Article -
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4235-4256
| New Generation Dopaminergic Agents. 1. Discovery of a Novel Scaffold Which Embraces the D2 Agonist Pharmacophore. Structure-Activity Relationships of a Series of 2-(Aminomethyl)chromans
Richard E. Mewshaw,
Joseph Kavanagh,
Gary Stack,
Karen L. Marquis,
Xiaojie Shi,
Michael Z. Kagan,
Michael B. Webb,
Alan H. Katz,
Anna Park,
Young H. Kang,
Magid Abou-Gharbia,
Rosemary Scerni,
Theodore Wasik,
Luz Cortes-Burgos,
Taylor Spangler,
Julie A. Brennan,
Michael Piesla,
Hossein Mazandarani,
Mark I. Cockett,
Rafal Ochalski,
Joseph Coupet, and
Terrance H. Andree
[Full Article -
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4257-4264
| A 3D QSAR Study of a Series of HEPT Analogues: The Influence of Conformational Mobility on HIV-1 Reverse Transcriptase Inhibition
Dmitri B. Kireev,
Jacques R. Chrétien,
David S. Grierson, and
Claude Monneret
[Full Article -
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4265-4280
| Design of [R-(Z)]-(+)- -(Methoxyimino)-1-azabicyclo[2.2.2]octane-3-acetonitrile (SB 202026), a Functionally Selective Azabicyclic Muscarinic M1 Agonist Incorporating the N-Methoxy Imidoyl Nitrile Group as a Novel Ester Bioisostere
Steven M. Bromidge,
Frank Brown,
Frederick Cassidy,
Michael S. G. Clark,
Steven Dabbs,
Michael S. Hadley,
Julie Hawkins,
Julia M. Loudon,
Christopher B. Naylor,
Barry S. Orlek, and
Graham J. Riley
[Full Article -
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4281-4289
| Synthesis and Pharmacological Evaluation of N-(2,5-Disubstituted phenyl)-N'-(3-substituted phenyl)-N'-methylguanidines As N-Methyl-D-aspartate Receptor Ion-Channel Blockers
Lain-Yen Hu,
Junqing Guo,
Sharad S. Magar,
James B. Fischer,
Kathleen J. Burke-Howie, and
Graham J. Durant
[Full Article -
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4290-4301
| Structure-Activity Relationship of 3-Substituted N-(Pyridinylacetyl)-4- (8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)- piperidine Inhibitors of Farnesyl-Protein Transferase: Design and Synthesis of in Vivo Active Antitumor Compounds
F. George Njoroge,
Bancha Vibulbhan,
Dinananth F. Rane,
W. Robert Bishop,
Joanne Petrin,
Robert Patton,
Mathew S. Bryant,
K.-J. Chen,
Amin A. Nomeir,
C.-C. Lin,
Ming Liu,
Ivan King,
Jianping Chen,
Suining Lee,
Bohdan Yaremko,
Janet Dell,
Philip Lipari,
Michael Malkowski,
Zujun Li,
Joseph Catino,
Ronald J. Doll,
V. Girijavallabhan, and
Ashit K. Ganguly
[Full Article -
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4302-4307
| Synthesis and Biological Evaluation of Potent, Selective, Hexapeptide CCK-A Agonist Anorectic Agents
M. Edward Pierson,
Jeanne M. Comstock,
Roy D. Simmons,
Frederick Kaiser,
Ronald Julien,
John Zongrone, and
James D. Rosamond
[Full Article -
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4308-4318
| Fibrinogen Receptor (GPIIb-IIIa) Antagonists Derived from 5,6-Bicyclic Templates. Amidinoindoles, Amidinoindazoles, and Amidinobenzofurans Containing the N--Sulfonamide Carboxylic Acid Function as Potent Platelet Aggregation Inhibitors
Ting Su,
Mary Ann H. Naughton,
Mark S. Smyth,
Jack W. Rose,
Ann E. Arfsten,
Jefferson R. McCowan,
Joseph A. Jakubowski,
Virginia L. Wyss,
Kenneth J. Ruterbories,
Daniel J. Sall, and
Robert M. Scarborough
[Full Article -
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4319-4328
| Comparative Molecular Field Analysis of A Series of Paclitaxel Analogues
Qiqing Zhu,
Zongru Guo,
Niu Huang,
Minmin Wang, and
Fengming Chu
[Full Article -
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4329-4339
| Novel N-Substituted 3-[Bis(4'-fluorophenyl)methoxy]tropane Analogues: Selective Ligands for the Dopamine Transporter
Gregory E. Agoston,
Jae H. Wu,
Sari Izenwasser,
Clifford George,
Jonathan Katz,
Richard H. Kline, and
Amy Hauck Newman
[Full Article -
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4340-4346
| Isothiocyanate Derivatives of 9-[3-(cis-3,5-Dimethyl-1-piperazinyl)propyl]- carbazole (Rimcazole): Irreversible Ligands for the Dopamine Transporter
Stephen M. Husbands,
Sari Izenwasser,
Richard J. Loeloff,
Jonathan L. Katz,
Wayne D. Bowen,
Bertold J. Vilner, and
Amy Hauck Newman
[Full Article -
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4347-4359
| Three-Dimensional Quantitative Structure-Activity Relationships from Molecular Similarity Matrices and Genetic Neural Networks. 1. Method and Validations
Sung-Sau So and
Martin Karplus
[Full Article -
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4360-4371
| Three-Dimensional Quantitative Structure-Activity Relationships from Molecular Similarity Matrices and Genetic Neural Networks. 2. Applications
Sung-Sau So and
Martin Karplus
[Full Article -
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4372-4377
| Synthesis and Evaluation of Polycyclic Pyrazolo[3,4-d]pyrimidines as PDE1 and PDE5 cGMP Phosphodiesterase Inhibitors
Yan Xia,
Samuel Chackalamannil,
Michael Czarniecki,
Hsingan Tsai,
Henry Vaccaro,
Renee Cleven,
John Cook,
Ahmad Fawzi,
Robert Watkins, and
Hongtao Zhang
[Full Article -
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4378-4385
| Synthesis and Biochemical Evaluation of N-(4-Phenylthiazol-2-yl)benzenesulfonamides as High-Affinity Inhibitors of Kynurenine 3-Hydroxylase
Stephan Röver,
Andrea M. Cesura,
Philipp Huguenin,
Rolf Kettler, and
Andre Szente
[Full Article -
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4386-4395
| Strategies for Rapid Deconvolution of Combinatorial Libraries: Comparative Evaluation Using a Model System
Danielle A. M. Konings,
Jacqueline R. Wyatt,
David J. Ecker, and
Susan M. Freier
[Full Article -
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4396-4405
| Synthesis and Structure-Activity Relationships of 3,7-Dimethyl-1-propargylxanthine Derivatives, A2A-Selective Adenosine Receptor Antagonists
Christa E. Müller,
Uli Geis,
Jo Hipp,
Ulrike Schobert,
Wolfram Frobenius,
Maciej Pawowski,
Fumio Suzuki, and
Jesús Sandoval-Ramírez
[Full Article -
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4406-4414
| Synthesis, Structure, Dopamine Transporter Affinity, and Dopamine Uptake Inhibition of 6-Alkyl-3-benzyl-2-[(methoxycarbonyl)methyl]tropane Derivatives
Stacey A. Lomenzo,
Sari Izenwasser,
Jonathan L. Katz,
Phyllis D. Terry,
Naijue Zhu,
Cheryl L. Klein, and
Mark L. Trudell
[Full Article -
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4415-4419
| 2-(1-Naphthyloxy)ethylamines with Enhanced Affinity for Human 5-HT1D (h5-HT1B) Serotonin Receptors
Abd M. Ismaiel,
Malgorzata Dukat,
Ho Law,
Rajender Kamboj,
Ermi Fan,
David K. H. Lee,
Lucia Mazzocco,
Donna Buekschkens,
Milt Teitler,
Myles E. Pierson, and
Richard A. Glennon
[Full Article -
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4420-4425
| Azinyl and Diazinyl Hydrazones Derived from Aryl N-Heteroaryl Ketones: Synthesis and Antiproliferative Activity
Johnny Easmon,
Gottfried Heinisch,
Gerhard Pürstinger,
Thierry Langer, and
Jürgen K. Österreicher
, Hans H. Grunicke and
Johann Hofmann
[Full Article -
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