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4027-4030
Synthesis and Antibacterial Activity of Acylides (3-O-Acyl-erythromycin Derivatives): A Novel Class of Macrolide Antibiotics
Tetsuya Tanikawa,
Toshifumi Asaka,
Masato Kashimura,
Yoko Misawa,
Keiko Suzuki,
Masakazu Sato,
Kazuya Kameo,
Shigeo Morimoto, and
Atsushi Nishida
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4031-4034
N-[3-(2-Dimethylaminoethyl)-2-methyl-1H- indol-5-yl]-4-fluorobenzamide: A Potent, Selective, and Orally Active 5-HT1F Receptor Agonist Potentially Useful for Migraine Therapy
Yao-Chang Xu,
Kirk W. Johnson,
Lee A. Phebus,
Marlene Cohen,
David L. Nelson,
Kathy Schenck,
Clint D. Walker,
James E. Fritz,
Stephen W. Kaldor,
Michael E. LeTourneau,
Robert E. Murff,
John M. Zgombick,
David O. Calligaro,
James E. Audia, and
John M. Schaus
[Full Article -
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4035-4038
Design, Synthesis, and Biological Activity of Methoctramine-Related Polyamines as Putative Gi Protein Activators
Carlo Melchiorre,
Maria L. Bolognesi,
Roberta Budriesi,
Carla Ghelardini,
Alberto Chiarini,
Anna Minarini,
Michela Rosini,
Vincenzo Tumiatti, and
Erik J. Wade
[Full Article -
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4039-4041
Synthesis, Nicotinic Acetylcholine Receptor Binding, and Antinociceptive Properties of 2-exo-2-(2'-Substituted-3'-phenyl-5'-pyridinyl)-7-azabicyclo[2.2.1]heptanes. Novel Nicotinic Antagonist
F. Ivy Carroll,
Jeffrey R. Lee,
Hernán A. Navarro,
Lawrence E. Brieaddy,
Philip Abraham,
M. I. Damaj, and
Billy R. Martin
[Full Article -
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4042-4049
Discovery and Biological Evaluation of a New Family of Potent Inhibitors of the Dual Specificity Protein Phosphatase Cdc25
John S. Lazo,
Diana C. Aslan,
Eileen C. Southwick,
Kathleen A. Cooley,
Alexander P. Ducruet,
Beomjun Joo,
Andreas Vogt, and
Peter Wipf
[Full Article -
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4050-4061
Monosaccharide-Linked Inhibitors of O6-Methylguanine-DNA Methyltransferase (MGMT): Synthesis, Molecular Modeling, and Structure-Activity Relationships
Jost Reinhard,
William E. Hull,
Claus-Wilhelm von der Lieth,
Uta Eichhorn,
Hans-Christian Kliem,
Bernd Kaina, and
Manfred Wiessler
[Full Article -
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4062-4071
Methyl Analogues of the Experimental Alzheimer Drug Phenserine: Synthesis and Structure/Activity Relationships for Acetyl- and Butyrylcholinesterase Inhibitory Action
Qian-sheng Yu,
Harold W. Holloway,
Judith L. Flippen-Anderson,
Brian Hoffman,
Arnold Brossi, and
Nigel H. Greig
[Full Article -
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4072-4081
Analysis of Selective Regions in the Active Sites of Human Cytochromes P450, 2C8, 2C9, 2C18, and 2C19 Homology Models Using GRID/CPCA
Marianne Ridderström,
Ismael Zamora,
Ola Fjellström, and
Tommy B. Andersson
[Full Article -
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4082-4091
Rational Design, Discovery, and Synthesis of a Novel Series of Potent Growth Hormone Secretagogues
Ping Huang,
Gilda H. Loew,
Hidenori Funamizu,
Mitsuo Mimura,
Nobuo Ishiyama,
Mitsuo Hayashida,
Tadashi Okuno,
Osafumi Shimada,
Akihiko Okuyama,
Satoru Ikegami,
Jun Nakano, and
Kiyoshi Inoguchi
[Full Article -
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4092-4113
The Biological Effects of Structural Variation at the Meta Position of the Aromatic Rings and at the End of the Alkenyl Chain in the Alkenyldiarylmethane Series of Non-Nucleoside Reverse Transcriptase Inhibitors
Guozhang Xu,
Mark Micklatcher,
Maximilian A. Silvestri,
Tracy L. Hartman,
Jennifer Burrier,
Mark C. Osterling,
Heather Wargo,
Jim A. Turpin,
Robert W. Buckheit, Jr., and
Mark Cushman
[Full Article -
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4114-4124
Novel Agouti-Related-Protein-Based Melanocortin-1 Receptor Antagonist
Ramanan Thirumoorthy,
Jerry Ryan Holder,
Rayna M. Bauzo,
Nigel G. J. Richards,
Arthur S. Edison, and
Carrie Haskell-Luevano
[Full Article -
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4125-4136
Neoceptor Concept Based on Molecular Complementarity in GPCRs: A Mutant Adenosine A3 Receptor with Selectively Enhanced Affinity for Amine-Modified Nucleosides
Kenneth A. Jacobson,
Zhan-Guo Gao,
Aishe Chen,
Dov Barak,
Soon-Ai Kim,
Kyeong Lee,
Andreas Link,
Philippe Van Rompaey,
Serge van Calenbergh, and
Bruce T. Liang
[Full Article -
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4137-4156
Novel Erythromycin Derivatives with Aryl Groups Tethered to the C-6 Position Are Potent Protein Synthesis Inhibitors and Active against Multidrug-Resistant Respiratory Pathogens
Zhenkun Ma,
Richard F. Clark,
Antony Brazzale,
Sanyi Wang,
Michael J. Rupp,
Leping Li,
George Griesgraber,
Suoming Zhang,
Hong Yong,
Ly Tam Phan,
Peter A. Nemoto,
Daniel T. W. Chu,
Jacob J. Plattner,
Xiaolin Zhang,
Ping Zhong,
Zhensheng Cao,
Angela M. Nilius,
Virginia D. Shortridge,
Robert Flamm,
Michael Mitten,
Jon Meulbroek,
Patty Ewing,
Jeff Alder, and
Yat Sun Or
[Full Article -
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4157-4169
Synthesis and Biological Evaluation of Prostaglandin-F Alkylphosphinic Acid Derivatives as Bone Anabolic Agents for the Treatment of Osteoporosis
David L. Soper,
Jared B. J. Milbank,
Glen E. Mieling,
Michelle J. Dirr,
Andrew S. Kende,
Robin Cooper,
Webster S. S. Jee,
Wei Yao,
Jian Liang Chen,
Mark Bodman,
Mark W. Lundy,
Biswanath De,
Mark E. Stella,
Frank H. Ebetino,
Yili Wang,
Mitchell A. deLong, and
John A. Wos
[Full Article -
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4170-4175
Design and Pharmacological Activity of Phosphinic Acid Based NAALADase Inhibitors
Paul F. Jackson,
Kevin L. Tays,
Keith M. Maclin,
Yao-Sen Ko,
Weixing Li,
Dil Vitharana,
Takashi Tsukamoto,
Doris Stoermer,
Xi-Chun M. Lu,
Krystyna Wozniak, and
Barbara S. Slusher
[Full Article -
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4176-4185
Design, Synthesis, and Transfection Biology of Novel Cationic Glycolipids for Use in Liposomal Gene Delivery
Rajkumar Banerjee,
Yenugonda Venkata Mahidhar, and
Arabinda Chaudhuri
, Vijaya Gopal and
Nalam Madhusudhana Rao
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4186-4195
Design and Optimization of 20-O-Linked Camptothecin Glycoconjugates as Anticancer Agents
Hans-Georg Lerchen,
Joerg Baumgarten,
Karsten von dem Bruch,
Thomas E. Lehmann,
Michael Sperzel,
Grazyna Kempka, and
Heinz-Herbert Fiebig
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4196-4206
5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-Based Potent and Selective CCK1 Receptor Antagonists: Structure-Activity Relationship Studies on the Central 1,3-Dioxoperhydropyrido[1,2-c]pyrimidine Scaffold
José M. Bartolomé-Nebreda,
M. Teresa García-López,
Rosario González-Muñiz,
Edurne Cenarruzabeitia,
Miriam Latorre,
Joaquín Del Río, and
Rosario Herranz
[Full Article -
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4207-4215
A Novel Anti-Ischemic ATP-Sensitive Potassium Channel (KATP) Opener without Vasorelaxation: N-(6-Aminobenzopyranyl)-N'-benzyl-N' '-cyanoguanidine Analogue
Sung-eun Yoo,
Kyu Yang Yi,
Sunkyung Lee,
Jeehee Suh,
Nakjeong Kim,
Byung Ho Lee,
Ho Won Seo,
Sun-Ok Kim,
Dong-Ha Lee,
Hong Lim, and
Hwa Sup Shin
[Full Article -
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4216-4224
The Synthesis of a Prodrug of Doxorubicin Designed to Provide Reduced Systemic Toxicity and Greater Target Efficacy
Victor M. Garsky,
Patricia K. Lumma,
Dong-Mei Feng,
Jenny Wai,
Harri G. Ramjit,
Mohinder K. Sardana,
Allen Oliff,
Raymond E. Jones,
Deborah DeFeo-Jones, and
Roger M. Freidinger
[Full Article -
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4225-4229
Synthesis and Antiviral Activity of Novel Acyclic Nucleoside Analogues of 5-(1-Azido-2-haloethyl)uracils
Rakesh Kumar,
Neerja Sharma,
Mahendra Nath,
Holly A. Saffran, and
D. Lorne J. Tyrrell
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4230-4251
Estrogen Receptor- Potency-Selective Ligands: Structure-Activity Relationship Studies of Diarylpropionitriles and Their Acetylene and Polar Analogues
Marvin J. Meyers,
Jun Sun,
Kathryn E. Carlson,
Gwendolyn A. Marriner,
Benita S. Katzenellenbogen, and
John A. Katzenellenbogen
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4252-4267
Design of Selective and Soluble Inhibitors of Tumor Necrosis Factor- Converting Enzyme (TACE)
Michael H. Rabinowitz,
Robert C. Andrews,
J. David Becherer,
D. Mark Bickett,
Dulce G. Bubacz,
James G. Conway,
David J. Cowan,
Micheal Gaul,,&
Kimberly Glennon,
Millard H. Lambert,
M. Anthony Leesnitzer,
Darryl L. McDougald,
Marcia L. Moss,
David L. Musso, and
Michele C. Rizzolio
[Full Article -
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4268-4276
A Prodrug Form of a Plasmodium falciparum Glutathione Reductase Inhibitor Conjugated with a 4-Anilinoquinoline
Elisabeth Davioud-Charvet,
Sandrine Delarue,
Christophe Biot,
Babett Schwöbel,
Catharina C. Boehme,
Andreas Müssigbrodt,
Louis Maes,
Christian Sergheraert,
Philippe Grellier,
R. Heiner Schirmer, and
Katja Becker
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4277-4283
Role of Hydrophilic Interaction in Binding of Hydroxylated 3-Deoxy C19 Steroids to the Active Site of Aromatase
Mitsuteru Numazawa,
Keiko Yamada,
Syoko Nitta,
Chika Sasaki, and
Kanae Kidokoro
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4284-4287
Fluorescent Tricyclic Analogues of Acyclovir and Ganciclovir. A Structure-Antiviral Activity Study
Bozenna Golankiewicz,
Tomasz Ostrowski,
Tomasz Goslinski,
Piotr Januszczyk,
Joanna Zeidler,
Daniel Baranowski, and
Erik de Clercq
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4288-4291
Salicylaldoxime Moiety as a Phenolic "A-Ring" Substitute in Estrogen Receptor Ligands
Filippo Minutolo,
Simone Bertini,
Chiara Papi,
Kathryn E. Carlson,
John A. Katzenellenbogen, and
Marco Macchia
[Full Article -
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4292-4295
5,6-Diphenylpyridazine Derivatives as Acyl-CoA:Cholesterol Acyltransferase Inhibitors
Maria Paola Giovannoni,
Vittorio Dal Piaz,
Byoung-Mog Kwon,
Mi-Kyung Kim,
Young-Kook Kim,
Lucio Toma,
Daniela Barlocco,
Franco Bernini, and
Monica Canavesi
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4296-4299
An Orally Active, Water-Soluble Neurokinin-1 Receptor Antagonist Suitable for Both Intravenous and Oral Clinical Administration
Timothy Harrison,
Andrew P. Owens,
Brian J. Williams,
Christopher J. Swain,
Angela Williams,
Emma J. Carlson,
Wayne Rycroft,
F. David Tattersall,
Margaret A. Cascieri,
Gary G. Chicchi,
Sharon Sadowski,
Nadia M. J. Rupniak, and
Richard J. Hargreaves
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4300-4303
Novel Potent Inhibitors of Lipid Peroxidation with Protective Effects against Reperfusion Arrhythmias
Maria Koufaki,
Theodora Calogeropoulou,
Anastasia Detsi,
Aristidis Roditis,
Angeliki P. Kourounakis,
Panagiota Papazafiri,
Karyofyllis Tsiakitzis,
Catherine Gaitanaki,
Isidoros Beis, and
Panos N. Kourounakis
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4304-4304
| Cytokine Inhibitors Edited by Gennaro Ciliberto and Rocco Savino. Marcel Dekker, New York. 2001. xiv + 372 pp. 15.5 × 23.5 cm. ISBN 0-0434-7. $165.00.
D. Eric Walters
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4304-4304
| Solid Phase Synthesis. Edited by Kevin Burgess. Wiley Interscience, New York. 2000. xiv + 277 pp. 15.5 × 23.5 cm. ISBN 0471318256. $69.95.
Patrick M. Woster
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4304-4305
| Metal Ions in Biological Systems. Volume 38. Probing of Proteins by Metal Ions and Their Low Molecular Weight Complexes Edited by Astrid Sigel and Helmut Sigel. Marcel Dekker, New York. 2001. xlvii + 690 pp. 16 × 23.5 cm. ISBN 0-8247-0289-1. $250.00.
John R. J. Sorenson
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4305-4305
| Advances in Protein Chemistry. Volume 56. Drug Discovery and Design Edited by Edward M. Scolnick. Academic Press, San Diego, CA. 2000. xi + 567 pp. 16 × 23.5 cm. ISBN 0-12-034256-1. $119.95.
Richard A. Hudson
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4305-4306
| Solid Phase Synthesis: A Practical Guide Edited by Steven A. Kates and Fernando Albericio. Marcel Dekker, Inc., New York. 2000. xx + 826 pp. 15.5 × 24 cm. ISBN 0-8247-0359-6. $250.00.
Lenore M. Martin
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4306-4306
| Combinatorial Chemistry Edited by Hicham Fenniri. Oxford University Press, Inc., New York. 2000. xxxii + 476 pp. 19 × 24.5 cm. ISBN 0-19-963754-7. $70.00 (paperback).
Robert G. Gentles
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ADDITIONS AND CORRECTIONS
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4307-4307
| Synthesis and Biological Evaluation of Prostaglandin-F Alkylphosphinic Acid Derivatives as Bone Anabolic Agents for the Treatment of Osteoporosis.
David L. Soper,
Jared B. J. Milbank,
Glen E. Mieling,
Michelle J. Dirr,
Andrew S. Kende,
Robin
Cooper,
Webster S. S. Jee,
Wei Yao,
Jian Liang
Chen,
Mark Bodman,
Mark W. Lundy,
Biswanath De,
Mark E. Stella,
Frank H. Ebetino,
Yili Wang,
Mitchell A. deLong, and
John A. Wos:
[Full Article -
PDF] | |