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`Journal of Medicinal Chemistry | Vol 47, No 17
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`Journal of Medicinal Chemistry | Vol 47, No 17
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`
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`August 12, 2004
`Volume 47, Issue 17
`Pages 4111-4338
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`About the Cover:
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`Ribbon rendered illustration of the nuclear receptor heterodimer RXRα(cyan):PPARRγ (red) ligand binding domains
`bound with coactivator peptides (magenta) and agonist ligands (space-lling atoms where green is carbon, red is
`oxygen, and blue is nitrogen) (Haffner, C. D.; et al. J. Med. Chem. 2004, 47, 2010-2029).
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`In this issue:
`
`Miniperspectives:Advances in Type 2 Diabetes
`Letters
`Articles
`Brief Articles
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`MINIPERSPECTIVES:ADVANCES IN TYPE 2 DIABETES
`
`Novel “Second-Generation” Approaches for the Control of Type 2 Diabetes
`
`David P. Rotella
`
`Journal of Medicinal Chemistry  2004, 47, 17, 4111-4112 (Perspective)
`Publication Date (Web): July 20, 2004
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` First Page
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` Full text
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` PDF
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`https://pubs.acs.org/toc/jmcmar/47/17
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`Diabetes Mellitus:  Pathogenesis and Treatment Strategies
`
`Jay S. Skyler
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`Journal of Medicinal Chemistry  2004, 47, 17, 4113-4117 (Perspective)
`Publication Date (Web): July 20, 2004
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` First Page
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`Journal of Medicinal Chemistry | Vol 47, No 17
`Peroxisome Proliferator-Activated Receptor α/γ Dual Agonists for the
`Treatment of Type 2 Diabetes
`
`Brad R. Henke
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`Journal of Medicinal Chemistry  2004, 47, 17, 4118-4127 (Perspective)
`Publication Date (Web): July 20, 2004
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` First Page
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`Glucagon-like Peptide-1:  The Basis of a New Class of Treatment for Type 2
`Diabetes
`
`Lotte Bjerre Knudsen
`
`Journal of Medicinal Chemistry  2004, 47, 17, 4128-4134 (Perspective)
`Publication Date (Web): July 20, 2004
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` First Page
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`Dipeptidyl Peptidase IV Inhibitors for the Treatment of Diabetes
`https://pubs.acs.org/toc/jmcmar/47/17
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`3/13/23, 9:13 AM
`Ann E. Weber
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`Journal of Medicinal Chemistry | Vol 47, No 17
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`Journal of Medicinal Chemistry  2004, 47, 17, 4135-4141 (Perspective)
`Publication Date (Web): July 20, 2004
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` First Page
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`Prospects for Inhibitors of Protein Tyrosine Phosphatase 1B as Antidiabetic
`Drugs
`
`Rob Hooft van Huijsduijnen, Wolfgang H. B. Sauer, Agnes Bombrun, and Dominique Swinnen
`
`Journal of Medicinal Chemistry  2004, 47, 17, 4142-4146 (Perspective)
`Publication Date (Web): July 20, 2004
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` First Page
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`LETTERS
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`https://pubs.acs.org/toc/jmcmar/47/17
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`Structure-Based Design, Synthesis, and Evaluation of Conformationally
`Constrained Mimetics of the Second Mitochondria-Derived Activator of
`Caspase That Target the X-Linked Inhibitor of Apoptosis Protein/Caspase-9
`Interaction Site
`
`Haiying Sun, Zaneta Nikolovska-Coleska, Chao-Yie Yang, Liang Xu, York Tomita, Krzysztof Krajewski, Peter P. Roller
`, and Shaomeng Wang
`
`Journal of Medicinal Chemistry  2004, 47, 17, 4147-4150 (Letter)
`Publication Date (Web): July 16, 2004
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` Abstract
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` Full text
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`Rational Approaches to Discovery of Orally Active and Brain-Penetrable
`Quinazolinone Inhibitors of Poly(ADP-ribose)polymerase
`
`Kouji Hattori, Yoshiyuki Kido, Hirofumi Yamamoto, Junya Ishida, Kazunori Kamijo, Kenji Murano, Mitsuru Ohkubo, 
`Takayoshi Kinoshita, Akinori Iwashita, Kayoko Mihara, Syunji Yamazaki, Nobuya Matsuoka, Yoshinori Teramura
`, and Hiroshi Miyake
`
`Journal of Medicinal Chemistry  2004, 47, 17, 4151-4154 (Letter)
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`https://pubs.acs.org/toc/jmcmar/47/17
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`3/13/23, 9:13 AM
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`Journal of Medicinal Chemistry | Vol 47, No 17
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` Abstract
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`1
`Dopamine/Serotonin Receptor Ligands. 9. Oxygen-Containing Midsized
`Heterocyclic Ring Systems and Nonrigidized Analogues. A Step toward
`Dopamine D Receptor Selectivity
`5
`
`Thomas W. Wittig, Michael Decker, and Jochen Lehmann
`
`Journal of Medicinal Chemistry  2004, 47, 17, 4155-4158 (Letter)
`Publication Date (Web): July 16, 2004
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` Abstract
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` ABSTRACT
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`https://pubs.acs.org/toc/jmcmar/47/17
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`Bulky Nonproteinogenic Amino Acids Permit the Design of Very Small and
`Effective Cationic Antibacterial Peptides
`
`Bengt Erik Haug, Wenche Stensen, Trine Stiberg, and John S. Svendsen
`
`Journal of Medicinal Chemistry  2004, 47, 17, 4159-4162 (Letter)
`Publication Date (Web): July 16, 2004
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` Abstract
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` Full text
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`A Nonpeptidic Sulfonamide Inhibits the p53−mdm2 Interaction and Activates
`p53-Dependent Transcription in mdm2-Overexpressing Cells
`
`Peter S. Galatin and Donald J. Abraham
`
`Journal of Medicinal Chemistry  2004, 47, 17, 4163-4165 (Letter)
`Publication Date (Web): July 21, 2004
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` Abstract
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` Full text
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`ARTICLES
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`Journal of Medicinal Chemistry | Vol 47, No 17
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` 
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`Human Integrin αvβ5:  Homology Modeling and Ligand Binding
`
`Luciana Marinelli, Kay-E. Gottschalk, Axel Meyer, Ettore Novellino, and Horst Kessler
`
`Journal of Medicinal Chemistry  2004, 47, 17, 4166-4177 (Article)
`Publication Date (Web): July 10, 2004
`
` Abstract
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` Full text
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` PDF
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` ABSTRACT
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`ADVERTISEMENT
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`https://pubs.acs.org/toc/jmcmar/47/17
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`10/19
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`DR. REDDY’S LABORATORIES, INC.
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`Journal of Medicinal Chemistry | Vol 47, No 17
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`Combining Pharmacophore Search, Automated Docking, and Molecular
`Dynamics Simulations as a Novel Strategy for Flexible Docking. Proof of
`Concept:  Docking of Arginine−Glycine−Aspartic Acid-like Compounds into the
`α β Binding Site
`v 3
`
`Nicolas Moitessier, Christophe Henry, Bernard Maigret, and Yves Chapleur
`
`Journal of Medicinal Chemistry  2004, 47, 17, 4178-4187 (Article)
`Publication Date (Web): July 20, 2004
`
` Abstract
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` Full text
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` PDF
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` ABSTRACT
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`Validation of Automated Docking Programs for Docking and Database
`Screening against RNA Drug Targets
`
`https://pubs.acs.org/toc/jmcmar/47/17
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`11/19
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`DR. REDDY’S LABORATORIES, INC.
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`3/13/23, 9:13 AM
`Carsten Detering and Gabriele Varani
`
`Journal of Medicinal Chemistry | Vol 47, No 17
`
`Journal of Medicinal Chemistry  2004, 47, 17, 4188-4201 (Article)
`Publication Date (Web): July 13, 2004
`
` Abstract
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` Full text
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` PDF
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` ABSTRACT
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` 
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`Tricyclic Alkylamides as Melatonin Receptor Ligands with Antagonist or Inverse
`Agonist Activity
`
`Valeria Lucini, Marilou Pannacci, Francesco Scaglione, Franco Fraschini, Sivia Rivara, Marco Mor, Fabrizio Bordi, 
`Pier Vincenzo Plazzi, Gilberto Spadoni, Annalida Bedini, Giovanni Piersanti, Giuseppe Diamantini, and Giorgio
`Tarzia
`
`Journal of Medicinal Chemistry  2004, 47, 17, 4202-4212 (Article)
`Publication Date (Web): July 17, 2004
`
` Abstract
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` Full text
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` PDF
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` ABSTRACT
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`https://pubs.acs.org/toc/jmcmar/47/17
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`12/19
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`DR. REDDY’S LABORATORIES, INC.
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`Journal of Medicinal Chemistry | Vol 47, No 17
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` 
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`Liver-Selective Glucocorticoid Antagonists:  A Novel Treatment for Type 2
`Diabetes
`
`Thomas W. von Geldern, Noah Tu, Philip R. Kym, James T. Link, Hwan-Soo Jae, Chunqiu Lai, Theresa Apelqvist, 
`Patrik Rhonnstad, Lars Hagberg, Konrad Koehler, Marlena Grynfarb, Annika Goos-Nilsson, Johnny Sandberg, Marie
`Österlund, Tomas Barkhem, Marie Höglund, Jiahong Wang, Steven Fung, Denise Wilcox, Phong Nguyen, Clarissa
`Jakob, Charles Hutchins, Mathias Färnegårdh, Björn Kauppi, Lars Öhman, and Peer B. Jacobson
`
`Journal of Medicinal Chemistry  2004, 47, 17, 4213-4230 (Article)
`Publication Date (Web): July 13, 2004
`
` Abstract
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` Full text
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` PDF
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` ABSTRACT
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`Solution Structure of Amyloid β-Peptide (25−35) in Different Media
`
`Anna M. D'Ursi, Maria R. Armenante, Remo Guerrini, Severo Salvadori, Giuseppe Sorrentino, and Delia Picone
`
`Journal of Medicinal Chemistry  2004, 47, 17, 4231-4238 (Article)
`
`https://pubs.acs.org/toc/jmcmar/47/17
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`13/19
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`DR. REDDY’S LABORATORIES, INC.
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`3/13/23, 9:13 AM
`Publication Date (Web): July 21, 2004
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`Journal of Medicinal Chemistry | Vol 47, No 17
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` Abstract
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` Full text
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` PDF
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` ABSTRACT
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`Design, Synthesis, and Biological Evaluation of New Cyclic Disulde
`Decapeptides That Inhibit the Binding of AP-1 to DNA
`
`Keiichi Tsuchida, Hisaaki Chaki, Tadakazu Takakura, Junichi Yokotani, Yukihiko Aikawa, Shunichi Shiozawa, Hiroaki
`Gouda, and Shuichi Hirono
`
`Journal of Medicinal Chemistry  2004, 47, 17, 4239-4246 (Article)
`Publication Date (Web): July 21, 2004
`
` Abstract
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` Full text
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` PDF
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` ABSTRACT
`
`Concise Synthesis and Structure−Activity Relationships of Combretastatin A-4
`Analogues, 1-Aroylindoles and 3-Aroylindoles, as Novel Classes of Potent
`Antitubulin Agents
`
`Jing-Ping Liou, Yi-Ling Chang, Fu-Ming Kuo, Chun-Wei Chang, Huan-Yi Tseng, Chiung-Chiu Wang, Yung-Ning Yang, 
`Jang-Yang Chang, Shiow-Ju Lee, and Hsing-Pang Hsieh
`
`Journal of Medicinal Chemistry  2004, 47, 17, 4247-4257 (Article)
`Publication Date (Web): July 17, 2004
`
` Abstract
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` Full text
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` PDF
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` ABSTRACT
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`https://pubs.acs.org/toc/jmcmar/47/17
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`14/19
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`DR. REDDY’S LABORATORIES, INC.
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`Journal of Medicinal Chemistry | Vol 47, No 17
`
` 
`Three-Dimensional Quantitative Structure−Activity Relationship Analysis of a
`
`Set of Plasmodium falciparum Dihydrofolate Reductase Inhibitors Using a
`Pharmacophore Generation Approach
`
`Marco Daniele Parenti, Sara Pacchioni, Anna Maria Ferrari, and Giulio Rastelli
`
`Journal of Medicinal Chemistry  2004, 47, 17, 4258-4267 (Article)
`Publication Date (Web): July 16, 2004
`
` Abstract
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` Full text
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` PDF
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` ABSTRACT
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`2-(1-Adamantyl)-4-(thio)chromenone-6-carboxylic Acids:  Potent Reversible
`Inhibitors of Human Steroid Sulfatase
`
`Amarylla Horvath, Peter Nussbaumer, Barbara Wolff, and Andreas Billich
`
`Journal of Medicinal Chemistry  2004, 47, 17, 4268-4276 (Article)
`Publication Date (Web): July 9, 2004
`
` Abstract
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` Full text
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` PDF
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` ABSTRACT
`
`Phenoxyphenyl Pyridines as Novel State-Dependent, High-Potency Sodium
`Channel Inhibitors
`
`Bin Shao, Sam Victory, Victor I. Ilyin, R. Richard Goehring, Qun Sun, Derk Hogenkamp, Diane D. Hodges, Khondaker
`Islam, Deyou Sha, Chongwu Zhang, Phong Nguyen, Silvia Robledo, George Sakellaropoulos, and Richard B. Carter
`
`Journal of Medicinal Chemistry  2004, 47, 17, 4277-4285 (Article)
`Publication Date (Web): July 16, 2004
`
`https://pubs.acs.org/toc/jmcmar/47/17
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`15/19
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` ABSTRACT
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` Full text
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`Journal of Medicinal Chemistry | Vol 47, No 17
`
` 
`
`
`Identication of Structurally Diverse Growth Hormone Secretagogue Agonists
`by Virtual Screening and Structure−Activity Relationship Analysis of 2-
`Formylaminoacetamide Derivatives
`
`Miyuki Shoda, Takeo Harada, Yuji Kogami, Ryuichi Tsujita, Hirotada Akashi, Hiroyuki Kouji, Florence L. Stahura, Ling
`Xue, and Jürgen Bajorath
`
`Journal of Medicinal Chemistry  2004, 47, 17, 4286-4290 (Article)
`Publication Date (Web): July 13, 2004
`
` Abstract
`
` Full text
`
` PDF
`
` ABSTRACT
`
`Piperazine Derivatives of [1,2,4]Triazolo[1,5-a][1,3,5]triazine as Potent and
`Selective Adenosine A Receptor Antagonists
`2a
`
`Chi B. Vu, Bo Peng, Gnanasambandam Kumaravel, Glenn Smits, Xiaowei Jin, Deepali Phadke, Thomas Engber, 
`Carol Huang, Jennifer Reilly, Stacy Tam, Donna Grant, Gregg Hetu, Liqing Chen, Jianbo Zhang, and Russell C. Petter
`
`Journal of Medicinal Chemistry  2004, 47, 17, 4291-4299 (Article)
`Publication Date (Web): July 13, 2004
`
` Abstract
`
` Full text
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` PDF
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` ABSTRACT
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`https://pubs.acs.org/toc/jmcmar/47/17
`
`16/19
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`DR. REDDY’S LABORATORIES, INC.
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`3/13/23, 9:13 AM
`Journal of Medicinal Chemistry | Vol 47, No 17
`Fluorescent Pirenzepine Derivatives as Potential Bitopic Ligands of the Human
`M1 Muscarinic Receptor
` 
`
`Chouaib Tahtaoui, Isabelle Parrot, Philippe Klotz, Fabrice Guillier, Jean-Luc Galzi, Marcel Hibert, and Brigitte Ilien
`
`Journal of Medicinal Chemistry  2004, 47, 17, 4300-4315 (Article)
`Publication Date (Web): July 16, 2004
`
` Abstract
`
` Full text
`
` PDF
`
` ABSTRACT
`
`Tetramethylcyclopropyl Analogue of a Leading Antiepileptic Drug, Valproic
`Acid. Synthesis and Evaluation of Anticonvulsant Activity of Its Amide
`Derivatives
`
`Eyal Sobol, Meir Bialer, and Boris Yagen
`
`Journal of Medicinal Chemistry  2004, 47, 17, 4316-4326 (Article)
`Publication Date (Web): July 20, 2004
`
` Abstract
`
` Full text
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` PDF
`
` ABSTRACT
`
`Zinc Ion Dependent B-Cell Epitope, Associated with Primary Sjogren's
`Syndrome, Resides within the Putative Zinc Finger Domain of Ro60kD
`Autoantigen:  Physical and Immunologic Properties
`
`John G. Routsias, Aggeliki Kosmopoulou, Athina Makri, Eugenia Panou-Pomonis, Constantinos Sakarellos, Maria
`Sakarellos-Daitsiotis, Haralampos M. Moutsopoulos, and Athanasios G. Tzioufas
`
`Journal of Medicinal Chemistry  2004, 47, 17, 4327-4334 (Article)
`Publication Date (Web): July 17, 2004
`
`https://pubs.acs.org/toc/jmcmar/47/17
`
`17/19
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`DR. REDDY’S LABORATORIES, INC.
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` Full text
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`Journal of Medicinal Chemistry | Vol 47, No 17
`
` 
`
`
`3/13/23, 9:13 AM
` Abstract
`
` ABSTRACT
`
`BRIEF ARTICLES
`
`O-Alkoxyamidine Prodrugs of Furamidine:  In Vitro Transport and Microsomal
`Metabolism as Indicators of in Vivo Ecacy in a Mouse Model of Trypanosoma
`brucei rhodesiense Infection
`
`John H. Ansede, Mariappan Anbazhagan, Reto Brun, Judy D. Easterbrook, James Edwin Hall, and David W. Boykin
`
`Journal of Medicinal Chemistry  2004, 47, 17, 4335-4338 (Brief Article)
`Publication Date (Web): July 16, 2004
`
` Abstract
`
` Full text
`
` PDF
`
` ABSTRACT
`
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`https://pubs.acs.org/toc/jmcmar/47/17
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`3/13/23, 9:13 AM
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`Glucagon-like Peptide-1:  The Basis of a New Class of Treatment
`for Type 2 Diabetes
`Lotte Bjerre Knudsen
`
`View Author Information 
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` Cite this: J. Med. Chem. 2004, 47, 17, 4128–4134
`Publication Date: July 20, 2004
`
`https://doi.org/10.1021/jm030630m
`Copyright © 2004 American Chemical Society
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`Glucagon-like Peptide-1:  The Basis of a New Class of Treatment for Type 2 Diabetes | Journal of Medicinal Chemistry
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`Anatomy, Carbohydrates, 
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`Glucagon-like Peptide-1:  The Basis of a New Class of Treatment for Type 2 Diabetes | Journal of Medicinal Chemistry
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`†  Phone:  +45 44434788. Fax:  +45 44663939. E-mail:  lbkn@ novonordisk.com.
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`Glucagon-like Peptide-1:  The Basis of a New Class of Treatment for Type 2 Diabetes | Journal of Medicinal Chemistry
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