4.5 Article

Pyridine-2-propanoic acids:: Discovery of dual PPARα/γ agonists as antidiabetic agents

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 16, 期 23, 页码 6116-6119

出版社

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.08.105

关键词

PPAR; diabetes; parallel synthesis; SAR; pharmacokinetic studies; in vivo efficacy

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A series of novel pyridine-2-propanoic acids was synthesized. A structure-activity relationship study of these compounds led to the identification of potent dual PPAR alpha/gamma agonists with varied isoform selectivity. Based on the results of efficacy studies in diabetic (db/db) mice, and the desired pharmacokinetic parameters, compound (S)-13 was selected for further profiling. (c) 2006 Elsevier Ltd. All rights reserved.

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