(S)-3-(4-(2-(5-Methyl-2-phenyloxazol-4-yl)ethoxy)phenyl)-2-(pipera zin-1-yl)propanoic acid compounds: Synthesis and biological evaluation of dual PPARa/g agonists

A series of novel, potent PPARa/g dual agonists were synthesized and appraised. The most potent analogue, compound 2b demonstrated EC sub(50) value of 0.012 +/- 0.002 and 0.032 +/- 0.01 kM, respectively, for hPPARa and hPPARg in transactivation assay. Additionally, compound 2b demonstrated good gluc...

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Published inBioorganic & medicinal chemistry letters Vol. 20; no. 8; pp. 2605 - 2608
Main Authors Zhou, Xinbo, Chen, Wei, Xu, Cheng, Fan, Shiyong, Xie, Yunde, Zhong, Wu, Wang, Lili, Li, Song
Format Journal Article
LanguageEnglish
Published 15.04.2010
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Summary:A series of novel, potent PPARa/g dual agonists were synthesized and appraised. The most potent analogue, compound 2b demonstrated EC sub(50) value of 0.012 +/- 0.002 and 0.032 +/- 0.01 kM, respectively, for hPPARa and hPPARg in transactivation assay. Additionally, compound 2b demonstrated good glucose and lipid lowering effect in genetic diabetic (db/db) mice.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
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ISSN:0960-894X
DOI:10.1016/j.bmcl.2010.02.071