(S)-3-(4-(2-(5-Methyl-2-phenyloxazol-4-yl) ethoxy) phenyl)-2-(piperazin-1-yl) propanoic acid compounds: Synthesis and biological evaluation of dual PPARα/γ …

…, W Chen, C Xu, S Fan, Y Xie, W Zhong, L Wang…

Index: Zhou, Xinbo; Chen, Wei; Xu, Cheng; Fan, Shiyong; Xie, Yunde; Zhong, Wu; Wang, Lili; Li, Song Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 8 p. 2605 - 2608

Full Text: HTML

Citation Number: 1

Abstract

A series of novel, potent PPARα/γ dual agonists were synthesized and appraised. The most potent analogue, compound 2b demonstrated EC50 value of 0.012±0.002 and 0.032±0.01 μM, respectively, for hPPARα and hPPARγ in transactivation assay. Additionally, compound 2b demonstrated good glucose and lipid lowering effect in genetic diabetic (db/db) mice.