2. Academic Validation
  3. (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 PPARalpha/gamma agonists

(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 PPARalpha/gamma agonists

  • Bioorg Med Chem Lett. 2010 Apr 15;20(8):2605-8. doi: 10.1016/j.bmcl.2010.02.071.
Xinbo Zhou 1,  Wei Chen,  Cheng Xu,  Shiyong Fan,  Yunde Xie,  Wu Zhong,  Lili Wang,  Song Li
Affiliations

Affiliation

  • 1 Beijing Institute of Pharmacology and Toxicology, Beijing 100850, PR China.
PMID: 20299214 DOI: 10.1016/j.bmcl.2010.02.071
Abstract

A series of novel, potent PPARalpha/gamma dual agonists were synthesized and appraised. The most potent analogue, compound 2b demonstrated EC(50) value of 0.012+/-0.002 and 0.032+/-0.01 microM, respectively, for hPPARalpha and hPPARgamma in transactivation assay. Additionally, compound 2b demonstrated good glucose and lipid lowering effect in genetic diabetic (db/db) mice.

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