(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.

Article Details

Citation

Zhou X, Chen W, Xu C, Fan S, Xie Y, Zhong W, Wang L, Li S

(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. Epub 2010 Mar 1.

PubMed ID
20299214 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
RosiglitazonePeroxisome proliferator-activated receptor alphaEC 50 (nM)10580N/AN/ADetails
RosiglitazonePeroxisome proliferator-activated receptor gammaEC 50 (nM)35N/AN/ADetails