Effect of Stilbene and Chalcone Scaffolds Incorporation in Clofibric Acid on PPARα  Agonistic Activity

Author(s): Letizia Giampietro, Alessandra D’Angelo, Antonella Giancristofaro, Alessandra Ammazzalorso, Barbara De Filippis, Mauro DiMatteo, Marialuigia Fantacuzzi, Pasquale Linciano, Cristina Maccallini, Rosa Amoroso.

Journal Name: Medicinal Chemistry

Volume 10 , Issue 1 , 2014

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Abstract:

In an effort to develop safe and efficacious compounds for the treatment of metabolic disorders, new compounds based on a combination of clofibric acid, the active metabolite of clofibrate, and trans-stilbene, chalcone, and other lipophilic groups were synthesized. They were evaluated for PPARα transactivation activity; all branched derivatives showed an increase of the transcriptional activity of receptor compared to the linear ones. Noteworthy, stilbene and benzophenone branched derivatives activated the PPARα better than clofibric acid.

Keywords: PPARs, clofibrate, chalcone, stilbene, transactivation assay.

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Article Details

VOLUME: 10
ISSUE: 1
Year: 2014
Page: [59 - 65]
Pages: 7
DOI: 10.2174/157340641001131226123613

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