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

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

Volume: 10 Issue: 1

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

Affiliation:

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

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.

Cite this article as:

Giampietro Letizia, D’Angelo Alessandra, Giancristofaro Antonella, Ammazzalorso Alessandra, Filippis De Barbara, DiMatteo Mauro, Fantacuzzi Marialuigia, Linciano Pasquale, Maccallini Cristina and Amoroso Rosa, Effect of Stilbene and Chalcone Scaffolds Incorporation in Clofibric Acid on PPARα Agonistic Activity, Medicinal Chemistry 2014; 10 (1) . https://dx.doi.org/10.2174/157340641001131226123613