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

[ Vol. 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   Pages 59 - 65 ( 7 )

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 PPAR α better than clofibric acid.

Keywords:

PPARs, clofibrate, chalcone, stilbene, transactivation assay.

Affiliation:

Dipartimento di Farmacia, Università di Chieti, via dei Vestini, 66100 Chieti, Italy.



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