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 )
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.
PPARs, clofibrate, chalcone, stilbene, transactivation assay.
Dipartimento di Farmacia, Università di Chieti, via dei Vestini, 66100 Chieti, Italy.