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Synthesis and structure–activity relationships of fibrate-based analogues inside PPARs
Authors:Letizia Giampietro  Alessandra D’Angelo  Antonella Giancristofaro  Alessandra Ammazzalorso  Barbara De Filippis  Marialuigia Fantacuzzi  Pasquale Linciano  Cristina Maccallini  Rosa Amoroso
Institution:Dipartimento di Farmacia, Università degli Studi ‘G. d’Annunzio’, via dei Vestini 31, 66100 Chieti, Italy
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 lipophilic groups derived from natural products chalcone and stilbene were synthesised. Some of them were found to be active at micromolar concentrations only on PPARα or PPARγ, while others were identified as dual agonists PPARα/γ.
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