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.
Synthesis and structure-activity relationships of fibrate-based analogues inside PPARs
GIAMPIETRO, Letizia;D'ANGELO, ALESSANDRA;GIANCRISTOFARO, ANTONELLA;AMMAZZALORSO, Alessandra;DE FILIPPIS, Barbara;FANTACUZZI, MARIALUIGIA;LINCIANO, PASQUALE;MACCALLINI, Cristina;AMOROSO, Rosa
2012-01-01
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.File in questo prodotto:
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