title: Discovery of gemfibrozil analogues that activate PPARα and enhance the expression of gene CPT1A involved in fatty acids catabolism.
abstract: A new series of gemfibrozil analogues conjugated with α-asarone, trans-stilbene, chalcone, and their bioisosteric modifications were synthesized and evaluated to develop PPARα agonists. In this attempt, we have removed the methyls on the phenyl ring of gemfibrozil and introduced the above scaffolds in para position synthesizing two series of derivatives, keeping the dimethylpentanoic skeleton of gemfibrozil unaltered or demethylated. Four compounds exhibited good activation of the PPARα receptor and were also screened for their activity on PPARα-regulated gene CPT1A.
authors: Dipartimento di Scienze del Farmaco, Università degli Studi G. d'Annunzio, Chieti, Italy.
authors: Barbara
authors: B
authors: De Filippis
authors: Antonella
authors: A
authors: Giancristofaro
authors: Alessandra
authors: A
authors: Ammazzalorso
authors: Alessandra
authors: A
authors: D'Angelo
authors: Marialuigia
authors: M
authors: Fantacuzzi
authors: Letizia
authors: L
authors: Giampietro
authors: Cristina
authors: C
authors: Maccallini
authors: Michele
authors: M
authors: Petruzzelli
authors: Rosa
authors: R
authors: Amoroso
mesh_terms: D002334:Carnitine O-Palmitoyltransferase / Q000235:genetics*; D005227:Fatty Acids / Q000378:metabolism*; D015248:Gemfibrozil / Q000031:analogs & derivatives* / Q000494:pharmacology*; D056945:Hep G2 Cells; D006801:Humans; D047493:PPAR alpha / Q000819:agonists* / Q000378:metabolism*; D015854:Up-Regulation / Q000187:drug effects
chemical_list: D005227:Fatty Acids; D047493:PPAR alpha; D002334:Carnitine O-Palmitoyltransferase; D015248:Gemfibrozil