title: Synthesis and structure-activity relationships of fibrate-based analogues inside PPARs.
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.
authors.affiliation: Dipartimento di Farmacia, Università degli Studi G. d'Annunzio, via dei Vestini 31, 66100 Chieti, Italy.
authors.forename: Letizia
authors.initials: L
authors.lastname: Giampietro
authors.forename: Alessandra
authors.initials: A
authors.lastname: D'Angelo
authors.forename: Antonella
authors.initials: A
authors.lastname: Giancristofaro
authors.forename: Alessandra
authors.initials: A
authors.lastname: Ammazzalorso
authors.forename: Barbara
authors.initials: B
authors.lastname: De Filippis
authors.forename: Marialuigia
authors.initials: M
authors.lastname: Fantacuzzi
authors.forename: Pasquale
authors.initials: P
authors.lastname: Linciano
authors.forename: Cristina
authors.initials: C
authors.lastname: Maccallini
authors.forename: Rosa
authors.initials: R
authors.lastname: Amoroso
mesh_terms: D002994:Clofibrate / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D057809:HEK293 Cells; D006801:Humans; D015394:Molecular Structure; D047493:PPAR alpha / Q000819:agonists*; D047495:PPAR gamma / Q000819:agonists*; D013329:Structure-Activity Relationship
chemical_list: D047493:PPAR alpha; D047495:PPAR gamma; D002994:Clofibrate