Synthesis and structure-activity relationships of fibrate-based analogues inside PPARs

Letizia Giampietro; Alessandra D'Angelo; Antonella Giancristofaro; Alessandra Ammazzalorso; Barbara De Filippis; Marialuigia Fantacuzzi; Pasquale Linciano; Cristina Maccallini; Rosa Amoroso

doi:10.1016/j.bmcl.2012.09.111

Synthesis and structure-activity relationships of fibrate-based analogues inside PPARs

Bioorg Med Chem Lett. 2012 Dec 15;22(24):7662-6. doi: 10.1016/j.bmcl.2012.09.111. Epub 2012 Oct 6.

Authors

Letizia Giampietro¹, Alessandra D'Angelo, Antonella Giancristofaro, Alessandra Ammazzalorso, Barbara De Filippis, Marialuigia Fantacuzzi, Pasquale Linciano, Cristina Maccallini, Rosa Amoroso

Affiliation

¹ Dipartimento di Farmacia, Università degli Studi G. d'Annunzio, via dei Vestini 31, 66100 Chieti, Italy.

PMID: 23102891
DOI: 10.1016/j.bmcl.2012.09.111

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Clofibrate / chemical synthesis
Clofibrate / chemistry
Clofibrate / pharmacology*
Dose-Response Relationship, Drug
HEK293 Cells
Humans
Molecular Structure
PPAR alpha / agonists*
PPAR gamma / agonists*
Structure-Activity Relationship

Substances

PPAR alpha
PPAR gamma
Clofibrate