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

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

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  • 1Dipartimento 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.

Copyright © 2012 Elsevier Ltd. All rights reserved.

PMID:
23102891
[PubMed - indexed for MEDLINE]

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