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

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Giampietro L, D'Angelo A, Giancristofaro A, Ammazzalorso A, De Filippis B, Fantacuzzi M, Linciano P, Maccallini C, Amoroso R

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.

PubMed ID

23102891 [ View in PubMed

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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 PPARalpha or PPARgamma, while others were identified as dual agonists PPARalpha/gamma.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Pioglitazone	Peroxisome proliferator-activated receptor gamma	EC 50 (nM)	800	N/A	N/A	Details