Dipartimento di Farmacia, Università degli Studi G. d'Annunzio, via dei Vestini 31, 66100 Chieti, Italy.
Bioorg Med Chem Lett. 2012 Dec 15;22(24):7662-6. doi: 10.1016/j.bmcl.2012.09.111. Epub 2012 Oct 6.
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.
为了开发治疗代谢紊乱的安全有效的化合物，研究人员合成了基于氯贝酸（氯贝特的活性代谢物）与天然产物查尔酮和芪的亲脂基团组合的新化合物。其中一些化合物仅在微摩尔浓度下对 PPARα 或 PPARγ 具有活性，而另一些则被鉴定为 PPARα/γ 双重激动剂。
