"PPARγ,激动剂二氢茚酮类衍生物的设计、合成与活性研究"

Design, synthesis, and PPARγ agonistic activity of novel indenone derivatives

过氧化物酶增殖因子活化受体γ(PPARγ)是用于治疗II型糖尿病的重要靶蛋白,二氢茚酮是一类非噻唑烷二酮类PPARγ激动剂。本文在已有二氢茚酮类化合物的基础上,设计合成了一系列新化合物并通过1H NMR和MS对其结构进行鉴定。活性结果显示,17b和19的激动活性明显高于对照品罗格列酮。

Agonists of peroxisome proliferator-activated receptor 7 （PPARy） are of interest as a treatment of type II diabetes, and indenone derivatives are a new class of non-TZD PPAR y agonists. Based on existing indenone derivatives, a series of novel ones have been designed and synthesized. Meanwhile the structures have been comfirmed with 1H NMR and MS. Among them, 17b and 19 showed higher agonistic activities than rosiglitazone.