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目的以C75为先导化合物,设计、合成γ-丁内酯类衍生物,并研究其脂肪酸合成酶(fatty acid syn-thase,FAS)的抑制活性,以期发现新颖的FAS抑制剂。方法以衣康酸酐为起始原料,经酯化、烃代、缩合/环合、水解4步反应合成目标化合物,采用体外方法初步筛选其FAS的抑制作用。结果与结论合成了11个目标化合物,其结构经核磁和质谱确证;初步活性评价结果显示,含饱和烷烃侧链的化合物具有较好的FAS抑制活性,随侧链烷基的延长,其抑酶活性有增强的趋势。
OBJECTIVE To design and synthesize γ-butyrolactone derivatives with C75 as the lead compound and study its inhibitory activity of fatty acid syn-thase (FAS) in order to find a novel FAS inhibitor. Methods Itaconic anhydride was used as starting material to synthesize target compounds by esterification, hydrocarbon substitution, condensation / cyclization and hydrolysis. The inhibitory effect of FAS was screened by in vitro method. RESULTS AND CONCLUSIONS Eleven target compounds were synthesized and their structures were confirmed by NMR and MS. The preliminary activity evaluation showed that the compounds containing saturated alkane side chains had good FAS inhibitory activity. With the extension of side chain alkyl groups, Activity has an increasing trend.