Polyunsaturated fatty acid anilides as inhibitors of acyl-CoA:cholesterol acyltransferase (ACAT)
作者:Naoto Matsuyama、Tetsuya Kosaka、Mina Fukuhara、Yasuji Soda、Koji Mizuno
DOI:10.1016/s0960-894x(99)00330-3
日期:1999.7
series of polyunsaturated fatty acid anilides were synthesized and evaluated as ACAT inhibitors. Compound 24 had potent inhibitory activity against microsomal ACAT derived from U937, HepG2 and Caco-2 cell lines. Therefore, it might be expected to act as an antiarteriosclerotic and hypocholesterolemic agent. Interestingly, the ACAT inhibitory potency of 24 varied significantly depending on the source of the
合成了一系列多不饱和脂肪酸酐,并作为ACAT抑制剂进行了评估。化合物24对源自U937,HepG2和Caco-2细胞系的微粒体ACAT具有有效的抑制活性。因此,可以预期它起着抗动脉硬化和降血脂药的作用。有趣的是,根据酶的来源,ACAT的抑制力为24,差异很大。