Inhibitors of acyl CoA: cholesterol acyltransferase

…, R Burrier, J Clader, H Davis, M Domalski…

文献索引：Vaccaro, Wayne; Amore, Cindy; Berger, Joel; Burrier, Robert; Clader, John; Davis, Harry; Domalski, Martin; Fevig, Tom; Salisbury, Brian; Sher, Rosy Journal of Medicinal Chemistry, 1996 , vol. 39, # 8 p. 1704 - 1719

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被引用次数: 49

摘要

Conformational restriction of previously disclosed acyclic diphenylethyl) diphenylacetamides led to the discovery of several potent inhibitors of acyl CoA: cholesterol acyltransferase (ACAT). cis-[2-(4-Hydroxyphenyl)-1-indanyl] diphenylacetamide (4a) was the most potent ACAT inhibitor identified (IC50= 0.04 μM in an in vitro rat hepatic microsomal ACAT assay, ED50= 0.72 mg/kg/day in cholesterol-fed hamsters).