Inhibitors of acyl CoA:cholesterol acyltransferase

被引：32

作者：

Vaccaro, W

Amore, C

Berger, J

Burrier, R

Clader, J

Davis, H

Domalski, M

Fevig, T

Salisbury, B

Sher, R

机构：

[1] Schering-Plough Research Institute, Kenilworth, NJ 07033-0539

[2] Hoechst Marion Roussel Inc., Cincinnati, OH 45215

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1996年 / 39卷 / 08期

关键词：

D O I：

10.1021/jm950833d

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

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 mo st potent ACAT inhibitor identified (IC50 = 0.04 mu M in an in vitro rat hepatic microsomal ACAT assay, ED(50) = 0.72 mg/kg/day in cholesterol-fed hamsters).

引用

页码：1704 / 1719

页数：16

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