New indole derivatives as ACAT inhibitors: Synthesis and structure-activity relationships

被引：11

作者：

Bellemin, R ^{[1
]}

Decerprit, J ^{[1
]}

Festal, D ^{[1
]}

机构：

[1] LIPHA RES & DEV CTR,F-69003 LYON,FRANCE

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1996年 / 31卷 / 02期

关键词：

indole derivative; aortic ACAT inhibition; intestinal ACAT inhibition; hypocholesterolaemic effect;

D O I：

10.1016/0223-5234(96)80445-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of ureas containing the indole group were synthesized and assessed for their ability to inhibit arterial and intestinal ACAT and to lower plasma total cholesterol in a cholesterol-fed rat model. The structural modulations carried out in this series led to compounds which proved to be very active in both the inhibition of aortic ACAT in vitro and the inhibition of rat cholesterol intestinal absorption in vivo. Several compounds from this series exhibit a remarkable hypocholesterolaemic effect with ED(25) less than 0.1 mg/kg po.

引用

页码：123 / 132

页数：10

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