SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF NEW ACAT INHIBITORS

被引：9
|
作者：
NIOCHE, JY [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 | 1995年 / 30卷 / 05期
关键词：
AORTIC ACAT; INTESTINAL INHIBITION; BENZOXEPIN; UREA; CHOLESTEROL; HYPOCHOLESTEROLEMIC;
D O I：
10.1016/0223-5234(96)88247-X
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of heterocyclic ureas were synthesized and their ability to inhibit arterial and intestinal ACAT was assessed in animals. The structural modifications carried out in this series led to N-2-(2,4-difluorophenyl)-N-1-8-(4-fluorophenyl)-2,3,4,5-tetrahydro-1-benzoxepin-5-yl-N-1-n-heptylurea 21, which proved to be very active on both the inhibition of aortic ACAT and the inhibition of rat cholesterol intestinal absorption, thus exhibiting a strong hypocholesterolemic effect po in the rat (ED(25) = 0.2 mg/kg).
引用
收藏
页码：377 / 385
页数：9
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