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

页码：377 / 385

页数：9

共 29 条

[11]

FONTAINE G, 1964, CR HEBD ACAD SCI, P4583

[12]

FREEDMAN J, 1989, J HETEROCYCLIC CHEM, V26, P1547

[13] REGULATION OF ACYL-COA - CHOLESTEROL ACYLTRANSFERASE ACTIVITY IN NORMAL AND ATHEROSCLEROTIC RABBIT AORTAS - ROLE OF A CHOLESTEROL SUBSTRATE POOL [J].