A NEW CLASS OF POTENT HYPOLIPEMIC AGENTS RAISING HIGH-DENSITY-LIPOPROTEINS - SYNTHESIS, REACTIONS AND PHARMACOLOGICAL PROPERTIES

被引：11

作者：

FURRER, H ^{[1
]}

GRANZER, E ^{[1
]}

WAGNER, R ^{[1
]}

机构：

[1] HOECHST AG,PRECLIN RES,PHARMACOL,D-65926 FRANKFURT,GERMANY

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1994年 / 29卷 / 11期

关键词：

THIAZOLOPYRIMIDINE; HDL CHOLESTEROL ENHANCEMENT; LDL CHOLESTEROL REDUCTION; LIPID MODULATION;

D O I：

10.1016/0223-5234(94)90105-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of thiazolo[3,2-c]pyrimidin-5,7-diones has been synthesized. Results from in vivo evaluations in rats have shown that many of these compounds produce a pronounced increase of HDL cholesterol and a marked decrease of LDL and VLDL cholesterol. The most potent compound 17 (30 mg/kg/d per os over 7 d in male rats) led to the following changes: HDL cholesterol + 101%, LDL cholesterol -40%, and VLDL cholesterol -98%. These effects may result in antiatherosclerotic properties in these compounds. The preparation of 7-amino-2,3-dihydrothiazolo[3,2-a]pyrimidin-5-ones and 5-amino-2,3-dihydrothiazolo[3,2-a] pyrimidin-7-ones is described.

引用

页码：819 / 829

页数：11

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