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

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 mark ed 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 -9 8%. These effects may result in antiatherosclerotic properties in thes e compounds. The preparation of 7-amino-2,3-dihydrothiazolo[3,2-a]pyri midin-5-ones and 5-amino-2,3-dihydrothiazolo[3,2-a] pyrimidin-7-ones i s described.