Abstract
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.
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