A new class of potent hypolipemic agents raising high-density lipoproteins. Synthesis, reactions and pharmacological properties
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.
A new class of potent hypolipemic agents raising high-density lipoproteins. Synthesis, reactions and pharmacological properties
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.
A new class of potent hypolipemic agents raising high-density lipoproteins. Synthesis, reactions and pharmacological properties
作者:H FURRER、E GRANZER、R WAGNER
DOI:10.1016/0223-5234(94)90105-8
日期:——
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.