Abstract
A novel series of 6,7-dihydro-4H-pyrazolo[1,5-a]pyrrolo[3,4-d]pyrimidine-5,8-dione inhibitors of the enzyme acyl-CoA:cholesterol O-acyltransferase is described. A number of these derivatives were found to be potent modulators of serum lipoprotein levels in cholesterol-fed rats. Further evaluation of one of the most effective analogues confirmed that it was significantly blocking the absorption of cholesterol from the gut.
MeSH terms
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Animals
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Anticholesteremic Agents / chemical synthesis*
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Anticholesteremic Agents / pharmacology
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Chemical Phenomena
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Chemistry
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Cholesterol / blood
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Cholesterol / metabolism
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Male
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Pyrimidinones / chemical synthesis*
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Pyrimidinones / pharmacology
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Rats
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Rats, Inbred Strains
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Sterol O-Acyltransferase / antagonists & inhibitors*
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Structure-Activity Relationship
Substances
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Anticholesteremic Agents
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Pyrimidinones
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Cholesterol
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Sterol O-Acyltransferase