Abstract
A series of 2-substituted thieno(2,3-d)pyrimidin-4-(3H) ones (1-15) was prepared by the reaction of thiophene ortho-aminoester (IV) with a variety of nitriles (V) under acidic conditions, and screened for antihyperlipaemic activity in various animal models. While most of these compounds were found active, 2-chloromethyl-5,6,7,8-tetrahydrobenzo(b)thieno(2,3-d) pyrimidin-4(3H)-one (5) was found to be the most active of all. The serum triglyceride lowering activity exhibited by 5 was found comparable to that of clofibrate and riboflavin tetrabutyrate. Compound 5 was also found to be safe as indicated by acute and chronic toxicity studies in mice and rats.
MeSH terms
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Animals
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Chemical Phenomena
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Chemistry
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Cholesterol, Dietary / pharmacology
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Ethanol
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Female
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Guinea Pigs
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Hypercholesterolemia / prevention & control
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Hyperlipidemias / chemically induced
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Hyperlipidemias / prevention & control
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Hypolipidemic Agents / chemical synthesis*
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Hypolipidemic Agents / toxicity
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Indicators and Reagents
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Lethal Dose 50
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Lipids / blood
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Male
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Mice
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Pyrimidinones / chemical synthesis*
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Pyrimidinones / pharmacology
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Pyrimidinones / toxicity
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Rabbits
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Rats
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Rats, Inbred Strains
Substances
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Cholesterol, Dietary
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Hypolipidemic Agents
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Indicators and Reagents
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Lipids
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Pyrimidinones
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Ethanol
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2-chloromethyl-5,6,7,8-tetrahydrobenzo(b)thieno(2,3-d)pyrimidin-4(3H)-one