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The action of the hypoglycemic compounds, tolbutamide, chlorpropamide, metahexamide, and phenethylbigu anide, on the biosynthesis of cholesterol has been investigated in vitro with both acetate-l-C14 and mevalonate-2-C14. The results show that the incorporation of acetate-l-C14 and mevalonate-2-C14 into cholesterol is inhibited by all compounds studied. The maximal inhibition occurs when the concentration of hypoglycemic compound is 4 X 10 ~3 m. It has been found that the inhibition of cholesterol biosynthesis by phenethylbigu anide takes place between isopentenyl pyrophosphate and the formation of squalene. The inhibition of cholesterol biosynthesis by the arylsulfonylurea compounds, on the other hand, takes place after the formation of squalene.

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