Synthetic Inhibitors of Alcohol Dehydrogenase. 4-Substituted Alkyl- and Cycloalkylpyrazoles.

Abstract

A series of pyrazoles substituted with alkyl or cycloalkyl groups in the 4-position was synthesized and tested for ability to inhibit the activity of the enzyme [human] liver alcohol dehydrogenase. The new pyrazoles were very strong inhibitors. Their activity seemed to be correlated to the lipophilicity of the substituent. The inhibitory power increased by a factor of about 2 for each methylene group that was added to an unbranched chain. Branching or cyclization of the chain lowered the activity. [Inhibitors of enzyme liver alcohol dehydrogenase (LADH) may be used to combat the ill effects of alcohol abuse in man.].