alexa Role of alkyl substitution in 2,3-disubstituted and 3-substituted 4-quinazolones on the inhibition of pyruvic acid oxidation
Microbiology

Microbiology

Journal of Chemical Biology & Therapeutics

Author(s): Parmar SS, Kishor K, Seth PK, Arora RC

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Several 2,3-disubstituted and 3-substituted 4-quinazolones have been synthesized to investigate structure-activity relationship of these quinazolones with respect to their ability to inhibit pyruvic acid oxidation by rat brain homogenate. 2-Methyl-3-(o-tolyl)-4-quinazolone was used for comparison. In general 2,3-disubstituted quinazolones exhibited greater inhibitory properties as compared to the coresponding 3-substituted quinazolones Introduction of the alkyl substituent(s) on the phenyl nucleus, attached to the 3 position of the quinazolone molecule, significantly influenced the enzyme inhibitory properties of these quinazolones. In both series, maximum inhibition of the oxidation of pyruvic acid was observed with quinazolones synthesized from 2,4-dimethylaniline. Increase in the concentration of the quinazolones simultaneously increased the enzyme inhibition Added NAD, responsible for the increase in the respiratory activity of brain homogenate during oxidation of pyruvic acid, reduced the inhibition produced by 2,3-disubstituted and 3-substituted 4-quinazolones.

This article was published in J Med Chem and referenced in Journal of Chemical Biology & Therapeutics

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