Zh. Sui et al., SYNTHESIS OF 2-SUBSTITUTED 4-QUINAZOLONE-5-CARBOXYLIC ACIDS AS INHIBITORS OF DNA-GYRASE, Journal of heterocyclic chemistry, 34(1), 1997, pp. 153-156
A series of 4-quinazolone-5-carboxylic acids were designed as bacteria
l DNA gyrase inhibitors. The syntheses of the target compounds were ac
complished by reacting 3-aminophthalimide with aroyl chlorides followe
d by rearrangement of the resulting 3-acylaminophthalimides under basi
c conditions. The designed compounds showed moderate DNA gyrase inhibi
tory activity.