Some novel compounds of 3-[3-chloro-2-(4-sustituted)-4-oxoazetidin-1-yl] 2-phenyl disubstituted quinazolin-4(3H)-one, 3-{[2-(3-chloro-4-substituted 2-oxoazetidin-1-yl)-1,3-thiazol-4-yl] amino}-2-phenyl disubstituted quinazolin-4(3H)-one were screened for their antifungal activity against fungi Candida albicans. These compounds have showed moderate and very good antifungal activity. The quantitative structure activity-relationships (QSAR) study on the quinazolin-4(3H)-one series was made using lipophilic, electronic and steric parameters. Several statistical expressions were developed and best models were validated. The studies confirm that the antifungal activity is dependent on selected lipophilic and electronic parameters. The study suggests that substitution on R1 group with increasing lipophilic nature and decreasing electronic factor favorable for antifungal activity. The QSAR study provides important structural insights in designing of potent antifungal agents.
Loading....