Biological Evaluation and Molecular Docking of Substituted Quinazolinones as Antimicrobial Agents

Antibiotic resistance in the community is a growing public health concern due to the continued emergence of multi drug resistant bacterial strains. In view of this fact, the design and synthesis of newer antibacterials are of immense significance and continue to attract the attention of numerous medicinal chemists. The aim of this study was to investigate the effect of four quinazolinone derivatives (Ia, II, III and IV) on the microbial cell morphology and genes coded for rRNA subunits. It was extended also to elucidate the effect of the most active derivatives on DNA-gyrase enzyme by performing a molecular docking study. Quinazolinone derivatives revealed good anti-bacterial activities, especially against Gram-positive strains through their interaction with cell wall and DNA structures. The tested compounds showed moderate activity against fungal strains through affecting the internal structures of fungal cell in addition to studied genes. Compound II was found to be the most active gyrase inhibitor as illustrated by the docking study. Conclusion: the type and position of chemical substituents confer the antimicrobial activity of quinazolinone.