Synthesis of 2-(2-oxo-2H-chromen-3-yl)-3-phenylquinazolin-4(3H)-ones as potent antimicrobial and antitubercular agents

Abstract

A series of novel quinazolin-4(3H)-one derivatives ( 4a-4j ) were synthesized and were screened for their in vitro antibacterial activity against Gram-positive bacterial strains (Bacillus subtilis, Staphylococcus aureus, and Streptococcus pyogenes), and Gram-negative bacterial strains (Escherichia coli, Klebsiella pneumonia, S. typhimurium) and antifungal against Aspergillus niger, Candida albicans, Aspergillus flavus (Fungi). The compound 4c has been identified as potent antimicrobial agent. All the synthesized compounds were also studied for their In vitro antitubercular activity against MTB H37Rv. Compounds 4c and 4 g were identified as potent antitubercular agent with MIC value 0.78 μM and 1.56 μM. Additionally, data obtained during molecular docking studies are very encouraging with respect to potential utilization of these compounds to help overcome microbe resistance to pharmaceutical drugs, as clearly noted in this manuscript.