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.

合成了一系列新型喹唑啉-4(3H)-one 衍生物 ( 4a-4j )，并筛选了它们对革兰氏阳性菌株（枯草芽孢杆菌、金黄色葡萄球菌和化脓性链球菌）和革兰氏阳性菌的体外抗菌活性。阴性菌株（大肠杆菌、肺炎克雷伯菌、鼠伤寒沙门氏菌）和抗真菌黑曲霉、白色念珠菌、黄曲霉（真菌）。化合物4c已被确定为有效的抗微生物剂。还研究了所有合成的化合物对 MTB H37Rv 的体外抗结核活性。化合物4C和4 克被鉴定为有效的抗结核药物，MIC 值分别为 0.78 μM 和 1.56 μM。此外，在分子对接研究期间获得的数据对于这些化合物的潜在利用非常令人鼓舞，以帮助克服微生物对药物的耐药性，如本手稿中明确指出的。