The Synthesis and Biological Evaluation of 2-(1-Indol-3-yl)quinazolin-4(3)-One Derivatives.

The treatment of many bacterial diseases remains a significant problem due to the increasing antibiotic resistance of their infectious agents. Among others, this is related to , especially methicillin-resistant (MRSA) and . In the present article, we report on antibacterial compounds with activity against both and MRSA. A straightforward approach to 2-(1-indol-3-yl)quinazolin-4(3)-one and their analogues was developed. Their structural and functional relationships were also considered. The antimicrobial activity of the synthesized compounds against HRv, ATCC 25923, MRSA ATCC 43300, ATCC 10231, and their role in the inhibition of the biofilm formation of were reported. 2-(5-Iodo-1-indol-3-yl)quinazolin-4(3)-one () showed a low minimum inhibitory concentration (MIC) of 0.98 μg/mL against MRSA. The synthesized compounds were assessed via molecular docking for their ability to bind long RSH (RelA/SpoT homolog) proteins using mycobacterial and streptococcal (p)ppGpp synthetase structures as models. The cytotoxic activity of some synthesized compounds was studied. Compounds , , , , , and 3 displayed significant antiproliferative activities against all the cancer cell lines tested. Indolylquinazolinones , , and showed a preferential suppression of the growth of rapidly dividing A549 cells compared to slower growing fibroblasts of non-tumor etiology.