Synthesis and anti-inflammatory and antimicrobial activities of some novel 2-methylquinazolin-4(3H)-one derivatives bearing urea, thiourea and sulphonamide functionalities

A variety of novel 2-methylquinazolin-4(3H)-one derivatives (1-29) bearing urea, thiourea and sulphonamide functionalities at position 3 of biological interest have been synthesized and screened for their anti-inflammatory (TNF-alpha and IL-6) and antimicrobial activities (antibacterial and antifungal). Biological evaluation study revealed that the compounds 3, 4, 6, 9, 16 and 18 were found to have promising anti-inflammatory activity (up to 62-84% TNF-alpha and 73-92% IL-6 inhibitory activity) at concentration of 10 mu M with reference to standard dexamethasone (75% TNF-alpha and 84% IL-6 inhibitory activities at 1 mu M) and 7, 10, 12, 23, 25 and 28 have antimicrobial activity at MIC of 10-30 mu g/mL against selected pathogenic bacteria and fungi.'' (C) 2014 Production and hosting by Elsevier B.V. on behalf of King Saud University.