Synthesis and anti-inflammatory and antimicrobial activities of some novel 2-methylquinazolin-4(3H)-one derivatives bearing urea,thiourea and sulphonamide functionalities |
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Institution: | 1. Department of Chemistry, Udaygiri Mahavidayla, Udgir, India;2. Department of Chemistry, The Institute of Science Bombay, India |
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Abstract: | 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-α 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-α and 73–92% IL-6 inhibitory activity) at concentration of 10 μM with reference to standard dexamethasone (75% TNF-α and 84% IL-6 inhibitory activities at 1 μM) and 7, 10, 12, 23, 25 and 28 have antimicrobial activity at MIC of 10–30 μg/mL against selected pathogenic bacteria and fungi.” |
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Keywords: | 2-Methylquinazolin-4(3H)-one Urea Thiourea Sulphonamide derivatives Anti-inflammatory Antimicrobial activity |
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