Synthesis and anti-inflammatory and antimicrobial activities of some novel 2-methylquinazolin-4(3H)-one derivatives bearing urea, thiourea and sulphonamide functionalities
نویسندگان
چکیده
2-Methylquinazolin-4(3H)one; Urea; Thiourea; Sulphonamide derivatives; Anti-inflammatory; Antimicrobial activity 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-a 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-a and 73–92% IL-6 inhibitory activity) at concentration of 10 lM with reference to standard dexamethasone (75% TNF-a and 84% IL-6 inhibitory activities at 1 lM) and 7, 10, 12, 23, 25 and 28 have antimicrobial activity at MIC of 10–30 lg/mL against selected pathogenic bacteria and fungi.’’ a 2014 Production and hosting by Elsevier B.V. on behalf of King Saud University. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/3.0/).
منابع مشابه
Design, Synthesis and Preliminary Pharmacological Screening (antimicrobial, analgesic and anti-inflammatory activity) of Some Novel Quinazoline Derivatives
Article history: Received on: 06/02/2017 Accepted on: 30/03/2017 Available online: 30/06/2017 Objectives: The present research work is designed to synthesize some new series of quinazoline-4-one/4-thione derivatives by modifying the structures retaining the fundamental structural features for the biological activity and screened for their anti-microbial, analgesic and anti-inflammatory properti...
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