Design and synthesis of novel quinazolinones conjugated ibuprofen, indole acetamide, or thioacetohydrazide as selective COX-2 inhibitors: anti-inflammatory, analgesic and anticancer activities
نویسندگان
چکیده
Novel quinazolinones conjugated with indole acetamide (4a-c), ibuprofen (7a-e), or thioacetohydrazide (13a,b, and 14a-d) were designed to increase COX-2 selectivity. The three synthesised series exhibited superior selectivity compared the previously reported their NSAID analogue had equipotent as celecoxib. Compared celecoxib, 4 b, 7c, 13 b showed similar anti-inflammatory activity in vivo, while 14a inhibition of inflammatory mediator nitric oxide, 7 greater antioxidant potential macrophages cells. Moreover, all selected compounds improved analgesic completely abolished pain response. Additionally, compound 4a anticancer tested cell lines HCT116, HT29, HCA7. Docking results consistent COX-1/2 enzyme assay results. In silico studies suggest high oral bioavailability. overall findings for (4a,b, 14c) support role agents.
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ژورنال
عنوان ژورنال: Journal of Enzyme Inhibition and Medicinal Chemistry
سال: 2021
ISSN: ['1475-6374', '1475-6366']
DOI: https://doi.org/10.1080/14756366.2021.1956912