Journal
MEDICINAL CHEMISTRY RESEARCH
Volume 22, Issue 1, Pages 340-350Publisher
SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-012-0037-7
Keywords
Quinazolin-4(3H)-one; Analgesic; Anti-inflammatory; Antimicrobial activity
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With the aim of developing potent analgesic, anti-inflammatory, and antimicrobial agents a series of novel quinazolin-4(3H)-one derivatives were synthesized and characterized by FT-IR, H-1-NMR, mass spectroscopy and bases of elemental analysis. Tail-flick technique, carrageenan-induced foot paw edema test, and agar streak dilution test were performed for screening analgesic, anti-inflammatory, and in vitro antimicrobial activity, respectively. Moreover, all compounds were examined for its ulcerogenicity. Results revealed that entire series of compounds exhibited mild to good analgesic, anti-inflammatory, and antimicrobial activity with low to moderate ulcer index. The relationship between the functional group variation and the biological activity of the evaluated compounds were discussed. Compound 2-(2-(4-(trifluoromethyl)benzylidene)hydrazinyl)-N-(4-(2-methyl-4-oxoquinazolin-3(4H)-yl) phenyl) acetamide 5e was determined to be the most active compound.
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