Synthesis, analgesic, anti-inflammatory and in vitro antimicrobial activities of some novel isoxazole coupled quinazolin-4(3H)-one derivatives.
Autor: Saravanan, Govindaraj; Alagarsamy, Veerachamy; Dineshkumar, Pandurangan
Publication year: 2021
Archives of pharmacal research
issn:1976-3786 0253-6269
doi: 10.1007/s12272-013-0262-8
Abstract:
A series of novel isoxazole coupled quinazolin-4(3H)-one derivatives were synthesized and characterized by FT-IR, (1)H NMR, mass spectroscopy and bases of elemental analysis with the aim of developing potent analgesic, anti-inflammatory and antimicrobial agents. 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 was discussed. Out of various synthesized compounds, 2-methyl-3-(4-(5-(4-(trifluoromethyl)phenyl) isoxazol-3-yl)phenyl)quinazolin-4(3H)-one 5e was found to be the most active compound.
Language: eng
Rights: © 2013. The Pharmaceutical Society of Korea.
Pmid: 24155019
Tags: Female; Male; Animals; Rats; Mice; Structure-Activity Relationship; Analgesic; Analgesics/chemical synthesis/chemistry/*pharmacology; Anti-Infective Agents/chemical synthesis/chemistry/*pharmacology; Anti-inflammatory; Anti-Inflammatory Agents/chemical synthesis/chemistry/*pharmacology; Antimicrobial activity; Disease Models, Animal; Isoxazole; Isoxazoles/chemical synthesis/chemistry/*pharmacology; Quinazolin-4(3H)-one; Quinazolinones/chemical synthesis/chemistry/*pharmacology; Rats, Wistar; Toxicity Tests
Link: https://pubmed.ncbi.nlm.nih.gov/24155019/
