title: Synthesis, analgesic, anti-inflammatory and in vitro antimicrobial activities of some novel isoxazole coupled quinazolin-4(3H)-one derivatives.
abstract: A series of novel isoxazole coupled quinazolin-4(3H)-one derivatives were synthesized and characterized by FT-IR,1H 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.
authors.affiliation: Medicinal Chemistry Research Laboratory, Bapatla College of Pharmacy, Bapatla, Andhra Pradesh, India. sarachem1981@gmail.com.
authors.forename: Govindaraj
authors.initials: G
authors.lastname: Saravanan
authors.affiliation: Medicinal Chemistry Research Laboratory, M.N.R. College of Pharmacy, Sangareddy, Andhra Pradesh, India.
authors.forename: Veerachamy
authors.initials: V
authors.lastname: Alagarsamy
authors.affiliation: Research Laboratory, Hindu College of Pharmacy, Guntur, Andhra Pradesh, India.
authors.forename: Pandurangan
authors.initials: P
authors.lastname: Dineshkumar
mesh_terms: D000700:Analgesics / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000890:Anti-Infective Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004195:Disease Models, Animal; D005260:Female; D007555:Isoxazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008297:Male; D051379:Mice; D052999:Quinazolinones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship; D018675:Toxicity Tests
chemical_list: D000700:Analgesics; D000890:Anti-Infective Agents; D000893:Anti-Inflammatory Agents; D007555:Isoxazoles; D052999:Quinazolinones
keywords: Analgesic; Anti-inflammatory; Antimicrobial activity; Isoxazole; Quinazolin-4(3H)-one