Synthesis, analgesic, anti-inflammatory, and in vitro antimicrobial activities of some novel quinazolin-4(3H)-one derivatives

被引:20
作者
Saravanan, Govindaraj [1 ]
Alagarsamy, Veerachamy [2 ]
Prakash, Chinnasamy Rajaram [3 ]
机构
[1] Jawaharlal Nehru Technol Univ, Bapatla Coll Pharm, Med Chem Res Lab, Hyderabad, Andhra Pradesh, India
[2] MNR Coll Pharm, Med Chem Res Lab, Sangareddy, Andhra Pradesh, India
[3] DCRM Pharm Coll, Dept Med Chem, Inkollu, Andhra Pradesh, India
关键词
Quinazolin-4(3H)-one; Analgesic; Anti-inflammatory; Antimicrobial activity; ANTIBACTERIAL ACTIVITIES; INHIBITORS;
D O I
10.1007/s00044-012-0037-7
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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.
引用
收藏
页码:340 / 350
页数:11
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