3-Arylidene-5-(4-isobutylphenyl)-2(3H)-furanones: a new series of anti-inflammatory and analgesic compounds having antimicrobial activity

被引：6

作者：

Alam, Mumtaz Mohammad ^{[1
]}

Husain, Asif ^{[1
]}

Hasan, Syed M. ^{[2
]}

Khanna, Suruchi ^{[3
]}

Shaquiquzzaman, Mohammad ^{[1
]}

机构：

[1] Jamia Hamdard, Fac Pharm, Dept Pharmaceut Chem, New Delhi 110062, India

[2] Coll Hlth Sci, Dept Pharm, Sakaka, Saudi Arabia

[3] Jamia Hamdard, Fac Pharm, Dept Pharmacol, New Delhi 110062, India

来源：

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2010年 / 25卷 / 03期

关键词：

Furanones; anti-inflammatory; ulcerogenic; lipid peroxidation; antimicrobial activity; BIOLOGICAL EVALUATION; CYCLOOXYGENASE-2; DERIVATIVES; INHIBITORS; DESIGN; DRUGS; 2(3H)-FURANONES; LACTONES; DAMAGE; ASSAY;

D O I：

10.3109/14756360903179435

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

070307 [化学生物学]; 071010 [生物化学与分子生物学];

摘要：

An ideal anti-inflammatory drug should have the desired effect in minimum dose with minimum side effects. Antimicrobial actions associated with such agents will be an added advantage as they broaden the spectrum of the compounds. Promising anti-inflammatory and antimicrobial activity together with low ulcerogenic properties of some 2(3H)-furanones, synthesized in our previous study, prompted us to investigate the effect of the isobutyl group on their pharmacological profile. Since compounds 3, 9, 13, and 14 have both anti-inflammatory and analgesic effects in addition to low ulcerogenic incidence, they were selected for investigation of their inhibitory effects on various cyclo-oxygenase enzymes. It was found that they were more selective toward COX-2 enzymes. An MIC of 6.25 mu g/mL was recorded for compounds 3, 13, and 14 against S. aureus, E. coli, R. oryza, and P. citrum. The study supports the development of furanone derivatives as potential anti-inflammatory agents with antimicrobial activity.</.

引用

页码：323 / 330

页数：8

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