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

Abstract

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 μg/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.

Keywords::

• Furanones
• anti-inflammatory
• ulcerogenic
• lipid peroxidation
• antimicrobial activity

Acknowledgements

We are also thankful to Professor (Mrs) P. K. Pillai, Head, Department of Microbiology, Majeedia Hospital, New Delhi, for help in performing antimicrobial studies of the compounds.

This article was presented in part at the 60th Indian Pharmaceutical Congress, 12–14 December, 2008 at New Delhi, India.

Declaration of interest: Financial support provided by the All India Council for Technical Education (AICTE), New Delhi, under the RPS scheme is gratefully acknowledged. No conflict of interest