Yerigeri, Mayur C. and Murari, S. K. and Kuntebommanahalli, N. T. and Shanta Kumar, S. M. and Vishwanath, B. S. (2008) Anti-tubercular and anti-inflammatory activities of azetidin-2-one derivatives and their effects on the activity of phospholipase A2. Medicinal Chemistry, 4 (2). pp. 190-193. ISSN 1573-4064
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The title compounds have been synthesized and tested for structure activity relationship for Phospholipase A2 (PLA2) [E.C. 3.1.1.4] enzyme inhibition. The in vitro anti-tubercular, PLA2 enzyme inhibitory activities of azetidin-2-one derivatives and in vivo anti-inflammatory studies using mice are highlighted. The analogues of azetidin-2-one were prepared based on the initial activity against Mycobacterium tuberculosis (Mtb). Certain azetidin-2-one analogues described herein showed moderate to good anti-tubercular activity. In particular, two compounds (4f) and (4g) exhibited MIC values of 1.56 and 0.78 μg/mL respectively against the Mtb H37Rv strain. Chloro substitution on aryloxy acid apparently enhanced the antimycobacterial activity and also PLA2 inhibition in the azetidin-2-one series described herein. The ability of azetidin-2-one analogues as anti-inflammatory agents has also been determined. The results show some correlation between anti-inflammatory, anti-tubercular activity and expression of PLA2 enzyme.
| Item Type: | Article |
|---|---|
| Subjects: | C Chemical Science > Biochemistry |
| Divisions: | Department of > Biochemistry |
| Depositing User: | Manjula P Library Assistant |
| Date Deposited: | 26 Aug 2019 06:43 |
| Last Modified: | 26 Aug 2019 06:43 |
| URI: | http://eprints.uni-mysore.ac.in/id/eprint/7032 |
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