6-Chloro-7-methyl-3', 4'-dimethoxyflavone – a Potent Selective COX-2 Inhibitor

Author(s): Rafia Bashir, Kalim Javed, Shafiya Yaseen, Syed Ovais, Pooja Rathore, Hinna Hamid, M. S. Alam, Mohammed Samim, Surender Singh, Vinod Nair

Journal Name: Medicinal Chemistry

Volume 9 , Issue 4 , 2013

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Some unnatural chalcones (1a-q) and flavones (2a-d) have been synthesized and evaluated for their antiinflammatory activity using carrageenan-induced rat paw edema assay. The flavone 2c (6-Chloro-7-methyl-3', 4'- dimethoxyflavone) had higher anti-inflammatory activity and superior gastrointestinal safety profiles than the reference drug celecoxib. Compound 2c showed almost two times better selective inhibitory activity towards COX-2 enzyme than celecoxib. 2'-Hydroxychalcones (1a-h) showed moderate to strong anti-inflammatory activity (38.6-82.4 % at 3h and 52.4–80.2 % at 5h). Among 2'-methoxychalcones (1i-q) 1k and 1q exhibited maximum activity 82.6% (at 3h) and 84.3% (at 5h) respectively.

Keywords: Chalcones, flavones, anti-inflammatory activity, selective COX-2 inhibitor

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Article Details

Year: 2013
Published on: 31 March, 2013
Page: [617 - 623]
Pages: 7
DOI: 10.2174/1573406411309040016
Price: $65

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