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Issue 56, 2015
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2,5-Diaryl-1,3,4-oxadiazoles as selective COX-2 inhibitors and anti-inflammatory agents

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Abstract

A new series of compounds comprising of 2,5-diaryl-1,3,4-oxadiazoles was synthesized and evaluated as potential COX-2 inhibitors. Compounds 6b, 6e, 6f, 7e and 7f were found to be the most potent and selective inhibitors of COX-2 (IC50 = 0.48–0.89 μM; SI = 67.96–132.83). Compounds 6e, 6f and 7f displayed anti-inflammatory activity superior to celecoxib in a carrageenan-induced rat paw edema assay. Structure–activity relationship analysis suggested that the compounds with methylsulfonyl moieties lead to more selective inhibition of COX-2, which is well supported by molecular docking studies. Cytotoxicity studies of the most potent compounds in RAW 264.7 and J774A.1 cells revealed cell viabilities of more than 89% when tested at the concentration of 30 μM.

Graphical abstract: 2,5-Diaryl-1,3,4-oxadiazoles as selective COX-2 inhibitors and anti-inflammatory agents

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Publication details

The article was received on 24 Jan 2015, accepted on 05 May 2015 and first published on 05 May 2015


Article type: Paper
DOI: 10.1039/C5RA01428J
RSC Adv., 2015,5, 45535-45544

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    2,5-Diaryl-1,3,4-oxadiazoles as selective COX-2 inhibitors and anti-inflammatory agents

    J. Grover, N. Bhatt, V. Kumar, N. K. Patel, B. J. Gondaliya, M. Elizabeth Sobhia, K. K. Bhutani and S. M. Jachak, RSC Adv., 2015, 5, 45535
    DOI: 10.1039/C5RA01428J

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