Design, synthesis and biological evaluation of piperic acid triazolyl derivatives as potent anti-inflammatory agents

• A library of 19 novel piperine based triazoles has been synthesized.
• Compounds showed significant in vivo anti-inflammatory activity.
• Compounds 3g and 3f alleviated TNF-α level without showing any cytotoxicity.
• Compounds 3g and 3f significantly suppressed protein expression of COX-2 and NF–kB.
• Compounds 3g and 3f did not cause any damage to the stomach.

Nineteen novel piperine based triazoles have been synthesized using click chemistry approach and were tested for in vivo anti-inflammatory activity. The most active compounds were evaluated for in vitro TNF-α expression. Compounds 3g and 3f were found to show significant in vivo inhibition of inflammation, 80.40% and 76.71%, respectively after 5 h in comparison to piperine (54.72%) and the standard drug indomethacin (77.02%) without causing any damage to the stomach. Compounds 3g and 3f suppressed TNF-α level by 73.73% and 70.64%, respectively and protein expression of COX-2, NF–κB and TNF-α more than indomethacin. Moreover, the compound 3g was found to show significant analgesic activity of 54.09% which was comparable with the indomethacin (57.43%).

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