Abstract
A library of novel bis-heterocycles containing benzoxazolinone based 1,2,3-triazoles has been synthesized using click chemistry approach. The compound 3f exhibited potent selective COX-2 inhibition of 59.48% in comparison to standard drug celecoxib (66.36% inhibition). The compound 3i showed significant (p < 0.001, 50.95%), TNF-α inhibitory activity as compared to indomethacin (p < 0.001, 64.01%). The results of the carrageenan induced hind paw oedema showed that compounds 3a, 3f, 3i, 3o, and 3e exhibited potent anti-inflammatory activity in comparison to Indomethacin. The molecular docking studies revealed that 3i exhibits strong inhibitory effect due to the extra stability of the complex because of an extra π–π bond. The histopathology report showed that none of the compounds caused gastric ulceration.
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•A library of 22 novel compounds has been synthesized using click chemistry approach.•The compounds have been evaluated for TNF-α based in silico molecular docking.•The compounds have been evaluated for in vitro COX-2 and TNF-α assay.•In vivo anti-inflammatory and antinociceptive activities have been done.•Tested compounds did not show any adverse ulcerogenic effect.