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Butenolide-based eighteen new amide derivatives (1–18) have been synthesized and evaluated for anti-inflammatory activity. The compounds 9, 17 and 4 exhibited significant in vivo inhibition of 84.69, 76.52 and 76.22 % inflammation, respectively, after 5 h without causing any damage to stomach and liver in comparison with the standard drug indomethacin which showed 79.04 % inhibition. The compounds showing potent anti-inflammatory activity were further evaluated for ex vivo TNF-α suppression. Compounds 9, 17 and 4 significantly suppressed TNF-α concentration to 74.83, 71.74 and 67.11 % as compared to indomethacin which exhibited a suppression of 69.01 %. Compounds 9 and 17 were also found to suppress the expression of COX-2 and NF-κB in the paw tissue. Moreover, compound 9 showed significant analgesic activity (57.03 %) which was comparable to indomethacin (61.03 %).

A library of 20 novel benzoxazolinone-based 1,2,4-triazoles has been synthesised and screened for their in vivo anti-inflammatory and antinociceptive activities. The compound 18e exhibited potent anti-inflammatory activity with 68.75 and 55.20 % inhibition in comparison to indomethacin which showed 65.62 and 60.41 % inhibition after 3 and 5 h, respectively. The five active compounds, i.e. 2a and 17e–20e showing significant in vivo anti-inflammatory activity have been screened for their in vivo COX-2, TNF-α, IL-1β and NO inhibitory activities. The COX-2 selectivity index of 17e was found to be 42.30 and thereby showing a high selectivity towards COX-2 inhibition. In silico molecular docking studies have been done in order to get an insight into the binding modes of these molecules with TNF-α protein. The compound 20e exhibited potent antinociceptive activity with 56.70 % inhibition of analgesia. The compounds 2a and 17e–20e did not exhibit any gastric ulceration.

Five (2a–e) benzenesulfonylurea derivatives bearing pyridazinone were synthesized by refluxing the appropriate 6-aryl-2-(p-sulfamylphenyl)-4,5-dihydropyridazine-3(2H)-one with benzylisocyanate in dry acetone over anhydrous K2CO3. These compounds were characterized by elemental analysis and various spectroscopic techniques viz; IR, 1H NMR, 13C NMR, and MS data. These compounds (2a–e) at the dose of 20 mg/kg were tested for blood glucose lowering activity in glucose-fed hyperglycemic normal rats. Compound 2b showed more potent anti-hyperglycemic activity than the standard drug gliclazide. The compound 2b was also tested for its hypoglycemic effect in fasted normal rats. It also showed significant hypoglycemic effect (but less than that of gliclazide).

Some new benzenesulfonylthiourea derivatives substituted with pyridazinone (2a–o) were synthesized by refluxing the appropriate 6-aryl-2-(p-sulfamylphenyl)-4,5-dihydropyridazine-3(2H)-ones with isothiocyanate in dry acetone over anhydrous K2CO3. All the synthesized compounds were characterized on the basis of IR, 1H NMR, 13C NMR, DEPT and MS data, and elemental analysis. These compounds at the dose of 20 mg/kg were tested for blood glucose lowering activity in glucose-fed hyperglycemic normal rats. Five compounds (2a, 2d, 2l, 2m, and 2n) markedly reduced the content of glucose in rat blood (by more than 25%). Compound 2d showed the maximum reduction (38.8%).