Background: A new series of Celecoxib analogues were easily synthesized via reactions of
4-(2-(1-chloro-2-oxopropylidene)hydrazinyl)benzene sulfonamide (1) with active methylene compounds
and dialkyl malonate. In addition, compound 1 was reacted also with thiourea derivatives and
thiosemicarbazone derivatives to afford thiazole derivatives 9 and 11, respectively. Furthermore, triazolo
pyrimidine derivatives 13 were prepared via reaction of compound 1 with pyrimidine thione
derivatives. The structures of the new synthesized compounds were assigned by elemental analysis and
spectroscopic data. The new analogues were screened for their in vivo anti-inflammatory activity using
carrageenan-induced paw edema method.
Conclusion: They showed moderate to good in vivo anti-inflammatory effects. Compounds 1, 6 and 11b
were the most active compounds that reduced the paw edema induced by carrageenan by 12.25 %, 12.96 %
and 12.97% respectively, as compared to the Indomethacin that inhibited the oedema volume by 7.47 %.
Keywords: Anti-inflammatory Activity, Hydrazonoyl halide, pyrazole, thiazole, sulphonamide, NSAID` drugs.
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