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Design, Synthesis and In-vivo Anti-inflammatory Activity of New Celecoxib Analogues as NSAID

[ Vol. 18 , Issue. 16 ]

Author(s):

Naglaa A. Abdel Hafez, Korany A. Ali*, Alhussein A. Ibrahim, Dina H. Elnaggar and Amany A. Sleem   Pages 1398 - 1408 ( 11 )

Abstract:


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.

Affiliation:

Applied Organic Chemistry Department, National Research Centre,12622, Dokki, Giza, Applied Organic Chemistry Department, National Research Centre,12622, Dokki, Giza, Applied Organic Chemistry Department, National Research Centre,12622, Dokki, Giza, Applied Organic Chemistry Department, National Research Centre,12622, Dokki, Giza, Department of Pharmacology, National Research Centre, 12622, Dokki, Giza

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