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

Author(s): Naglaa A. Abdel Hafez , Korany A. Ali* , Alhussein A. Ibrahim , Dina H. Elnaggar , Amany A. Sleem .

Journal Name: Mini-Reviews in Medicinal Chemistry

Volume 18 , Issue 16 , 2018

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Graphical 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.

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Article Details

Year: 2018
Page: [1398 - 1408]
Pages: 11
DOI: 10.2174/1389557518666180530124509
Price: $58

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