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

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

Volume: 18 Issue: 16

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

Affiliation:

• Applied Organic Chemistry Department, National Research Centre,12622, Dokki, Giza,Egypt

Keywords: Anti-inflammatory Activity, Hydrazonoyl halide, pyrazole, thiazole, sulphonamide, NSAID` drugs.

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 %.

Cite this article as:

Abdel Hafez A. Naglaa , Ali A. Korany *, Ibrahim A. Alhussein , Elnaggar H. Dina and Sleem A. Amany , Design, Synthesis and In-vivo Anti-inflammatory Activity of New Celecoxib Analogues as NSAID, Mini-Reviews in Medicinal Chemistry 2018; 18 (16) . https://dx.doi.org/10.2174/1389557518666180530124509