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Synthesis and Anti-inflammatory Activity of New N-Acyl-2-pyrazolines Bearing Homologous Alkyloxy Side Chains

Muhammad Moazzam Naseer, Asghar Abbas

Abstract


A series of new pyrazoline derivatives (1b-8c) equipped with N-acyl arms and homologous alkyloxy side chains were synthesized and characterized on the basis of spectroscopic data and microanalysis. All the synthesized compounds were screened for their in-vitro anti-inflammatory activity to examine the effect of alkyloxy side chain length on activity. Compounds with odd number of carbons in alkyloxy side chain showed better activity as compared to even ones. Compound 3c (96% inhibition, IC50 = 173.06 ± 2.312 mM)was found to be the most active compound of the series with activity better than the standard (Indomethacine, 92% inhibition, IC50 = 273.12 ± 2.33 mM). Compound 1b (86%, IC50 = 296.16 ± 2.091 mM) was the second best with comparable activity to the standard drug. However, the other compounds of series showed moderate to low activity.  Interestingly, parallel cytotoxicity studies of compound 1b-8c against PC-3 cell line revealed either no or very low cytotoxicity. The study may contribute in developing useful alternatives to presently used NSAIDs with harmful gastric effects due to direct cytotoxicity.

Keywords


N-Acyl-2-pyrazolines; synthesis; anti-inflammatory; cytotoxicity

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