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  • Title: 1,3,4-Trisubstituted pyrazole analogues as promising anti-inflammatory agents.
    Author: Alegaon SG, Alagawadi KR, Garg MK, Dushyant K, Vinod D.
    Journal: Bioorg Chem; 2014 Jun; 54():51-9. PubMed ID: 24793214.
    Abstract:
    Twenty-two 1,3,4-trisubstituted pyrazole (3a-d), (4a-d), (5a-d), (6a-l) derivatives were synthesized and structure of newly synthesized compounds were characterized by IR, (1)H NMR, (13)C NMR, and mass spectral analysis. These compounds were screened for the anti-inflammatory activity by carrageenan-induced paw edema method. Compounds 5a, and 5b showed excellent anti-inflammatory activity (⩾84.2% inhibition) and 3a, 3b, and 3c showed good anti-inflammatory activity (⩾64.6% inhibition) compared to that of the standard drug diclofenac (86.72%) when measured 3h after the carrageenan injection. Moreover, the cyclooxygenase (COX) enzyme inhibitor activity of selected compounds, which are the excellent anti-inflammatory activities in carrageenan-induced paw edema model, was investigated in vitro COX inhibition assay. Molecular docking study further helped in supporting the observed activity. In addition compound 5a exhibited considerable cytotoxic activity against MCF-7 cell line with IC50 value 6.5 μM.
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