Journal
SYNTHETIC COMMUNICATIONS
Volume 51, Issue 20, Pages 3125-3140Publisher
TAYLOR & FRANCIS INC
DOI: 10.1080/00397911.2021.1964530
Keywords
Antifungal; anti-inflammatory; [3+2] cycloaddition; N-Arylsydnone; pyrazole
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Funding
- DST, SAIF [SR/RS/DH-1/20132 Dt:15/05/2013]
- DST, New Delhi [Purse Phase II]
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This paper reports the synthesis of novel pyrazoles and their in vitro anti-inflammatory and antifungal assay results. The compounds showed potential anti-inflammatory activity and significant inhibition against Aspergillus fumigatus.
In this paper, the synthesis of novel pyrazoles and their in vitro anti-inflammatory and in-vitro antifungal assay have been reported. These compounds were docked into the inducible nitric oxide synthase (iNOS) oxygenase dimer. The compounds 3c, 7a, 7c, 8a, 8c have exhibited the C-score values more than the standard drug aminoguanidine (5.35). Upon the favorable docking results, the anti-inflammatory potential of the title compounds was determined by analyzing the reduction in the NO production by activated macrophages using in-vitro assays. The compounds 4c, 5c, 6a, 6c, 7a, 8a, 8c exhibited the potential anti-inflammatory activity at 1.00 mu g/mL. Further, the docking study of the title compounds 3b, 3c, 4a, 5a, 5c with Aspergillus fumigatus N-myristoyl transferase (NMT) showed appreciable C-score values as against that of fluconazole (5.56). This observation was further substantiated by in-vitro antifungal activity in which the compounds 3b-c, 4a-c, 5a-c, 6a-c, 7a-b, 9a-c have excellent inhibition against A. fumigatus.
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