Abstract
A series of eighteen pyrazole-imidazole-triazole hybrid (2-(4-((2-(substituted-1H-pyrazol-1-yl)-4-phenyl-1H-imidazol-1-yl)methyl)-1H-1,2,3-triazol-1-yl)-N-(substituted)phenylacetami- de) (6a-6r) are synthesized through click reaction between in situ generated 2-azido-N-substituted acetamide and N-propargylated pyrazole-imidazole derivatives which in turn has been obtained regioselectively from 1-(1H-imidazol-2-yl)-1H-pyrazole and propargyl bromide. The structure of synthesized compounds (6a-6r) was confirmed by various spectroscopic studies (1D and 2D NMR, FT-IR, HRMS) and evaluated for antimicrobial activity. The compound 6m demonstrated excellent potency for A. niger (MIC value 0.0064 µmol/mL); even better than that of the reference drug Fluconazole (MIC value 0.0112 µmol/mL). Further, the binding conformation of most active compounds was ascertained by molecular docking studies.
Published Version
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