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Abstract A series of urea-1,2,3-triazole-amide hybrids was designed and synthesized via click reaction of urea derivatives containing a propargyl unit with 2-bromo-N-phenylacetamide derivatives and characterized by FTIR, NMR and HRMS… Click to show full abstract
Abstract A series of urea-1,2,3-triazole-amide hybrids was designed and synthesized via click reaction of urea derivatives containing a propargyl unit with 2-bromo-N-phenylacetamide derivatives and characterized by FTIR, NMR and HRMS data. The antimicrobial evaluation of these synthesized compounds towards three bacteria (Bacillus subtilis, Escherichia coli and Staphylococcus aureus) and two fungi (Aspergillus niger and Candida albicans) was carried out. The activity results revealed that all these hybrids 4(a-r) exhibited better activity than their precursors i.e. alkynes 2(a-c). Moreover, almost all the synthesized triazoles were found to be more potent than the reference drug Fluconazole against C. albicans. Further, docking studies of compound 4j in the active sites of S. aureus DNA gyrase complexed with DNA and antifungal target Lanosterol 14-α demethylase were also carried out.
Journal Title: Journal of Molecular Structure
Year Published: 2020
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