Facile expeditious one-pot synthesis and antifungal evaluation of disubstituted 1,2,3-triazole with two amide linkages

ABSTRACT

A library of twenty five amide linked 1,4-disubstituted 1,2,3-triazoles have been prepared through a facile expeditious synthetic protocol involving Cu(I) mediated cyclization of N-(2-methylbut-3-yn-2-yl)aromatic amides and in situ generated 2-azido-N-substituted propanamides. Structures of newly synthesized compounds (5a–5y) were confirmed by analytical techniques, such as FTIR, ¹H NMR, ¹³C NMR, and HRMS. In vitro antifungal activity was also examined against two fungal strains Candida albicans and Aspergillus niger by serial dilution method. The compounds 5 m and 5w exhibited appreciable potent activity.

GRAPHICAL ABSTRACT

KEYWORDS:

• 1,3-Dipolar cycloaddition
• 1,4-disubstituted 1,2,3-triazoles
• antifungal activity
• synthesis