Synthesis, Characterization and Antimicrobial Activities of 1,4- Disubstituted 1,2,3-Triazole Compounds

Abstract

Background: 1,2,3-triazoles are five-membered heterocyclic scaffold; their broad-spectrum biological activities are known. Researchers around the world are increasingly being interested in this emerging area, owing to its immense pharmacological scope.

Objective: This work summarizes the synthesis of 1,2,3-triazoles and the significance of this pattern as a lead structure for new drug molecules discovery.

Methods: 1,2,3-triazoles can be obtained on a multigram scale through "click chemistry" under ambient conditions.

Results: Sixteen compounds were synthesized and evaluated on five microbial strains E. coli, E. faecalis, P. aeruginosa, S. aureus and C. albicans. NMR, MS and IR were used to characterize all compounds. They were evaluated with their Minimum Inhibitory Concentrations (MICs) and interesting results were obtained with compounds 12a, 12b, 3, 2a and 2c, with MIC 0.14 μM (P. aeruginosa), 1.08 μM (E. coli), 1.20 μM (E. faecalis and C. albicans), 3.5 μM (E. faecalis) and 4.24 μM (C. albicans), respectively. P. aeruginosa and C. albicans were the most sensitive among all the strains.

Conclusion: The synthesized compounds were found as potential antimicrobial agents against Gram (+), Gram (-) strains and fungi.

Keywords: Activities; Antimicrobial; Biological activities; Click chemistry; Minimal inhibitory concentrations; Triazoles.