Design, synthesis and antimicrobial activities of 1,2,3-triazole hybrids with amine-ester functionality

Due to the notable therapeutic importance of 1,4-disubstituted-1,2,3-triazoles linked with amine and ester groups, a series of 1,2,3-triazole hybrid containing amine-ester functionality have been synthesized. This synthesis involves a Cu(I) catalyzed [3 + 2] dipolar cycloaddition between N-substituted(prop-2-yn-1-yl)amines (3a–3d) and benzyl 2-azidoacetates (6a–6e). The triazoles were thoroughly characterized using different spectral techniques. In vitro assay of developed synthetics with different microbial strains including S. aureus, B. Subtilis, E. Coli, S. enterica, C albicans and R. Oryzae have been conducted. Moderate to excellent activity was observed from majority of the compounds against the tested strains. Notably, compound 7o (MIC = 0.0558 μmol/mL) exhibited substantial potency against most of the tested microbes. Furthermore, an ADME analysis was performed, indicating that the compounds possess a favorable profile and can be considered as patient compliant.