Synthesis, Characterization, and Antimicrobial Activity of 1,2,3-Triazoles Containing a Theophylline Moiety

Abstract

A new series of substituted 1,2,3-triazoles have been synthesized from theophylline and substituted 2-azido-N-phenylacetamides through copper(I)-catalyzed azide–alkyne cycloaddition (CuAAC) reaction. The proposed method features minimal number of steps, high yields, straightforward conditions, and no need for further purification. The structures of the synthesized substituted 1,2,3–triazole derivatives were confirmed using spectral and analytical techniques. Their antimicrobial activity was tested in vitro, revealing that the nature of the substituents on the triazole ring significantly influences antimicrobial efficacy, as demonstrated by a preliminary structure–activity relationship analysis.