Objective: Due to the incidence of resistance, a series of sulfonamide-derived 1,2,4-
triazoles were synthesized and evaluated.
Results: In vitro antimicrobial evaluation found that 2-chlorobenzyl sulfonamide 1,2,4-triazole 7c
exhibited excellent antibacterial activities against MRSA, B. subtilis, B. typhi and E. coli with MIC
values of 0.02-0.16 μmol/mL, which were comparable or even better than Chloromycin. The preliminary
mechanism suggested that compound 7c could effectively bind with DNA, and also it
could bind with human microsomal heme through hydrogen bonds in molecular docking. Computational
chemical studies were performed on compound 7c to understand the structural features
that are essential for activity. Additionally, compound 7c could generate a small amount of reactive
oxygen species (ROS).
Conclusion: Compound 7c could serve as a potential clinical antimicrobial candidate.