Synthesis of N-Benzenesulfonylbenzotriazole Derivatives, and Evaluation of their Antimicrobial Activity

A series of benzenesulfonyl compounds, 1a-i, containing a BZT moiety was synthesized and characterized, and their antifungal and antibacterial activities were investigated. Compounds 1a and 1d showed the highest activity against Escherichia coli ATCC 25922; in addition 1a presented bactericidal activity against E. coli and Staphylococcus aureus at 8.6 mM. The ability of 1a to generate superoxide anion (O2 .-) was measured and it showed more stimuli in S. aureus compared to sulfathiazole, indicating that 1a can be involved in oxidative stress of bacteria. None of the compounds inhibited the growth of the dermatophytes strains at the tested concentration (250 μg/ml). Keywords: Benzenesulfonyl, Benzotriazole, Antibacterial, Antifungal