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A series of benzotriazole derivatives (compounds 1-27 ) were synthesized, and 24 (compounds 1-5 , 9-27 ) of which were first reported. Their chemical structures were confirmed by means of 1 H NMR, IR and elemental analyses, coupled with one selected single crystal structure (compound 1 ). All the compounds were assayed for antibacterial activities against three Gram positive bacterial strains ( Bacillus subtilis, Staphylococcus aureus and Streptococcus faecalis ) and three Gram negative bacterial strains ( Escherichia coli, Pseudomonas aeruginosa and Enterobacter cloacae ) by MTT method. Among the compounds tested, most of them exhibited potent antibacterial activity against the six bacterial strains. Most importantly, compound 3-benzotriazol-1-yl-1-(4-bromo-phenyl)-2-[1,2,4]triazol-1-ylpropan-1-one ( 19 ) showed the most favourable antibacterial activity against B. subtilis, S. aureus, S. faecalis, P. aeruginosa, E. coli and E. cloacae with MIC of 1.56 µg/mL, 1.56 µg/mL, 1.56 µg/mL, 3.12 µg/mL, 6.25 µg/mL and 6.25 µg/mL, respectively.

Facile synthesis of novel benzotriazole derivatives and their antibacterial activities