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Synthesis and in vitro Antibacterial Activity of 5-Halogenomethylsulfonyl- Benzimidazole and Benzotriazole Derivatives

[ Vol. 9 , Issue. 8 ]


Zbigniew Ochal, Maria Bretner, Renata Wolinowska and Stefan Tyski   Pages 1129 - 1136 ( 8 )


A series of 5-halogenomethylsulfonylbenzimidazole and benzotriazole derivatives was synthesized as potential antibacterial agents. A new method of synthesis of benzimidazoles was developed. The antimicrobial activities of these compounds were tested against a series of reference and clinical strains. The reference strains include Gram-positive bacteria (S. aureus, S. epidermidis, B. subtilis, B. cereus, E. hirae, M. luteus) and Gram-negative rods (E. coli, P. vulgaris, P. aeruginosa, B. bronchiseptica). The clinical strains include six methicillin-resistant (MRSA) and two methicillin-sensitive (MSSA) S. aureus strains, one methicillin-resistant S. epidermidis, three E. faecalis and two E. faecium strains. Compound with trifluoromethyl- substituent at C-2 position (4) displayed significant antibacterial activities comparable with nitrofurantoin against four strains, and higher against Micrococcus luteus. MIC values for clinical Staphylococci strains (MRSA) were 12.5-25 μg/mL; for Enterococcus strains these values were 50-100 μg/mL. MIC values for reference and clinical strains of Staphylococcus and Enterococcus group were similar, respectively.


5-Halogenomethylsulfonylbenzimidazole and benzotriazole derivatives, Amberlyst 15, Antibacterial activity, MRSA, MSSA, Nitrofurantoin.


Warsaw University of Technology, Faculty of Chemistry, 3 Noakowskiego St., 00-664 Warszawa, Poland.

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