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

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

Volume: 9 Issue: 8

Author(s): Zbigniew Ochal, Maria Bretner, Renata Wolinowska and Stefan Tyski

Affiliation:

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

Abstract: 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.

Cite this article as:

Ochal Zbigniew, Bretner Maria, Wolinowska Renata and Tyski Stefan, Synthesis and in vitro Antibacterial Activity of 5-Halogenomethylsulfonyl- Benzimidazole and Benzotriazole Derivatives, Medicinal Chemistry 2013; 9 (8) . https://dx.doi.org/10.2174/1573406411309080015