With the increase in antibiotic resistance, the need for new antibacterial agents also increases. Benzimidazole derivatives seem to be good candidates for new antimicrobial drugs.  In this study we describe  antimicrobial activity of new benzimidazole derivatives. Two novel groups of polyhalogenated benzimidazoles were synthesized for such investigations. The first group, composed by 4,5,6,7-tetrachloro- 2‑polyfluoroalkylbenzimidazoles, was obtained by chlorination in „aqua regia” respective  2-trifluorometylo, -pentafluoroethyl, ‑heptafluoropropylo i -nonafluorobutylobenzimidazoles. N-Substituted derivatives of 4,5,6,7- tetrachlorobenzimidazole formed the second group.  The alkylation of tetrachlorobenzimidazole with bromoacetic acid ethyl ester provided N¹-substituted compound, which underwent further modifications. The respective acid, hydrazide and  amides substituted with morpholine, piperidine and N-methylpiperazine, were obtained. Antiprotozoal activity was investigated against  Trichomonas vaginalis, Entamoeba hystolitica and Giardia lamblia. The most potent against T. vaginalis appeared N-methylpiperazinylamide of  4,5,6,7-tetrachlorobenzimidazole-1-acetic acids (IC₅₀ = 0.22 μg/ml). 4,5,6,7-Tetrachloro-2-pentafluoroethylbenzimidazole showed the best activity against E. hystolitica (IC₅₀ = 0.18 μg/ml). Gram-positive and Gram-negative bacteria were also susceptible to new obtained compounds. Of all derivatives 2-trifluoromethyl- and 2-pentafluoroethyl-  -4,5,6,7-tetrachlorobenzimidazoles  showed significant inhibition zone diameters  (45-50 mm) for Staphylococcus and Enterococcus species.

The study was supported by the Foundation for Development Diagnostics and Therapy, Warsaw (AO and ZK).

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