Parasitic diseases are still a major health problem in developing countries. Mucosal infections by protozoa affect more than a billion people every year. The most important protozoan infections include giardiosis, amoebiosis and trichomonosis, whose causal agents are Giardia intestinalis, Entamoeba histolytica and Trichomonas vaginalis, respectively. During the last decade benzimidazole nucleus emerged as a promising scaffold to develop new antiprotozoal agents. As part of our effort to ?nd new antiparasitic agents, in this work we report the synthesis of 19 new 2-{[2-(1H-imidazol-1-yl)ethyl]sulfanyl}-1H-benzimidazole derivatives and their in vitro antiprotozoal activity. All compounds synthesized were tested against the protozoa T. vaginalis, G. intestinalis and E. histolytica.  Experimental evaluations revealed a strong activity for all compounds tested having IC50 values in the nanomolar range, which were even better than the drug of choice for these parasites (metronidazole).

Synthesis and antiprotozoal activity of some 2-{[2-(1<i>H</i>-imidazol-1-yl)ethyl]sulfanyl}-1<i>H</i>-benzimidazole derivatives

244th National Meeting (2012)

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Synthesis and antiprotozoal activity of some 2-{[2-(1H-imidazol-1-yl)ethyl]sulfanyl}-1H-benzimidazole derivatives