Synthesis and in vitro cysticidal activity of new benzimidazole derivatives

Despite albendazole being the drug of choice in neurocysticercosis treatment, its low solubility limits its bioavailability; therefore, more research is required in order to find new molecules with cestocidal activity and adequate aqueous solubility. A set of 13 benzimidazole derivatives were synthesized and their in vitro activities were evaluated against Taenia crassiceps cysts, using albendazole sulfoxide as reference molecule, showing that two of them exhibited good activity. Molecular modelling revealed that the cysticidal efficacy depends on the presence on the molecule of an H in the 1-position, a planar carbamate group at 2-position, and if the substituent in 5-position is voluminous, it should be orthogonal to the benzimidazole ring.

A set of 13 benzimidazole derivatives were synthesized and their in vitro cysticidal activities were evaluated using albendazole sulfoxide as control. Derivatives 5 and 6 showed good activity.Figure optionsDownload as PowerPoint slide