We previously reported on the excellent anti-trypanosomal and anti-pneumocystis carinii activity of several bisbenzamidines linked with an alkanediamide chain. To further evaluate the potential anti-protozoal properties of these compounds, an expanded series of 15 alkanediamide-linked bisbenzamidines were synthesized and screened against Trypanosoma cruzi, Leishmania donovani and Plasmodium falciparum and their cytotoxicity towards rat skeletal myoblasts was determined. These compounds were the most active toward P. falciparum with nine of the compounds demonstrating IC50 values in the low nanomolar ranges. The details of the structure-activity relationship data for these compounds will be presented.

Structure-activity relationships of alkanediamide-linked bisbenzamidines as potential antimalarial agents

245th National Meeting (2013)

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