Tres Cantos Open Lab Foundation: Identifying benzimidazole-derived leads against <em>Plasmodium falciparum</em>

The benzimidazole derivatives synthesized at the University of Helsinki have shown activity against protozoan parasites. Linked to this discovery, a structure search of the Tres Cantos Antimalarial Set (TCAMS) was undertaken and led to the identification of some structural analogues which are endowed with antiplasmodial properties.

During this one-year project two researchers will work on the optimization of this series based on analysis of TCAMS and in silico ADME studies. Chemical synthesis will afford new optimized molecules with better potencies and promising developability profiles. The objective is to find a lead with good therapeutic efficacy in the mouse model of Plasmodium falciparum infection, that could eventually be further developed.