The goal of this collaborative project with Actelion Pharmaceuticals is the discovery of new antimalarial molecules with unknown mechanism(s) of action. Cell-based antimalarial screens were performed at the beginning of this project in order to find new lead structures. In a library with an assortment of aspartic protease inhibitors and compounds with undefined targets, novel piperazine-containing compounds were identified.
These compounds are highly active against Plasmodium falciparum and are currently in medicinal chemistry programs with the goal to further improve drugability. Hopes are high that a clinical program for a new antimalarial drug can be initiated in the near future. Additionally, interesting results are coming out of a PhD thesis addressing the elucidation of the mode of action of these novel compounds.