Aryl piperazine and pyrrolidine as antimalarial agents. Synthesis and investigation of structure-activity relationships

► In this paper, written in collaboration between Southern (Peru and Colombia) and Northern (Spain and France) University teams, we showed that some synthetic piperazine derivatives were able to impair the growth of Plasmodium falciparum in vitro, with low cytotoxicity. ► The most active compound was also able to reduce (moderately) the growth of Plasmodium berghei in mice. ► Finally, we showed (with in silico studies) that the most active compound targets plasmepsin II enzyme.