Synthesis of precursors and macrocycle analogs of aerucyclamides as anti-trypanosomal agents

Abstract

In the search for candidates of antiparasitic new drugs, macrocycle analogs and key fragments of aerucyclamides were obtained. The activities against Trypanosoma brucei brucei and cytotoxicities on murine macrophages (cell line J774) were evaluated. Two of the prepared compounds displayed similar anti-trypanosomal activities as aerucyclamides B and C. In addition, the compound with the highest activity presents a 150-fold selectivity (SI = 150) for the parasite than against the murine macrophage.