Enlarging the chemical space of anti-leishmanials: a structure–activity relationship study of peptoids against Leishmania mexicana, a causative agent of cutaneous leishmaniasis

Abstract

Peptoids, a class of peptide mimetics, have emerged as promising anti-infective agents against a range of bacterial and fungal infections. Recently we have shown peptoids to be novel anti-parasitic and, specifically, anti-leishmanial, compounds. In this study, we have expanded the chemical space of our peptoid library and have identified peptoids with low micromolar activity against Leishmania mexicana axenic amastigotes and significantly, the first peptoids with promising activity against intracellular amastigotes, which are the clinical cause of cutaneous leishmaniasis.