Antiplasmodial activity of short peptide-based compounds

Abstract

Three series of short peptide-based compounds were synthesized, which upon evaluation against chloroquine-sensitive (D6) and chloroquine-resistant (W2) strains of Plasmodium falciparum in vitro, produced IC₅₀ values ranging between 1.4–4.7 μg mL⁻¹. Importantly, higher antimalarial activity against the drug-resistant strain of P. falciparum (W2) was observed for the tested peptides, indicating their potential in the treatment of drug-resistant malaria parasites. The lack of cytotoxicity in all tested peptides provides evidence of their safety profile. The selected peptides were evaluated in an enzymatic inhibitory assay against plasmepsin II, a potential target for antiplasmodial activity, also indicated from the results of the molecular docking studies.