Synthesis and Evaluation of 2-Hydroxy-1,4-naphthoquinone Derivatives as Potent Antimalarial Agents

A series of 3-substituted-2-hydroxy-1,4-naphthoquinone derivatives with a variety side chains were successfully synthesized by Mannich reaction 2-hydroxy-1,4-naphthoquinone (lawsone) selected amines and aldehydes. All substances (1–16) evaluated for in-vitro antimalarial activity against strains Plasmodium falciparum microculture radioisotope technique. Bioassay data revealed that ten (1–8, 11 13) displayed significantly good values IC50 ranging from 0.77 to 4.05 µg/mL. The best biological profile (IC50 = µg/mL) was observed in compound 1, possessing n-butyl substituted aminomethyl group. Experimental results support the potential use our active components as promising agents fight malaria infections multidrug resistance problems.