Antimalarial activity of HIV-1 protease inhibitor in chromone series.

摘要: Increasing parasite resistance to nearly all available antimalarial drugs becomes a serious problem human health and necessitates the need continue search for new effective drugs. Recent studies have shown that clinically utilized HIV-1 protease (HIV-1 PR) inhibitors can inhibit in vitro vivo growth of Plasmodium falciparum. In this study, series chromone derivatives possessing PR inhibitory activity has been tested against P. falciparum (K1 multi-drug resistant strain). Chromone 15, potent inhibitor (IC50=0.65μM), was found be most compound with IC50=0.95μM while primaquine tafenoquine showed IC50=2.41 1.95μM, respectively. Molecular docking study compounds plasmepsin II, an aspartic enzyme important hemoglobin degradation, revealed 15 exhibited higher binding affinity (binding energy=-13.24kcal/mol) than known PM II inhibitors. Thus, potential class agent.