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

Abstract：

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

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Lerdsirisuk P,Maicheen C,Ungwitayatorn J

doi

10.1016/j.bioorg.2014.10.006

subject

Has Abstract

pub_date

2014-12-01 00:00:00

pages

142-147

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(14)00105-9

journal_volume

57

pub_type

杂志文章

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