Publication: Antimalarial activity of HIV-1 protease inhibitor in chromone series
Issued Date
2014-01-01
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ISSN
10902120
00452068
00452068
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2-s2.0-84910636566
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Mahidol University
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SCOPUS
Bibliographic Citation
Bioorganic Chemistry. Vol.57, (2014), 142-147
Suggested Citation
Pradith Lerdsirisuk, Chirattikan Maicheen, Jiraporn Ungwitayatorn Antimalarial activity of HIV-1 protease inhibitor in chromone series. Bioorganic Chemistry. Vol.57, (2014), 142-147. doi:10.1016/j.bioorg.2014.10.006 Retrieved from: https://repository.li.mahidol.ac.th/handle/20.500.14594/33393
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Title
Antimalarial activity of HIV-1 protease inhibitor in chromone series
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Abstract
© 2014 Elsevier Inc. All rights reserved. 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= 0.65 μM), was found to be the most potent antimalarial compound with IC50= 0.95 μM while primaquine and tafenoquine showed IC50= 2.41 and 1.95 μM, 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 = -13.24 kcal/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.