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Journal Articles ChemistryOpen Year : 2022

Synthesis and Antimalarial Activities of New Hybrid Atokel Molecules

Christian Bijani

Abstract

The currently spreading resistance of the malaria parasite Plasmodium falciparum to artemisinin-based combination therapies makes an urgent need for new efficient drugs. Aiming to kill artemisinin-resistant Plasmodium, a series of novel hybrid drugs named Atokels were synthesized and characterized. Atokels are based on an 8-amino- or 8-hydroxyquinoline entity covalently bound to a 1,4-naphthoquinone through a polyamine linker. These drugs have been designed to target the parasite mitochondrion by their naphthoquinone moiety reminiscent of the antimalarial drug atovaquone, and to trigger a damaging oxidative stress due to their ability to chelate metal ions in order to generate redox active complexes in situ. The most effective Atokel drug shown a promising antimalarial activity (IC50=622 nm on an artemisinin-resistant P. falciparum strain) and no cytotoxicity at 50 μm indicating a specific antiplasmodial mode of action.
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hal-03681793 , version 1 (30-05-2022)

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Youzhi Li, Anthony Loureiro, Michel Nguyen, Marion Laurent, Christian Bijani, et al.. Synthesis and Antimalarial Activities of New Hybrid Atokel Molecules. ChemistryOpen, 2022, 11 (5), pp.e202200064. ⟨10.1002/open.202200064⟩. ⟨hal-03681793⟩
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