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Issue 4, 1998
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Is alkylation the main mechanism of action of the antimalarial drug artemisinin?

Abstract

Artemisinin is a sesquiterpene lactone with an endoperoxide function essential for its antimalarial activity against chloroquine-resistant strains of Plasmodium falciparum. The mechanism of action of this paradigm molecule for endoperoxide-containing antimalarial drugs is still open to debate. Are the artemisinin derivatives only responsible for oxidative stress or are they able to alkylate heme and parasite proteins? The characterization of a covalent artemisinin-heme model adduct supports the role of C-centered radicals generated by the reductive activation of the peroxidic bond of this class of drugs. Artemether (an artemisinin analogue) and BO7 (a synthetic antimalarial trioxane) are also able to alkylate a porphyrin cycle.

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Article type: Paper
DOI: 10.1039/A827273Z
Citation: Chem. Soc. Rev., 1998,27, 273-274
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    Is alkylation the main mechanism of action of the antimalarial drug artemisinin?

    A. Robert and B. Meunier, Chem. Soc. Rev., 1998, 27, 273
    DOI: 10.1039/A827273Z

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