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Issue 15, 2018
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Synthesis of plasmodione metabolites and 13C-enriched plasmodione as chemical tools for drug metabolism investigation

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Abstract

Malaria is a tropical parasitic disease threatening populations in tropical and sub-tropical areas. Resistance to antimalarial drugs has spread all over the world in the past 50 years, thus new drugs are urgently needed. Plasmodione (benzylmenadione series) has been identified as a potent antimalarial early lead drug, acting through a redox bioactivation on asexual and young sexual blood stages. To investigate its metabolism, a series of plasmodione-based tools, including a fully 13C-labelled lead drug and putative metabolites, have been designed and synthesized for drug metabolism investigation. Furthermore, with the help of UHPLC-MS/MS, two of the drug metabolites have been identified from urine of drug-treated mice.

Graphical abstract: Synthesis of plasmodione metabolites and 13C-enriched plasmodione as chemical tools for drug metabolism investigation

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Article information


Submitted
26 Jan 2018
Accepted
06 Mar 2018
First published
06 Mar 2018

Org. Biomol. Chem., 2018,16, 2647-2665
Article type
Paper

Synthesis of plasmodione metabolites and 13C-enriched plasmodione as chemical tools for drug metabolism investigation

L. Feng, D. A. Lanfranchi, L. Cotos, E. Cesar-Rodo, K. Ehrhardt, A. Goetz, H. Zimmermann, F. Fenaille, S. A. Blandin and E. Davioud-Charvet, Org. Biomol. Chem., 2018, 16, 2647
DOI: 10.1039/C8OB00227D

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