Issue 15, 2018

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

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

Supplementary files

Article information

Article type
Paper
Submitted
26 yan 2018
Accepted
06 mar 2018
First published
06 mar 2018

Org. Biomol. Chem., 2018,16, 2647-2665

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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