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Article Dans Une Revue Organic & Biomolecular Chemistry Année : 2018

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

Résumé

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.

Mots clés

CBM

Domaines

Chimie organique
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Dates et versions

hal-02161631 , version 1 (12-01-2024)

Identifiants

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Liwen Feng, Don Antoine Lanfranchi, Leandro Cotos Munoz, Elena Cesar Rodo, Katharina Ehrhardt, et al.. Synthesis of plasmodione metabolites and 13C-enriched plasmodione as chemical tools for drug metabolism investigation. Organic & Biomolecular Chemistry, 2018, 15, pp.2647-2665. ⟨10.1039/C8OB00227D⟩. ⟨hal-02161631⟩
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