Organic & biomolecular chemistry · 2018
Synthesis of plasmodione metabolites and 13C-enriched plasmodione as chemical tools for drug metabolism investigation.
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Feng Liwen, Lanfranchi Don Antoine, Cotos Leandro, Cesar-Rodo Elena, Ehrhardt Katharina, Goetz Alice-Anne, Zimmermann Herbert, Fenaille François, Blandin Stephanie A, Davioud-Charvet Elisabeth
Аннотация
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.