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

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

doi:10.1039/C8OB00227D

Item

ITEM ACTIONSEXPORT

Add to Basket

Local TagsRelease HistoryDetailsSummary

Released

Journal Article

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

MPS-Authors

/persons/resource/persons128263

Zimmermann, Herbert
Department of Biomolecular Mechanisms, Max Planck Institute for Medical Research, Max Planck Society;

External Resource

http://pubs.rsc.org/en/content/articlepdf/2018/ob/c8ob00227d
(Any fulltext)

http://www.rsc.org/suppdata/c8/ob/c8ob00227d/c8ob00227d1.pdf
(Supplementary material)

https://doi.org/10.1039/C8OB00227D
(Any fulltext)

Fulltext (restricted access)

There are currently no full texts shared for your IP range.

Fulltext (public)

There are no public fulltexts stored in PuRe

Supplementary Material (public)

There is no public supplementary material available

Citation

Feng, L., Lanfranchi, D. A., Cotos, L., Cesar-Rodo, E., Ehrhardt, K., Goetz, A.-A., et al. (2018). Synthesis of plasmodione metabolites and 13C-enriched plasmodione as chemical tools for drug metabolism investigation. Organic & Biomolecular Chemistry, 16(15), 2647-2665. doi:10.1039/C8OB00227D.

Cite as: https://hdl.handle.net/21.11116/0000-0001-2E6E-2

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.