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

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.

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Item Permalink: https://hdl.handle.net/21.11116/0000-0001-2E6E-2 Version Permalink: https://hdl.handle.net/21.11116/0000-0001-2E6F-1
Genre: Journal Article

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 Creators:
Feng, Liwen, Author
Lanfranchi, Don Antoine, Author
Cotos, Leandro, Author
Cesar-Rodo, Elena, Author
Ehrhardt, Katharina, Author
Goetz, Alice-Anne, Author
Zimmermann, Herbert1, Author           
Fenaille, François, Author
Blandin, Stephanie A., Author
Davioud-Charvet, Elisabeth, Author
Affiliations:
1Department of Biomolecular Mechanisms, Max Planck Institute for Medical Research, Max Planck Society, ou_1497700              

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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.

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Language(s): eng - English
 Dates: 2018-01-262018-03-062018-03-06
 Publication Status: Issued
 Pages: 20
 Publishing info: -
 Table of Contents: -
 Rev. Type: Peer
 Identifiers: DOI: 10.1039/C8OB00227D
URI: https://www.ncbi.nlm.nih.gov/pubmed/29542786
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Title: Organic & Biomolecular Chemistry
  Other : Organic and Biomolecular Chemistry
  Abbreviation : Org. Biomol. Chem.
Source Genre: Journal
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Publ. Info: Cambridge : Royal Society of Chemistry
Pages: - Volume / Issue: 16 (15) Sequence Number: - Start / End Page: 2647 - 2665 Identifier: ISSN: 1477-0520
CoNE: https://pure.mpg.de/cone/journals/resource/954925269322