| Autor: |
Feng L; CNRS-Université de Strasbourg-Université de Haute-Alsace UMR 7042, Laboratoire d'Innovation Moléculaire et Applications (LIMA), Team Bioorganic and Medicinal Chemistry, ECPM 25 Rue Becquerel, 67087 Strasbourg, France. elisabeth.davioud@unistra.fr., Lanfranchi DA, Cotos L, Cesar-Rodo E, Ehrhardt K, Goetz AA, Zimmermann H, Fenaille F, Blandin SA, Davioud-Charvet E |
| Jazyk: |
angličtina |
| Zdroj: |
Organic & biomolecular chemistry [Org Biomol Chem] 2018 Apr 18; Vol. 16 (15), pp. 2647-2665. |
| DOI: |
10.1039/c8ob00227d |
| Abstrakt: |
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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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