Status: Bibliographieeintrag
Standort: ---
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| Online-Ressource |
Verfasst von: | Lanfranchi, Don A. [VerfasserIn]  |
| Müller, Tobias [VerfasserIn]  |
| Lanzer, Michael [VerfasserIn]  |
| Davioud-Charvet, Elisabeth [VerfasserIn]  |
Titel: | Exploring the trifluoromenadione core as a template to design antimalarial redox-active agents interacting with glutathione reductase |
Verf.angabe: | Don Antoine Lanfranchi, Didier Belorgey, Tobias Müller, Hervé Vezin, Michael Lanzer, Elisabeth Davioud-Charvet |
E-Jahr: | 2012 |
Jahr: | 17 Apr 2012 |
Umfang: | 12 S. |
Fussnoten: | Gesehen am 18.10.2018 |
Titel Quelle: | Enthalten in: Organic & biomolecular chemistry |
Ort Quelle: | Cambridge : Royal Society of Chemistry, 2003 |
Jahr Quelle: | 2012 |
Band/Heft Quelle: | 10(2012), 24, Seite 4795-4806 |
ISSN Quelle: | 1477-0539 |
Abstract: | Menadione is the 2-methyl-1,4-naphthoquinone core used to design potent antimalarial redox-cyclers to affect the redox equilibrium of Plasmodium-infected red blood cells. Exploring the reactivity of fluoromethyl-1,4-naphthoquinones, in particular trifluoromenadione, under quasi-physiological conditions in NADPH-dependent glutathione reductase reactions, is discussed in terms of chemical synthesis, electrochemistry, enzyme kinetics, and antimalarial activities. Multitarget-directed drug discovery is an emerging approach to the design of new antimalarial drugs. Combining in one single 1,4-naphthoquinone molecule, the trifluoromenadione core with the alkyl chain at C-3 of the known antimalarial drug atovaquone, revealed a mechanism for CF3 as a leaving group. The resulting trifluoromethyl derivative 5 showed a potent antimalarial activity per se against malarial parasites in culture. |
DOI: | doi:10.1039/C2OB25229E |
URL: | Bitte beachten Sie: Dies ist ein Bibliographieeintrag. Ein Volltextzugriff für Mitglieder der Universität besteht hier nur, falls für die entsprechende Zeitschrift/den entsprechenden Sammelband ein Abonnement besteht oder es sich um einen OpenAccess-Titel handelt.
Volltext ; Verlag: http://dx.doi.org/10.1039/C2OB25229E |
| Volltext: https://pubs.rsc.org/en/content/articlelanding/2012/ob/c2ob25229e |
| DOI: https://doi.org/10.1039/C2OB25229E |
Datenträger: | Online-Ressource |
Sprache: | eng |
K10plus-PPN: | 1582083401 |
Verknüpfungen: | → Zeitschrift |
Exploring the trifluoromenadione core as a template to design antimalarial redox-active agents interacting with glutathione reductase / Lanfranchi, Don A. [VerfasserIn]; 17 Apr 2012 (Online-Ressource)
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