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Cyclization-blocked proguanil as a strategy to improve the antimalarial activity of atovaquone

Atovaquone-proguanil (Malarone®) is used for malaria prophylaxis and treatment. While the cytochrome bc1-inhibitor atovaquone has potent activity, proguanil’s action is attributed to its cyclization-metabolite, cycloguanil. Evidence suggests that proguanil has limited intrinsic activity, associated...

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Detalles Bibliográficos
Autores principales: Skinner-Adams, Tina S., Fisher, Gillian M., Riches, Andrew G., Hutt, Oliver E., Jarvis, Karen E., Wilson, Tony, von Itzstein, Mark, Chopra, Pradeep, Antonova-Koch, Yevgeniya, Meister, Stephan, Winzeler, Elizabeth A., Clarke, Mary, Fidock, David A., Burrows, Jeremy N., Ryan, John H., Andrews, Katherine T.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group UK 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6499835/
https://www.ncbi.nlm.nih.gov/pubmed/31069275
http://dx.doi.org/10.1038/s42003-019-0397-3