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Discovery of a Quinoline-4-carboxamide Derivative with a Novel Mechanism of Action, Multistage Antimalarial Activity, and Potent in Vivo Efficacy

[Image: see text] The antiplasmodial activity, DMPK properties, and efficacy of a series of quinoline-4-carboxamides are described. This series was identified from a phenotypic screen against the blood stage of Plasmodium falciparum (3D7) and displayed moderate potency but with suboptimal physicoche...

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Detalles Bibliográficos
Autores principales: Baragaña, Beatriz, Norcross, Neil R., Wilson, Caroline, Porzelle, Achim, Hallyburton, Irene, Grimaldi, Raffaella, Osuna-Cabello, Maria, Norval, Suzanne, Riley, Jennifer, Stojanovski, Laste, Simeons, Frederick R. C., Wyatt, Paul G., Delves, Michael J., Meister, Stephan, Duffy, Sandra, Avery, Vicky M., Winzeler, Elizabeth A., Sinden, Robert E., Wittlin, Sergio, Frearson, Julie A., Gray, David W., Fairlamb, Alan H., Waterson, David, Campbell, Simon F., Willis, Paul, Read, Kevin D., Gilbert, Ian H.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2016
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5108032/
https://www.ncbi.nlm.nih.gov/pubmed/27631715
http://dx.doi.org/10.1021/acs.jmedchem.6b00723