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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Publié dans:J Med Chem
Auteurs principaux: 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.
Format: Artigo
Langue:Inglês
Publié: American Chemical Society 2016
Accès en ligne:https://ncbi.nlm.nih.gov/pmc/articles/PMC5108032/
https://ncbi.nlm.nih.gov/pubmed/27631715
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.6b00723
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