Trisubstituted Pyrimidines as Efficacious and Fast-Acting Antimalarials

[Image: see text] In this paper we describe the optimization of a phenotypic hit against Plasmodium falciparum, based on a trisubstituted pyrimidine scaffold. This led to compounds with good pharmacokinetics and oral activity in a P. berghei mouse model of malaria. The most promising compound (13) s...

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Detalles Bibliográficos
Autores principales: Norcross, Neil R., Baragaña, Beatriz, Wilson, Caroline, Hallyburton, Irene, Osuna-Cabello, Maria, Norval, Suzanne, Riley, Jennifer, Stojanovski, Laste, Simeons, Frederick R. C., Porzelle, Achim, Grimaldi, Raffaella, Wittlin, Sergio, Duffy, Sandra, Avery, Vicky M., Meister, Stephan, Sanz, Laura, Jiménez-Díaz, Belén, Angulo-Barturen, Iñigo, Ferrer, Santiago, Martínez, María Santos, Gamo, Francisco Javier, Frearson, Julie A., Gray, David W., Fairlamb, Alan H., Winzeler, Elizabeth A., 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/PMC4947981/
https://www.ncbi.nlm.nih.gov/pubmed/27314305
http://dx.doi.org/10.1021/acs.jmedchem.6b00028

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