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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Publicat a:J Med Chem
Autors principals: 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.
Format: Artigo
Idioma:Inglês
Publicat: American Chemical Society 2016
Accés en línia:https://ncbi.nlm.nih.gov/pmc/articles/PMC4947981/
https://ncbi.nlm.nih.gov/pubmed/27314305
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.6b00028
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