A Developability-Focused Optimization Approach Allows Identification of in Vivo Fast-Acting Antimalarials: N‑[3-[(Benzimidazol-2-yl)amino]propyl]amides

Malaria continues to be a major global health problem, being particularly devastating in the African population under the age of five. Artemisinin-based combination therapies (ACTs) are the first-line treatment recommended by the WHO to treat Plasmodium falciparum malaria, but clinical resistance ag...

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Veröffentlicht in:	Journal of medicinal chemistry 2015-06, Vol.58 (11), p.4573-4580
Hauptverfasser:	Keurulainen, Leena, Vahermo, Mikko, Puente-Felipe, Margarita, Sandoval-Izquierdo, Elena, Crespo-Fernández, Benigno, Guijarro-López, Laura, Huertas-Valentín, Leticia, de las Heras-Dueña, Laura, Leino, Teppo O, Siiskonen, Antti, Ballell-Pages, Lluís, Sanz, Laura M, Castañeda-Casado, Pablo, Jiménez-Díaz, M. Belén, Martínez-Martínez, María S, Viera, Sara, Kiuru, Paula, Calderón, Félix, Yli-Kauhaluoma, Jari
Format:	Artikel
Sprache:	eng
Schlagworte:	Amides - chemical synthesis Amides - pharmacokinetics Amides - pharmacology Animals Antimalarials - chemical synthesis Antimalarials - pharmacokinetics Antimalarials - pharmacology Benzamides - chemical synthesis Benzamides - pharmacokinetics Benzamides - pharmacology Benzimidazoles - chemical synthesis Benzimidazoles - chemistry Benzimidazoles - pharmacokinetics Benzimidazoles - pharmacology Cell Proliferation - drug effects Cells, Cultured Drug Design ERG1 Potassium Channel Ether-A-Go-Go Potassium Channels - antagonists & inhibitors Female Humans Malaria, Falciparum Mice, Inbred NOD Mice, SCID Models, Molecular Molecular Structure Plasmodium falciparum Structure-Activity Relationship Tissue Distribution
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