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

Abstract

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 against them has already been reported. As a consequence… (More)
DOI: 10.1021/acs.jmedchem.5b00114

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@article{Keurulainen2015ADO, title={A Developability-Focused Optimization Approach Allows Identification of in Vivo Fast-Acting Antimalarials: N-[3-[(Benzimidazol-2-yl)amino]propyl]amides.}, author={Leena Keurulainen and Mikko Vahermo and Margarita Puente-Felipe and Elena Sandoval-Izquierdo and Benigno Crespo-Fern{\'a}ndez and Laura Guijarro-L{\'o}pez and Leticia Huertas-Valent{\'i}n and Laura de las Heras-Due{\~n}a and Teppo O. Leino and Antti O Siiskonen and Llu{\'i}s Ballell-Pages and Laura Sanz and Pablo Casta{\~n}eda-Casado and Mar{\'i}a Bel{\'e}n Jim{\'e}nez-D{\'i}az and Mar{\'i}a Santos Mart{\'i}nez-Mart{\'i}nez and Sara Viera and Paula S Kiuru and F{\'e}lix Calder{\'o}n and Jari Yli-Kauhaluoma}, journal={Journal of medicinal chemistry}, year={2015}, volume={58 11}, pages={4573-80} }