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

…, P Kiuru, F Calderón, J Yli-Kauhaluoma

Index: Keurulainen, Leena; Salin, Olli; Siiskonen, Antti; Kern, Jan Marco; Alvesalo, Joni; Kiuru, Paula; Maass, Matthias; Yli-Kauhaluoma, Jari; Vuorela, Pia Journal of Medicinal Chemistry, 2010 , vol. 53, # 21 p. 7664 - 7674

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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, novel chemotypes are urgently needed. Herein we report a novel, in vivo active, fast- ...