A Developability-Focused Optimization Approach Allows Identification of in Vivo Fast-Acting Antimalarials: N-[3-[(Benzimidazol-2-yl)amino]propyl]amides
Research output: Contribution to journal › Article › Scientific › peer-review
|Number of pages||8|
|Journal||JOURNAL OF MEDICINAL CHEMISTRY|
|Publication status||Published - 11 Jun 2015|
|Publication type||A1 Journal article-refereed|
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-acting antimalarial chemotype based on a benzimidazole core. This discovery is the result of a medicinal chemistry plan focused on improving the developability profile of an antichlamydial chemical class previously reported by our group.
- PLASMODIUM-FALCIPARUM, STARTING POINTS, DE-POINTES, MALARIA, BENZIMIDAZOLES, PROLONGATION, TCAMS