A Developability-Focused Optimization Approach Allows Identification of in Vivo Fast-Acting Antimalarials: N-[3-[(Benzimidazol-2-yl)amino]propyl]amides.
J Med Chem
; 58(11): 4573-80, 2015 Jun 11.
Article
em En
| MEDLINE
| ID: mdl-25906200
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-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.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Benzamidas
/
Benzimidazóis
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Desenho de Fármacos
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Proliferação de Células
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Antimaláricos
Tipo de estudo:
Diagnostic_studies
Limite:
Animals
/
Female
/
Humans
Idioma:
En
Ano de publicação:
2015
Tipo de documento:
Article