Identification of Fast-Acting 2,6-Disubstituted Imidazopyridines That Are Efficacious in the in Vivo Humanized Plasmodium falciparum NODscidIL2Rγ null Mouse Model of Malaria.
J Med Chem
; 61(9): 4213-4227, 2018 05 10.
Article
en En
| MEDLINE
| ID: mdl-29665687
ABSTRACT
Optimization of a chemical series originating from whole-cell phenotypic screening against the human malaria parasite, Plasmodium falciparum, led to the identification of two promising 2,6-disubstituted imidazopyridine compounds, 43 and 74. These compounds exhibited potent activity against asexual blood stage parasites that, together with their in vitro absorption, distribution, metabolism, and excretion (ADME) properties, translated to in vivo efficacy with clearance of parasites in the PfSCID mouse model for malaria within 48 h of treatment.
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Plasmodium falciparum
/
Piridinas
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Descubrimiento de Drogas
/
Imidazoles
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Malaria
Tipo de estudio:
Diagnostic_studies
Límite:
Animals
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Humans
Idioma:
En
Revista:
J Med Chem
Asunto de la revista:
QUIMICA
Año:
2018
Tipo del documento:
Article
País de afiliación:
Sudáfrica