Discovery and optimisation studies of antimalarial phenotypic hits.
Eur J Med Chem
; 103: 530-8, 2015 Oct 20.
Article
en En
| MEDLINE
| ID: mdl-26408453
ABSTRACT
There is an urgent need for the development of new antimalarial compounds. As a result of a phenotypic screen, several compounds with potent activity against the parasite Plasmodium falciparum were identified. Characterization of these compounds is discussed, along with approaches to optimise the physicochemical properties. The in vitro antimalarial activity of these compounds against P. falciparum K1 had EC50 values in the range of 0.09-29 µM, and generally good selectivity (typically >100-fold) compared to a mammalian cell line (L6). One example showed no significant activity against a rodent model of malaria, and more work is needed to optimise these compounds.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Plasmodium berghei
/
Plasmodium falciparum
/
Descubrimiento de Drogas
/
Antimaláricos
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Eur J Med Chem
Año:
2015
Tipo del documento:
Article
País de afiliación:
Reino Unido