Design, synthesis and evaluation of 5-substituted amino-2,4-diamino-8-chloropyrimido-[4,5-b]quinolines as novel antimalarials.
Bioorg Med Chem Lett
; 15(1): 73-6, 2005 Jan 03.
Article
em En
| MEDLINE
| ID: mdl-15582413
ABSTRACT
Novel 5-substituted amino-2,4-diamino-8-chloropyrimido-[4,5-b]quinolines were designed based on a pharmacophore developed for potent antimalarial activity using Chem-X and MOE softwares. The designed molecules were synthesized by following a novel route and were evaluated by Rane's test for blood schizonticidal activity in mice infected by Plasmodium berghei. Based on the Mean Survival Time (MST) data, of the nine compounds evaluated, three had curative potential when compared with chloroquine.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Quinolonas
/
Antimaláricos
Limite:
Animals
Idioma:
En
Ano de publicação:
2005
Tipo de documento:
Article