Design, synthesis, and biological activities of conformationally restricted analogs of primaquine with a 1,10-phenanthroline framework.
Bioorg Med Chem Lett
; 18(16): 4666-9, 2008 Aug 15.
Article
em En
| MEDLINE
| ID: mdl-18653332
ABSTRACT
A series of primaquine analogs was prepared, according to a conformationally restricted conformation of primaquine. In vitro antiplasmodial activities were evaluated and showed that all compounds were active on different strains of Plasmodium falciparum. In particular compounds 5 and 15 possessing a methoxy group were more active than was primaquine. Furthermore, analog 5 displayed good in vitro gametocytocidal activity. In addition selectivity indexes were calculated in respect with cytotoxic activities on Vero cell lines.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Fenantrolinas
/
Química Farmacêutica
/
Antimaláricos
Idioma:
En
Ano de publicação:
2008
Tipo de documento:
Article