Novel amodiaquine congeners as potent antimalarial agents.
Bioorg Med Chem
; 16(14): 6813-23, 2008 Jul 15.
Article
em En
| MEDLINE
| ID: mdl-18562202
ABSTRACT
To develop new classes of antimalarial agents, the possibility of replacing the phenolic ring of amodiaquine, tebuquine, and isoquine with other aromatic nuclei was investigated. Within a first set of pyrrole analogues, several compounds displayed high activity against both D10 (CQ-S) and W-2 (CQ-R) strains of Plasmodium falciparum. The isoquine structure was also modified by replacing the diethylamino group with more metabolically stable bicyclic moieties and by replacing the aromatic hydroxyl function with a chlorine atom. Among these compounds, two quinolizidinylmethylamino derivatives (6f and 7f) displayed high activity against both CQ-S and CQ-R strains.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Amodiaquina
/
Antimaláricos
Limite:
Animals
Idioma:
En
Ano de publicação:
2008
Tipo de documento:
Article