1-Azaaurones derived from the naturally occurring aurones as potential antimalarial drugs.
Bioorg Med Chem
; 18(15): 5724-31, 2010 Aug 01.
Article
em En
| MEDLINE
| ID: mdl-20630767
We report the synthesis and in vitro antiplasmodial activity of 35 compounds, designed as analogues of the naturally occurring aurones. Several of these analogues showed submicromolar antimalarial activity against a chloroquine-resistant strain of Plasmodium falciparum (FcB1-Columbia strain) cultured on human erythrocytes. Substitution of the intracyclic oxygen in aurones by a nitrogen atom and systematic variation of the substituent at the B-ring revealed promising leads showing good activity on the CQ-resistant strain. In particular, 4,6-dimethoxy-4'-ethylazaaurone 22 showed antiplasmodial potency without noticeable toxicity. The easy synthesis of this family of compounds and the relevant antiplasmodial activity are in favor of promising candidates for further development.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Compostos Aza
/
Benzofuranos
/
Indóis
/
Antimaláricos
Limite:
Humans
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article