1,4-naphthoquinone cations as antiplasmodial agents: hydroxy-, acyloxy-, and alkoxy-substituted analogues.
ACS Med Chem Lett
; 3(12): 1029-33, 2012 Dec 13.
Article
em En
| MEDLINE
| ID: mdl-24936235
ABSTRACT
Cations of hydroxy-substituted 1,4-naphthoquinones were synthesized and evaluated as antiplasmodial agents against Plasmodium falciparum. The atovaquone analogues were found to be inactive as antagonists of parasite growth, which was attributed to ionization of the acidic hydroxyl moiety. Upon modification to an alkoxy substituent, the antiplasmodial activity was restored in the sub-100 nM range. Optimal inhibitors were found to possess IC50 values of 17.4-49.5 nM against heteroresistant P. falciparum W2.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Idioma:
En
Revista:
ACS Med Chem Lett
Ano de publicação:
2012
Tipo de documento:
Article
País de afiliação:
Estados Unidos