Discovery of an irreversible HCV NS5B polymerase inhibitor.
Bioorg Med Chem Lett
; 23(24): 6585-7, 2013 Dec 15.
Article
em En
| MEDLINE
| ID: mdl-24252545
ABSTRACT
The discovery of lead compound 2e was described. Its covalent binding to HCV NS5B polymerase enzyme was investigated by X-ray analysis. The results of distribution, metabolism and pharmacokinetics were reported. Compound 2e was demonstrated to be potent (replicon GT-1b EC50 = 0.003 µM), highly selective, and safe in in vitro and in vivo assays.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Quinolinas
/
Proteínas não Estruturais Virais
/
Hepacivirus
/
Inibidores Enzimáticos
/
Indóis
Limite:
Animals
/
Humans
/
Male
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2013
Tipo de documento:
Article
País de afiliação:
Estados Unidos