6-Hydrazinopurine 2'-methyl ribonucleosides and their 5'-monophosphate prodrugs as potent hepatitis C virus inhibitors.
Bioorg Med Chem Lett
; 17(9): 2456-8, 2007 May 01.
Article
em En
| MEDLINE
| ID: mdl-17331718
ABSTRACT
A series of 6-hydrazinopurine 2'-methyl ribonucleosides was synthesized and tested for its inhibitory activity against the hepatitis C virus (HCV). The lack of antiviral activity of these nucleosides was associated with a poor affinity for adenosine kinase, which prompted us to synthesize several of their 5'-monophosphate prodrugs. Some of these prodrugs exhibited more than 1000-fold improvement in anti-HCV activity when compared to their parent nucleosides (EC(50) of 24 nM vs 92 microM for the parent).
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Base de dados:
MEDLINE
Assunto principal:
Antivirais
/
Fosfatos
/
Ribonucleosídeos
/
Replicação Viral
/
Hepatite C
/
Proteínas não Estruturais Virais
/
Hepacivirus
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2007
Tipo de documento:
Article
País de afiliação:
Estados Unidos