Improved replicon cellular activity of non-nucleoside allosteric inhibitors of HCV NS5B polymerase: from benzimidazole to indole scaffolds.
Bioorg Med Chem Lett
; 16(19): 4987-93, 2006 Oct 01.
Article
em En
| MEDLINE
| ID: mdl-16908138
ABSTRACT
Benzimidazole-based allosteric inhibitors of the hepatitis C virus (HCV) NS5B polymerase were diversified to a variety of topologically related scaffolds. Replacement of the polar benzimidazole core by lipophilic indoles led to inhibitors with improved potency in the cell-based subgenomic HCV replicon system. Transposing the indole scaffold into a previously described series of benzimidazole-tryptophan amides generated the most potent inhibitors of HCV RNA replication in cell culture reported to date in this series (EC(50) approximately 50 nM).
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Replicon
/
Benzimidazóis
/
Proteínas não Estruturais Virais
/
Hepacivirus
/
Indóis
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Ano de publicação:
2006
Tipo de documento:
Article