Discovery of proline sulfonamides as potent and selective hepatitis C virus NS5b polymerase inhibitors. Evidence for a new NS5b polymerase binding site.
J Med Chem
; 49(11): 3052-5, 2006 Jun 01.
Article
em En
| MEDLINE
| ID: mdl-16722622
ABSTRACT
Through high throughput screening, substituted proline sulfonamide 6 was identified as HCV NS5b RNA-dependent RNA polymerase inhibitor. Optimization of various regions of the lead molecule resulted in compounds that displayed good potency and selectivity. The crystal structure of 6 and NS5b polymerase complex confirmed the binding near the active site region. The optimization approach and SAR are discussed in detail.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Antivirais
/
Sulfonamidas
/
Prolina
/
Proteínas não Estruturais Virais
Idioma:
En
Ano de publicação:
2006
Tipo de documento:
Article