Non-nucleoside inhibitors of HCV polymerase NS5B. Part 2: Synthesis and structure-activity relationships of benzothiazine-substituted quinolinediones.
Bioorg Med Chem Lett
; 19(13): 3642-6, 2009 Jul 01.
Article
em En
| MEDLINE
| ID: mdl-19457662
ABSTRACT
A new series of benzothiazine-substituted quinolinediones were evaluated as inhibitors of HCV polymerase NS5B. SAR studies on this series revealed a methyl sulfonamide group as a high affinity feature. Analogues with this group showed submicromolar potencies in the HCV cell based replicon assay. Pharmacokinetic and toxicology studies were also performed on a selected compound (34) to evaluate in vivo properties of this new class of inhibitors of HCV NS5B polymerase.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Antivirais
/
Quinolinas
/
Tiazinas
/
RNA Polimerases Dirigidas por DNA
/
Proteínas não Estruturais Virais
/
Hepacivirus
/
Quinolonas
/
Inibidores Enzimáticos
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2009
Tipo de documento:
Article