Synthesis and structure-activity relationships of novel anti-hepatitis C agents: N3,5'-cyclo-4-(beta-D-ribofuranosyl)-vic-triazolo[4,5-b]pyridin-5-one derivatives.
J Med Chem
; 48(20): 6454-60, 2005 Oct 06.
Article
em En
| MEDLINE
| ID: mdl-16190771
ABSTRACT
Several 6- and 7-monosubstituted N3,5'-cyclo-4-(beta-d-ribofuranosyl)-vic-triazolo[4,5-b]pyridin-5-one derivatives as well as the 5-thiono analogue were synthesized, providing structure-anti-hepatitis C virus (HCV) activity relationships for the series. Among the compounds synthesized, the 6-bromo, 7-methylamino, and 5-thiono analogues exhibited more potent anti-HCV activity in an HCV subgenomic replicon cell based assay (EC90 = 1.9, 7.4, and 10.0 microM, respectively) than the lead compound N3,5'-cyclo-4-(beta-D-ribofuranosyl)-vic-triazolo[4,5-b]pyridin-5-one (EC90 = 79.8 microM).
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Base de dados:
MEDLINE
Assunto principal:
Antivirais
/
Hidrocarbonetos Aromáticos com Pontes
/
Hepacivirus
/
Nucleosídeos
Idioma:
En
Ano de publicação:
2005
Tipo de documento:
Article