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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.
- Source :
-
Journal of medicinal chemistry [J Med Chem] 2005 Oct 06; Vol. 48 (20), pp. 6454-60. - Publication Year :
- 2005
-
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).
- Subjects :
- Antiviral Agents chemistry
Antiviral Agents pharmacology
Bridged-Ring Compounds chemistry
Bridged-Ring Compounds pharmacology
Cell Line, Tumor
Hepacivirus genetics
Humans
Nucleosides chemistry
Nucleosides pharmacology
RNA, Viral antagonists & inhibitors
Structure-Activity Relationship
Antiviral Agents chemical synthesis
Bridged-Ring Compounds chemical synthesis
Hepacivirus drug effects
Nucleosides chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 0022-2623
- Volume :
- 48
- Issue :
- 20
- Database :
- MEDLINE
- Journal :
- Journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 16190771
- Full Text :
- https://doi.org/10.1021/jm058223t