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5,5'- and 6,6'-dialkyl-5,6-dihydro-1H-pyridin-2-ones as potent inhibitors of HCV NS5B polymerase.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2009 Nov 01; Vol. 19 (21), pp. 6047-52. Date of Electronic Publication: 2009 Sep 17. - Publication Year :
- 2009
-
Abstract
- The discovery of 5,5'- and 6,6'-dialkyl-5,6-dihydro-1H-pyridin-2-ones as potent inhibitors of the HCV RNA-dependent RNA polymerase (NS5B) is described. Several of these agents also display potent antiviral activity in cell culture experiments (EC50 <0.10 microM). In vitro DMPK data for selected compounds as well as crystal structures of representative inhibitors complexed with the NS5B protein are also disclosed.
- Subjects :
- Animals
Antiviral Agents chemical synthesis
Antiviral Agents pharmacology
Binding Sites
Crystallography, X-Ray
Enzyme Inhibitors chemical synthesis
Enzyme Inhibitors pharmacology
Humans
Macaca fascicularis
Microsomes, Liver metabolism
Pyridones chemical synthesis
Pyridones pharmacology
RNA-Dependent RNA Polymerase metabolism
Structure-Activity Relationship
Antiviral Agents chemistry
Enzyme Inhibitors chemistry
Hepacivirus enzymology
Pyridones chemistry
RNA-Dependent RNA Polymerase antagonists & inhibitors
Viral Nonstructural Proteins metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 19
- Issue :
- 21
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 19796938
- Full Text :
- https://doi.org/10.1016/j.bmcl.2009.09.051