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Discovery of a Potent Boronic Acid Derived Inhibitor of the HCV RNA-Dependent RNA Polymerase
Discovery of a Potent Boronic Acid Derived Inhibitor of the HCV RNA-Dependent RNA Polymerase
- Source :
- Journal of Medicinal Chemistry. 57:1902-1913
- Publication Year :
- 2013
- Publisher :
- American Chemical Society (ACS), 2013.
-
Abstract
- A boronic acid moiety was found to be a critical pharmacophore for enhanced in vitro potency against wild-type hepatitis C replicons and known clinical polymorphic and resistant HCV mutant replicons. The synthesis, optimization, and structure-activity relationships associated with inhibition of HCV replication in a subgenomic replication system for a series of non-nucleoside boron-containing HCV RNA-dependent RNA polymerase (NS5B) inhibitors are described. A summary of the discovery of 3 (GSK5852), a molecule which entered clinical trials in subjects infected with HCV in 2011, is included.
- Subjects :
- Models, Molecular
Magnetic Resonance Spectroscopy
Hepacivirus
Viral Nonstructural Proteins
Antiviral Agents
Structure-Activity Relationship
chemistry.chemical_compound
RNA polymerase
Drug Resistance, Viral
Drug Discovery
Structure–activity relationship
Replicon
Enzyme Inhibitors
NS5B
Subgenomic mRNA
Drug discovery
virus diseases
RNA-Dependent RNA Polymerase
Boronic Acids
Virology
Molecular biology
digestive system diseases
In vitro
chemistry
Molecular Medicine
Pharmacophore
Subjects
Details
- ISSN :
- 15204804 and 00222623
- Volume :
- 57
- Database :
- OpenAIRE
- Journal :
- Journal of Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....e6ce7599d644e69b47104c8ac1a7db2e
- Full Text :
- https://doi.org/10.1021/jm400317w