Synthesis and evaluation of novel HCV replication inhibitors
| Autor: | Kristof Van Emelen, Kenneth Simmen, Frederik Pauwels, Mourad Daoubi Khamlichi, Pierre Jean-Marie Bernard Raboisson, David McGowan, Alex De Groot, Frédéric Delouvroy |
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| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
viruses Hepacivirus medicine.medical_treatment Hepatitis C virus Chemistry Techniques Synthetic Viral Nonstructural Proteins medicine.disease_cause Virus Replication Antiviral Agents Catalysis Cell Line Inorganic Chemistry 03 medical and health sciences Drug Discovery medicine Physical and Theoretical Chemistry NS5A Molecular Biology Polymerase Protease biology Chemistry Organic Chemistry virus diseases General Medicine Hepatitis C biology.organism_classification medicine.disease Virology digestive system diseases 030104 developmental biology Viral replication biology.protein Nucleoside Information Systems |
| Zdroj: | Molecular diversity. 21(2) |
| ISSN: | 1573-501X |
| Popis: | Direct acting antiviral agents to cure hepatitis C virus (HCV) infection has emerged as the gold standard therapy. Along with protease inhibitors, nucleoside polymerase inhibitors and non-nucleoside polymerase inhibitors, the inhibition of NS5a has proved to be an effective way to treat HCV patients. Here we report on novel HCV NS5a inhibitors which were synthesized and evaluated in the HCV replicon assay. A series of inhibitors were formed by a cycloaddition reaction in parallel to establish new leads and explore the effects of unsymmetrical cap substitution. This led to the identification of several triazoles with picomolar potency in vitro against hepatitis C virus. |
| Databáze: | OpenAIRE |
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