Synthesis and evaluation of novel HCV replication inhibitors

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...

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Bibliographic Details
Published in:Molecular diversity 2017-05, Vol.21 (2), p.475-481
Main Authors: McGowan, David C., Khamlichi, Mourad D., De Groot, Alex, Pauwels, Frederik, Delouvroy, Frédéric, Van Emelen, Kristof, Simmen, Kenneth, Raboisson, Pierre
Format: Article
Language:English
Subjects:
Antiviral Agents - chemical synthesis
Antiviral Agents - pharmacology
Antiviral drugs
Biochemistry
Biomedical and Life Sciences
Cell Line
Chemistry Techniques, Synthetic
Hepacivirus - drug effects
Hepacivirus - physiology
Hepatitis
Inhibitor drugs
Life Sciences
Organic Chemistry
Pharmaceutical sciences
Pharmacy
Polymer Sciences
Short Communication
Viral Nonstructural Proteins - antagonists & inhibitors
Virus Replication - drug effects
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Summary: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. Graphical Abstract
ISSN:1381-1991
1573-501X
DOI:10.1007/s11030-017-9733-z