Title of article
Improved replicon cellular activity of non-nucleoside allosteric inhibitors of HCV NS5B polymerase: From benzimidazole to indole scaffolds
Author/Authors
Pierre L. Beaulieu، نويسنده , , James Gillard، نويسنده , , Darren Bykowski، نويسنده , , Christian Brochu، نويسنده , , Nathalie Dansereau، نويسنده , , Jean-Simon Duceppe، نويسنده , , Bruno Haché، نويسنده , , Araz Jakalian، نويسنده , , Lisette Lagacé، نويسنده , , Steven Laplante، نويسنده , , Ginette McKercher، نويسنده , , Elaine Moreau، نويسنده , , Stephane Perreault، نويسنده , , Timothy Stammers، نويسنده , , Louise Thauvette، نويسنده , , Jeff Warrington، نويسنده , , George Kukolj، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
7
From page
4987
To page
4993
Abstract
Benzimidazole-based allosteric inhibitors of the hepatitis C virus (HCV) NS5B polymerase were diversified to a variety of topologically related scaffolds. Replacement of the polar benzimidazole core by lipophilic indoles led to inhibitors with improved potency in the cell-based subgenomic HCV replicon system. Transposing the indole scaffold into a previously described series of benzimidazole–tryptophan amides generated the most potent inhibitors of HCV RNA replication in cell culture reported to date in this series (EC50 50 nM).
Keywords
HCV NS5B polymerase , hepatitis C virus , Replicon , antiviral , Allosteric Inhibitors , indoles
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797315
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