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 ,
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
