Discovery of pentacyclic compounds as potent inhibitors of hepatitis C virus NS5B RNA polymerase

Abstract We report a new series of inhibitors for hepatitis C virus NS5B RNA polymerase containing a constrained pentacyclic scaffold. Our SAR studies led to the identification of hexahydroindolo[2,1- a ]pyrrolo[3,2- d ][2]benzazepines exposing basic groups. The compounds displayed a high activity in the enzyme assay and displayed good activity in the cell-based (replicon) assay in the presence of serum proteins.