Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 3, Pages 633-638Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.12.039
Keywords
HCV; HCV NS5B polymerase inhibitor; Pauson-Khand reaction; [1,3]-Dipolar cycloaddition
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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. (c) 2008 Elsevier Ltd. All rights reserved.
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