Article

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

Department of Medicinal Chemistry, IRBM P. Angeletti S.p.A., Merck Research Laboratories Rome, Via Pontina km 30,600, I-00040 Pomezia, Rome, Italy.
Bioorganic & medicinal chemistry letters (Impact Factor: 2.33). 02/2009; 19(3):633-8. DOI: 10.1016/j.bmcl.2008.12.039
Source: PubMed

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.

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