Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1372866 | Bioorganic & Medicinal Chemistry Letters | 2009 | 6 Pages |
Abstract
The discovery of 5,5′- and 6,6′-dialkyl-5,6-dihydro-1H-pyridin-2-ones as potent inhibitors of the HCV RNA-dependent RNA polymerase (NS5B) is described. Several of these agents also display potent antiviral activity in cell culture experiments (EC50 <0.10 μM). In vitro DMPK data for selected compounds as well as crystal structures of representative inhibitors complexed with the NS5B protein are also disclosed.
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Authors
David A. Ellis, Julie K. Blazel, Chinh V. Tran, Frank Ruebsam, Douglas E. Murphy, Lian-Sheng Li, Jingjing Zhao, Yuefen Zhou, Helen M. McGuire, Alan X. Xiang, Stephen E. Webber, Qiang Zhao, Qing Han, Charles R. Kissinger, Matthew Lardy, Alberto Gobbi,