| Literature DB >> 19796938 |
David A Ellis1, 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, Richard E Showalter, Amit M Shah, Mei Tsan, Rupal A Patel, Laurie A LeBrun, Ruhi Kamran, Darian M Bartkowski, Thomas G Nolan, Daniel A Norris, Maria V Sergeeva, Leo Kirkovsky.
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 microM). In vitro DMPK data for selected compounds as well as crystal structures of representative inhibitors complexed with the NS5B protein are also disclosed.Entities:
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Year: 2009 PMID： 19796938 DOI： 10.1016/j.bmcl.2009.09.051
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823