| Literature DB >> 21145235 |
Dange V Kumar1, Roopa Rai, Ken A Brameld, John R Somoza, Ravi Rajagopalan, James W Janc, Yu M Xia, Tony L Ton, Michael B Shaghafi, Huiyong Hu, Isabelle Lehoux, Nhat To, Wendy B Young, Michael J Green.
Abstract
Hepatitis C virus (HCV) infection is treated with a combination of peginterferon alfa-2a/b and ribavirin. To address the limitations of this therapy, numerous small molecule agents are in development, which act by directly affecting key steps in the viral life-cycle. Herein we describe our discovery of quinolone derivatives, novel small-molecules that inhibit NS5b polymerase, a key enzyme of the viral life-cycle. A crystal structure of a quinoline analog bound to NS5B reveals that this class of compounds binds to allosteric site-II (non-nucleoside inhibitor-site 2, NNI-2) of this protein.Entities:
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Year: 2010 PMID： 21145235 DOI： 10.1016/j.bmcl.2010.11.068
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823