| Literature DB >> 19700319 |
Javier de Vicente1, Robert T Hendricks, David B Smith, Jay B Fell, John Fischer, Stacey R Spencer, Peter J Stengel, Peter Mohr, John E Robinson, James F Blake, Ramona K Hilgenkamp, Calvin Yee, Junping Zhao, Todd R Elworthy, Jahari Tracy, Elbert Chin, Jim Li, Al Lui, Beihan Wang, Connie Oshiro, Seth F Harris, Manjiri Ghate, Vincent J P Leveque, Isabel Najera, Sophie Le Pogam, Sonal Rajyaguru, Gloria Ao-Ieong, Ludmila Alexandrova, Bill Fitch, Michael Brandl, Mohammad Masjedizadeh, Shao-Yong Wu, Steve de Keczer, Tatyana Voronin.
Abstract
Benzothiazine-substituted tetramic acids were discovered as highly potent non-nucleoside inhibitors of HCV NS5B polymerase. X-ray crystallography studies confirmed the binding mode of these inhibitors with HCV NS5B polymerase. Rational optimization of time dependent inactivation of CYP 3A4 and clearance was accomplished by incorporation of electron-withdrawing groups to the benzothiazine core.Entities:
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Year: 2009 PMID： 19700319 DOI： 10.1016/j.bmcl.2009.08.023
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823