| Literature DB >> 19457662 |
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, George Adjabeng, Todd R Elworthy, Jahari Tracy, Elbert Chin, Jim Li, Beihan Wang, Joe T Bamberg, Rebecca Stephenson, Connie Oshiro, Seth F Harris, Manjiri Ghate, Vincent Leveque, Isabel Najera, Sophie Le Pogam, Sonal Rajyaguru, Gloria Ao-Ieong, Ludmila Alexandrova, Susan Larrabee, Michael Brandl, Andrew Briggs, Sunil Sukhtankar, Robert Farrell, Brian Xu.
Abstract
A new series of benzothiazine-substituted quinolinediones were evaluated as inhibitors of HCV polymerase NS5B. SAR studies on this series revealed a methyl sulfonamide group as a high affinity feature. Analogues with this group showed submicromolar potencies in the HCV cell based replicon assay. Pharmacokinetic and toxicology studies were also performed on a selected compound (34) to evaluate in vivo properties of this new class of inhibitors of HCV NS5B polymerase.Entities:
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Year: 2009 PMID： 19457662 DOI： 10.1016/j.bmcl.2009.05.004
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823