Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1372256 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
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.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Javier de Vicente, 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,