Synthesis and biological activity of heteroaryl 3-(1,1-dioxo-2H-(1,2,4)-benzothiadizin-3-yl)-4-hydroxy-2(1H)-quinolinone derivatives as hepatitis C virus NS5B polymerase inhibitors |
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| Authors: | Rosanna Tedesco Deping Chai Michael G Darcy Dashyant Dhanak Duke M Fitch Adam Gates Victor K Johnston Richard M Keenan Juili Lin-Goerke Robert T Sarisky Antony N Shaw Klara L Valko Kenneth J Wiggall Michael N Zimmerman Kevin J Duffy |
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| Institution: | 1. Department of Medicinal Chemistry, GlaxoSmithKline Pharmaceuticals, Collegeville, PA 19426, USA;2. Department of Virology, GlaxoSmithKline Pharmaceuticals, Collegeville, PA 19426, USA;3. Department of Analytical Sciences, GlaxoSmithKline Pharmaceuticals, Stevenage, Herts, SG1 2NY, UK |
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| Abstract: | Modification of the benzo rings of 3-(1,1-dioxo-2H-(1,2,4)-benzothiadiazin-3-yl)-4-hydroxy-2(1H)-quinolinones into heteroaromatic systems was investigated to enhance physicochemical properties and potency profile of this class of inhibitors. The synthesis and biological activity of the derived compounds is discussed. |
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