3-(1, 1-Dioxo-2 H-(1, 2, 4)-benzothiadiazin-3-yl)-4-hydroxy-2 (1 H)-quinolinones, potent inhibitors of hepatitis C virus RNA-dependent RNA polymerase

R Tedesco, AN Shaw, R Bambal, D Chai…

文献索引：Tedesco, Rosanna; Shaw, Antony N.; Bambal, Ramesh; Chai, Deping; Concha, Nestor O.; Darcy, Michael G.; Dhanak, Dashyant; Fitch, Duke M.; Gates, Adam; Gerhardt, Warren G.; Halegoua, Dina L.; Han, Chao; Hofmann, Glenn A.; Johnston, Victor K.; Kaura, Arun C.; Liu, Nannan; Keenan, Richard M.; Lin-Goerke, Juili; Sarisky, Robert T.; Wiggall, Kenneth J.; Zimmerman, Michael N.; Duffy, Kevin J. Journal of Medicinal Chemistry, 2006 , vol. 49, # 3 p. 971 - 983

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被引用次数: 136

摘要

Recently, we disclosed a new class of HCV polymerase inhibitors discovered through high- throughput screening (HTS) of the GlaxoSmithKline proprietary compound collection. This interesting class of 3-(1, 1-dioxo-2 H-1, 2, 4-benzothiadiazin-3-yl)-4-hydroxy-2 (1 H)- quinolinones potently inhibits HCV polymerase enzymatic activity and inhibits the ability of the subgenomic HCV replicon to replicate in Huh-7 cells. This report will focus on the ...