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Pyrrolo[1,2-b]pyridazin-2-ones as potent inhibitors of HCV NS5B polymerase |
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| Authors: | Ruebsam Frank Webber Stephen E Tran Martin T Tran Chinh V Murphy Douglas E Zhao Jingjing Dragovich Peter S Kim Sun Hee Li Lian-Sheng Zhou Yuefen Han Qing Kissinger Charles R Showalter Richard E Lardy Matthew Shah Amit M Tsan Mei Patel Rupal Lebrun Laurie A Kamran Ruhi Sergeeva Maria V Bartkowski Darian M Nolan Thomas G Norris Daniel A Kirkovsky Leo |
| Affiliation: | Anadys Pharmaceuticals, Inc., 3115 Merryfield Row, San Diego, CA 92121, USA. fruebsam@anadyspharma.com |
| Abstract: | Pyrrolo[1,2-b]pyridazin-2-one analogs were discovered as a novel class of inhibitors of genotype 1 HCV NS5B polymerase. Structure-based design led to the discovery of compound 3 k, which displayed potent inhibitory activities in biochemical and replicon assays (IC(50) (1b)<10nM; EC(50) (1b)=12 nM) as well as good stability towards human liver microsomes (HLM t(1/2)>60 min). |
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