Highly Potent HCV NS4B Inhibitors with Activity against Multiple Genotypes

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• 作者：Barton Phillips ; Ruby Cai ; William Delaney ; Zhimin Du ; Mingzhe Ji ; Haolun Jin ; Johnny Lee ; Jiayao Li ; Anita Niedziela-Majka ; Michael Mish ; Hyung-Jung Pyun ; Joe Saugier ; Neeraj Tirunagari ; Jianhong Wang ; Huiling Yang ; Qiaoyin Wu ; Chris Sheng ; Catalin Zonte
• 刊名：Journal of Medicinal Chemistry
• 出版年：2014
• 出版时间：March 13, 2014
• 年：2014
• 卷：57
• 期：5
• 页码：2161-2166
• 全文大小：304K
• 年卷期：v.57,no.5(March 13, 2014)
• ISSN：1520-4804

文摘

The exploration of novel inhibitors of the HCV NS4B protein that are based on a 2-oxadiazoloquinoline scaffold is described. Optimization to incorporate activity across genotypes led to a potent new series with broad activity, of which inhibitor 1 displayed the following EC₅₀ values: 1a, 0.08 nM; 1b, 0.10 nM; 2a, 3 nM; 2b, 0.6 nM, 3a, 3.7 nM; 4a, 0.9 nM; 6a, 3.1 nM.