Article
Highly potent HCV NS4B inhibitors with activity against multiple genotypes.
Journal of medicinal chemistry - 13 Mar 2014
Phillips Barton, Cai Ruby, Delaney William, Du Zhimin, Ji Mingzhe, Jin Haolun, Lee Johnny, Li Jiayao, Niedziela-Majka Anita, Mish Michael, Pyun Hyung-Jung, Saugier Joe, Tirunagari Neeraj, Wang Jianhong, Yang Huiling, Wu Qiaoyin, Sheng Chris, Zonte Catalin
Abstract excerpt
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.
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