Highly Potent HCV NS4B Inhibitors with Activity against Multiple Genotypes
Journal of Medicinal Chemistry2014Vol. 57(5), pp. 2161–2166
Citations Over TimeTop 14% of 2014 papers
Barton W. Phillips, Ruby Cai, William E. Delaney, Zhimin Du, Mingzhe Ji, Haolun Jin, Johnny W. Lee, Jiayao Li, Anita Niedziela‐Majka, Michael Mish, Hyung‐Jung Pyun, Joe Saugier, Neeraj Tirunagari, Jianhong Wang, Huiling Yang, Qiaoyin Wu, Chris Sheng, C. Sebastian Zonte
Abstract
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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