Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1361319 | Bioorganic & Medicinal Chemistry Letters | 2012 | 4 Pages |
Abstract
A novel series of P3 oxo-modified macrocyclic hepatitis C virus NS3/4A serine protease inhibitor was designed, synthesized and biologically evaluated. The hydroxy-substituted inhibitor 10 demonstrated high potency in genotype 1a and 1b replicon and in the panel of HCV protease mutants. Interestingly, the t-butyl carbonate analog 9c, while not the most potent one in this series, exhibited a virtually flat potency profile in the panel of HCV protease mutants, thus providing opportunity for further optimization.
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Related Topics
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Organic Chemistry
Authors
Maosheng Duan, Wieslaw Kazmierski, Renae Crosby, Margaret Gartland, Jinjing Ji, Matt Tallant, Amy Wang, Robert Hamatake, Lois Wright, Min Wu, Yong-Kang Zhang, Charles Z. Ding, Xianfeng Li, Yang Liu, Suoming Zhang, Yasheen Zhou, Jacob J. Plattner,