摘要: Cyanohydrin derivatives as enterovirus 71 (EV71) 3C protease (3C(pro)) inhibitors have been synthesized and assayed for their biochemical and antiviral activities. Compared with the reported inhibitors, cyanohydrins (1S,2S,2'S,5S)-16 and (1R,2S,2'S,5S)-16 exhibited significantly improved activity and attractive selectivity profiles against other proteases, which were a result of the specific interactions between the cyanohydrin moiety and the catalytic site of 3C(pro). Cyanohydrin as an anchoring group with high selectivity and excellent inhibitory activity represents a useful choice for cysteine protease inhibitors.
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期刊：
JOURNAL OF MEDICINAL CHEMISTRY
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分类：
生物学
>>
生物物理学
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引用：
ChinaXiv:201605.01253
(或此版本
ChinaXiv:201605.01253V1)
DOI:10.12074/201605.01253V1
CSTR:32003.36.ChinaXiv.201605.01253.V1
- 推荐引用方式：
Zhai, Yangyang,Zhao, Xiangshuai,Cui, Zhengjie,Wang, Man,Li, Linfeng,Yang, Xi,Zeng, Debin,Liu, Ying,Shang, Luqing,Yin, Zheng,Zhai, Yangyang,Zhao, Xiangshuai,Cui, Zhengjie,Wang, Man,Li, Linfeng,Yang, Xi,Zeng, Debin,Liu, Ying,Shang, Luqing,Yin, Zheng,Zhai, Yangyang,Zhao, Xiangshuai,Cui, Zhengjie,Wang, Man,Li, Linfeng,Yang, Xi,Zeng, Debin,Liu, Ying,Shang, Luqing,Yin, Zheng,Wang, Yaxin,Lou, Zhiyong,Wang, Yaxin,Lou, Zhiyong,Wang, Yaxin,Lou, Zhiyong,Sun, Qi,Sun, Qi,Sun, Yuna.(2016).Cyanohydrin as an Anchoring Group for Potent and Selective Inhibitors of Enterovirus 71 3C Protease.中国科学院科技论文预发布平台.[ChinaXiv:201605.01253]
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