Cyanohydrin as an Anchoring Group for Potent and Selective Inhibitors of Enterovirus 71 3C Protease

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• 作者：Yangyang Zhai ; Xiangshuai Zhao ; Zhengjie Cui ; Man Wang ; Yaxin Wang ; Linfeng Li ; Qi Sun ; Xi Yang ; Debin Zeng ; Ying Liu ; Yuna Sun ; Zhiyong Lou ; Luqing Shang ; Zheng Yin
• 刊名：Journal of Medicinal Chemistry
• 出版年：2015
• 出版时间：December 10, 2015
• 年：2015
• 卷：58
• 期：23
• 页码：9414-9420
• 全文大小：423K
• ISSN：1520-4804

文摘

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鈥?i>S,5S)-16 and (1R,2S,2鈥?i>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.