Zhai Yangyang, Zhao Xiangshuai, Cui Zhengjie, Wang Man, Wang Yaxin, Li Linfeng, Sun Qi, Yang Xi, Zeng Debin, Liu Ying, Sun Yuna, Lou Zhiyong, Shang Luqing, Yin Zheng
College of Pharmacy and State Key Laboratory of Elemento-Organic Chemistry, Nankai University , 94 Weijin Road, Nankai District, Tianjin 300071, China.
Collaborative Innovation Center of Chemical Science and Engineering (Tianjin) , Tianjin 300071, China.
J Med Chem. 2015 Dec 10;58(23):9414-20. doi: 10.1021/acs.jmedchem.5b01013. Epub 2015 Nov 25.
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.
已合成氰醇衍生物作为肠道病毒71型（EV71）3C蛋白酶（3C（pro））抑制剂，并对其生化和抗病毒活性进行了测定。与已报道的抑制剂相比，氰醇（1S，2S，2'S，5S）-16和（1R，2S，2'S，5S）-16表现出显著提高的活性以及针对其他蛋白酶的良好选择性，这是氰醇部分与3C（pro）催化位点之间特异性相互作用的结果。氰醇作为具有高选择性和优异抑制活性的锚定基团，是半胱氨酸蛋白酶抑制剂的一个有用选择。
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