氰醇
化学
蛋白酵素
部分
蛋白酶
选择性
立体化学
半胱氨酸
生物化学
酶
催化作用
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
标识
DOI:10.1021/acs.jmedchem.5b01013
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.
科研通智能强力驱动
Strongly Powered by AbleSci AI