Cyanohydrin as an anchoring group for potent and selective inhibitors of enterovirus 71 3C protease

Article abstract of DOI:10.1021/acs.jmedchem.5b01013

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.