1065478-35-4Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of peptidomimetic aldehydes as broad-spectrum inhibitors against enterovirus and sars-cov-2
Dai, Wenhao,Jochmans, Dirk,Xie, Hang,Yang, Hang,Li, Jian,Su, Haixia,Chang, Di,Wang, Jiang,Peng, Jingjing,Zhu, Lili,Nian, Yong,Hilgenfeld, Rolf,Jiang, Hualiang,Chen, Kaixian,Zhang, Leike,Xu, Yechun,Neyts, Johan,Liu, Hong
, (2021/05/06)
A novel series of peptidomimetic aldehydes was designed and synthesized to target 3C protease (3Cpro) of enterovirus 71 (EV71). Most of the compounds exhibited high antiviral activity, and among them, compound 18p demonstrated potent enzyme inhibitory activity and broad-spectrum antiviral activity on a panel of enteroviruses and rhinoviruses. The crystal structure of EV71 3Cpro in complex with 18p determined at a resolution of 1.2 ? revealed that 18p covalently linked to the catalytic Cys147 with an aldehyde group. In addition, these compounds also exhibited good inhibitory activity against the 3CLpro and the replication of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), especially compound 18p (IC50 = 0.034 μM, EC50 = 0.29 μM). According to our previous work, these compounds have no reasons for concern regarding acute toxicity. Compared with AG7088, compound 18p also exhibited good pharmacokinetic properties and more potent anticoronavirus activity, making it an excellent lead for further development.
Design, synthesis, and evaluation of 3C protease inhibitors as anti-enterovirus 71 agents
Kuo, Chih-Jung,Shie, Jiun-Jie,Fang, Jim-Min,Yen, Guei-Rung,Hsu, John T.-A.,Liu, Hun-Ge,Tseng, Sung-Nain,Chang, Shih-Cheng,Lee, Ching-Yin,Shih, Shin-Ru,Liang, Po-Huang
, p. 7388 - 7398 (2008/12/22)
Human enterovirus (EV) belongs to the picornavirus family, which consists of over 200 medically relevant viruses. A peptidomimetic inhibitor AG7088 was developed to inhibit the 3C protease of rhinovirus (a member of the family), a chymotrypsin-like protea
