- Discovery of Potent EV71 Capsid Inhibitors for Treatment of HFMD
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Enterovirus 71 (EV71) is a major causative agent of hand, foot, and mouth disease (HFMD), which can spread its infections to the central nervous and other systems with severe consequences. The viral caspid protein VP1 is a well-known target for antiviral efficacy because its occupancy by suitable compounds could stabilize the virus capsid, thus preventing uncoating of virus for RNA release. In this Letter, design, synthesis, and biological evaluation of novel anti-EV71 agents (aminopyridyl 1,2,5-thiadiazolidine 1,1-dioxides) are described. One of the most promising compounds (14) showed excellent antiviral activity against EV71 (EC50 = 4 nM) and exhibited excellent in vivo efficacy in the EV71 infected mouse model.
- Li, Peng,Yu, Jun,Hao, Fei,He, Haiying,Shi, Xuyang,Hu, Jiao,Wang, Li,Du, Chunyan,Zhang, Xiao,Sun, Ya,Lin, Fusen,Gu, Zhengxian,Xu, Deming,Chen, Xinsheng,Shen, Liang,Hu, Guoping,Li, Jian,Chen, Shuhui,Xiao, Wei,Wang, Zhenzhong,Guo, Qingming,Chang, Xiujuan,Tian, Xuyang,Lin, Tianwei
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- Cyclohexane derivatives and their use as therapeutic agents
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The present invention relates compounds of formula (I), wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of formulae: (a), (b), (c), (d), and (e); and R1, R2, R3, R4, R5, R6, R7, R13, R14, R15, R16, R17, R21a and R21b are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.
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