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Discovery of Potent EV71 Capsid Inhibitors for Treatment of HFMD.

ABSTRACT: 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.

SUBMITTER: Li P

PROVIDER: S-EPMC5554915 | biostudies-literature | 2017 Aug

REPOSITORIES: biostudies-literature

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Discovery of Potent EV71 Capsid Inhibitors for Treatment of HFMD.

Li Peng P Yu Jun J Hao Fei F He Haiying H Shi Xuyang X Hu Jiao J Wang Li L Du Chunyan C Zhang Xiao X Sun Ya Y Lin Fusen F Gu Zhengxian Z Xu Deming D Chen Xinsheng X Shen Liang L Hu Guoping G Li Jian J Chen Shuhui S Xiao Wei W Wang Zhenzhong Z Guo Qingming Q Chang Xiujuan X Tian Xuyang X Lin Tianwei T

ACS medicinal chemistry letters 20170710 8

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 ...[more]

PMID: 28835799

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