62491-96-7Relevant articles and documents
Discovery of Potent EV71 Capsid Inhibitors for Treatment of HFMD
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
supporting information, p. 841 - 846 (2017/08/16)
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.
INHIBITORS OF PROTEIN TYROSINE KINASE ACTIVITY
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Page/Page column 66, (2010/11/29)
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Synthesis and antipicornavirus activity of (R)- and (S)-1-[5-(4′- chlorobiphenyl-4-yloxy)-3-methylpentyl]-3-pyridin-4-yl-imidazolidin-2-one
Chern, Jyh-Haur,Chang, Chih-Shiang,Tai, Chia-Liang,Lee, Yen-Chun,Lee, Chung-Chi,Kang, Iou-Jiun,Lee, Ching-Yin,Shih, Shin-Ru
, p. 4206 - 4211 (2007/10/03)
The new pyridyl imidazolidinone derivative, 1-[5-(4′-chlorobiphenyl- 4-yloxy)-3-methylpentyl]-3-pyridin-4-yl-imidazolidin-2-one (±)-1a, was synthesized and found to have an excellent antiviral activity against EV71 (IC50 = 0.009 μM). Therefore, both the enantiomers, (S)-(+)-1a and (R)-(-)-1a, have been prepared starting from readily available monomethyl (R)-3-methylglutarate (7) as a useful chiral building block and their antiviral activity was evaluated in a plaque reduction assay. Interestingly, we observed that the enantiomer (S)-(+)-1a was 10-fold more active against enterovirus71 (EV71) (IC50 = 0.003 μM) than the corresponding enantiomer (R)-(-)-1a (IC50 = 0.033 μM). Similar results were found against all five strains (1743, 2086, 2231, 4643, and BrCr) of EV71 tested. This demonstrated that the absolute configuration of the chiral carbon atom at the 3-position of the alkyl linker considerably influenced the anti-EV71 activity of these pyridyl imidazolidinones.