52210-90-9Relevant 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
, 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
-
Page/Page column 66, (2010/11/29)
-
Design, synthesis, and antipicornavirus activity of 1-[5-(4-arylphenoxy) alkyl]-3-pyridin-4-ylimidazolidin-2-one derivatives
Chang, Chih-Shiang,Lin, Ying-Ting,Shih, Shin-Ru,Lee, Chung-Chi,Lee, Yen-Chun,Tai, Chia-Liang,Tseng, Sung-Nien,Chern, Jyh-Haur
, p. 3522 - 3535 (2007/10/03)
A series of pyridylimidazolidinone derivatives was synthesized and tested in vitro against enterovirus 71 (EV71). On the basis of compound 33 (DBPR103), introduction of a methyl group at the 2- or 3-position of the linker between the imidazolidinone and the biphenyl resulted in markedly improved antiviral activity toward EV71 with IC50 values of 5.0 nM (24b) and 9.3 nM (14a), respectively. Increasing the branched chain to propyl resulted in a progressive decrease in activity, while inserting different heteroatoms entirely rendered the compound only weakly active. The introduction of a bulky group (cyclohexyl, phenyl, or benzyl) led to loss of activity against EV71. The 4-chlorophenyl moiety in 14a was replaced with bioisosteric groups such as oxadiazole (28a-d) or tetrazole (32a,b), dramatically improving anti-EV71 activity and selectivity indices. Compounds 14a, 24b, 28b, 28d, and 32a exhibited a strong activity against lethal EV71, and no apparent cellular toxicity was observed. Three of the more potent imidazolidinone compounds, 14a, 28b, and 32b, were subjected to a large group of picornaviruses to determine their spectrum of antiviral activity.