文献类型：期刊文献

英文题名：Pyrazolo[3,4-d]pyrimidine derivatives containing a Schiff base moiety as potential antiviral agents

作者：Wang, Yan-Yan Xu, Fang-Zhou Zhu, Yun-Ying Song, Baoan Liu, Dexia Yu, Gang Chen, Shunhong Xue, Wei Wu, Jian

第一作者：Wang, Yan-Yan

通信作者：Song, BA[1];Wu, J[1]

机构：[1]Guizhou Univ, Res & Dev Ctr Fine Chem, State Key Lab Breeding Base Green Pesticide & Agr, Key Lab Green Pesticide & Agr Bioengn,Minist Educ, Guiyang 550025, Guizhou, Peoples R China;[2]Guizhou Inst Technol, Sch Chem Engn, Guiyang 550001, Guizhou, Peoples R China

第一机构：Guizhou Univ, Res & Dev Ctr Fine Chem, State Key Lab Breeding Base Green Pesticide & Agr, Key Lab Green Pesticide & Agr Bioengn,Minist Educ, Guiyang 550025, Guizhou, Peoples R China

通信机构：corresponding author), Guizhou Univ, Res & Dev Ctr Fine Chem, State Key Lab Breeding Base Green Pesticide & Agr, Key Lab Green Pesticide & Agr Bioengn,Minist Educ, Guiyang 550025, Guizhou, Peoples R China.

年份：2018

卷号：28

期号：17

起止页码：2979-2984

外文期刊名：BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

收录：;Scopus(收录号：2-s2.0-85049465355);WOS:【SCI-EXPANDED(收录号:WOS:000441514700033)】；

基金：This work was supported by the National Natural Science Foundation of China (Nos. 21562012, No. 21762012), the National Key Technologies R&D Project (No. 2017YFD0201302-03), the S&T Planning Project of Guizhou Province (No. [2017]1402), and the Guizhou Province Governor Foundation for Outstanding Talents (No. 2015-15#).

语种：英文

外文关键词：Pyrazolo [3, 4-d]pyrimidine; Schiff base; Antiviral activity; Molecular docking

摘要：A series of pyrazolo [3,4-d]pyrimidine derivatives containing a Schiff base moiety were synthesized, characterised, and evaluated for their activity against tobacco mosaic virus (TMV). Biological assays indicated that several of the derivatives exhibited significant activity against TMV. In particularly, compounds 5y and 5aa displayed excellent inactivating activity against TMV, with half maximal effective concentration (EC50) values of 70.3 and 53.65 mu g/mL, respectively, which were much better than that of ribavirin (150.45 mu g/mL), and 5aa was superior to ningnanmycin (EC50 = 55.35 mu g/mL). Interactions of compounds 5y and 5aa with TMV coat protein (TMV-CP) were investigated using microscale thermophoresis and molecular docking. Compounds 5y and 5aa displayed strong binding capability to TMV-CP with dissociation constant (K-d) values of 22.6 and 9.8 mu M, respectively. These findings indicate that pyrazolo [3,4-d]pyrimidine derivatives containing a Schiff base may be potential antiviral agents.