期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 28, 期 17, 页码 2979-2984出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2018.06.049
关键词
Pyrazolo [3, 4-d]pyrimidine; Schiff base; Antiviral activity; Molecular docking
资金
- National Natural Science Foundation of China [21562012, 21762012]
- National Key Technologies RD Project [2017YFD0201302-03]
- S&T Planning Project of Guizhou Province [[2017]1402]
- Guizhou Province Governor Foundation for Outstanding Talents [2015-15]
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.
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