Sie befinden Sich nicht im Netzwerk der Universität Paderborn. Der Zugriff auf elektronische Ressourcen ist gegebenenfalls nur via VPN oder Shibboleth (DFN-AAI) möglich. mehr Informationen...
A series of pyrazolo[3,4-d]pyrimidine derivatives containing Schiff base was synthesized. Compounds 5y and 5aa exhibited excellent antiviral activity against TMV. The interaction mode of 5y and 5aa with TMV-CP was conducted through molecular docking and microscale thermophoresis (MST) techniques.
[Display omitted]
•Pyrazolo[3,4-d]pyrimidines with a Schiff base moiety were synthesized.•Compounds 5y and 5aa exhibited excellent antiviral activity against TMV.•Interactions of 5y (5aa) with TMV-CP were conducted using MST and docking.•Compound 5aa showed strong combining capability with TMV-CP.
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 μg/mL, respectively, which were much better than that of ribavirin (150.45 μg/mL), and 5aa was superior to ningnanmycin (EC50 = 55.35 μg/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 (Kd) values of 22.6 and 9.8 μM, respectively. These findings indicate that pyrazolo[3,4-d]pyrimidine derivatives containing a Schiff base may be potential antiviral agents.