摘要
Many pyrazole derivatives were reported to exhibit highly activity towards tobacco mosaic virus（TMV）.In this work,an optimized pyrazole Schiff base scaffold was designed and introduced to derive novel potential TMV inhibitors.Thirty-six compounds were synthesized,characterized by elemental analysis,mass spectra and nuclear magnetic resonance（NMR） spectroscopy and evaluated by biological experiments.The bioassay results showed that some of the synthesized compounds exhibited excellent anti-TMV activities.Especially,5-chloro-3-methyl-1H-pyrazole contained compound 4j showed ningnanmycin comparable inhibitory activity and can be considered as potential anti-TMV candidate agent.With molecular docking,compound 4j insert into nucleotide sequence（GAAGUU） of OriRNA stably which revealed nucleotide could be a target of these compounds.
Many pyrazole derivatives were reported to exhibit highly activity towards tobacco mosaic virus（TMV）.In this work,an optimized pyrazole Schiff base scaffold was designed and introduced to derive novel potential TMV inhibitors.Thirty-six compounds were synthesized,characterized by elemental analysis,mass spectra and nuclear magnetic resonance（NMR） spectroscopy and evaluated by biological experiments.The bioassay results showed that some of the synthesized compounds exhibited excellent anti-TMV activities.Especially,5-chloro-3-methyl-1H-pyrazole contained compound 4j showed ningnanmycin comparable inhibitory activity and can be considered as potential anti-TMV candidate agent.With molecular docking,compound 4j insert into nucleotide sequence（GAAGUU） of OriRNA stably which revealed nucleotide could be a target of these compounds.
基金
supported by National Natural Science Foundation of China (No. 21302002)
Anhui Provincial Natural Science Foundation (No. 1408085QB33)
Key Scientific and Technological Project of Anhui Provincial Tobacoo Company (No. 20150551007)
