Discovery of novel double pyrazole Schiff base derivatives as anti-tobacco mosaic virus (TMV) agents

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• 作者：Xian-Hai Lv^a ; Zi-Li Ren^a ; Dong-Dong Li^c ; ^d ; Ban-Feng Ruan^b ; ^{ruanbf@huft.edu.cn} ; Qing-Shan Li^b ; Ming-Jie Chu^a ; Cheng-Ying Ai^a ; Dao-Hong Liu^a ; Kai Mo^a ; Hai-Qun Cao^a ; ^{haiquncao@163.com}
• 关键词：Pyrazole ; Schiff base ; Anti-TMV ; Molecule docking
• 刊名：Chinese Chemical Letters
• 出版年：2017
• 出版时间：February 2017
• 年：2017
• 卷：28
• 期：2
• 页码：377-382
• 全文大小：788 K
• 卷排序：28

文摘

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.