文献类型：期刊文献

英文题名：Synthesis and Docking Study of N-(Cinnamoyl)-N′-(substituted)acryloyl Hydrazide Derivatives Containing Pyridinium Moieties as a Novel Class of Filamentous Temperature-Sensitive Protein Z Inhibitors against the Intractable Xanthomonas oryzae pv. oryzae Infections in Rice

作者：Zhou, Xiang[1];Feng, Yu-Mei[1];Qi, Pu-Ying[1];Shao, Wu-Bin[1];Wu, Zhi-Bing[1];Liu, Li-Wei[1];Wang, Yi[1];Ma, Hao-Dong[1];Wang, Pei-Yi[1];Li, Zhong[2];Yang, Song[1,2]

机构：[1]Guizhou Univ, State Key Lab Breeding Base Green Pesticide & Agr, Key Lab Green Pesticide & Agr Bioengn, Minist Educ,Ctr R&D Fine Chem, Guiyang 550025, Peoples R China;[2]East China Univ Sci & Technol, Coll Pharm, Shanghai 200237, Peoples R China

年份：2020

卷号：68

期号：31

起止页码：8132

外文期刊名：JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY

收录：;EI(收录号：20203609123444);WOS:【SCI-EXPANDED(收录号:WOS:000558794400004)】；

基金：We acknowledge the National Natural Science Foundation of China (nos. 21877021, 21702037, 31860516, and 21662009), Research Project of Ministry of Education of China (nos. 20135201110005 and 213033A), Guizhou Provincial S&T Program (no. [2017]5788), and Program of Introducing Talents of Discipline to Universities of China (111 Program, no. D20023).

语种：英文

外文关键词：rice bacterial blight; diacylhydrazine derivatives; FtsZ inhibitor; antibacterial assay

摘要：Xanthomonas oryzae pv. oryzae (Xoo) is an offensive phytopathogen that can invade a wide range of plant hosts to develop bacterial diseases, including the well-known rice bacterial leaf blight. However, few agrochemicals have been identified to effectively prevent and eliminate Xoo-induced diseases. Thus, designing novel antibacterial compounds on the basis of the potential targets from Xoo may lead to the discovery of highly efficient and innovative anti-Xoo agents. Filamentous temperature-sensitive protein Z (FtsZ), an important functional protein in the progression of cell division, has been widely reported and exploited as a target for creating antibacterial drugs in the field of medicine. Therefore, the fabrication of innovative frameworks targeting XooFtsZ may be an effective method for managing bacterial leaf blight diseases via blocking the binary division and reproduction of Xoo. As such, a series of novel N-(cinnamoyl)-N'-(substituted)acryloyl hydrazide derivatives containing pyridinium moieties were designed, and the anti-Xoo activity was determined. The bioassay results showed that compound A7 had excellent anti-Xoo activity (EC50 = 0.99 mg L-1) in vitro and distinct curative activity (63.2% at 200 mg L-1) in vivo. Further studies revealed that these designed compounds were XooFtsZ inhibitors, validating by the reduced GTPase activity of recombinant XooFtsZ, the nonfilamentous XooFtsZ assembly observed in the TEM images, and the prolonged Xoo cells from the fluorescence patterns. Computational docking studies showed that compound A(7) had strong interactions with ASN34, GLN193, and GLN197 residues located in the alpha helix regions of XooFtsZ. The present study demonstrates the developed FtsZ inhibitors can serve as agents to control Xoo-induced infections.