Novel Ethyl-3-Aryl-2-Nitroacrylate Derivatives as Potential T3SS Inhibitors against Xanthomonas oryzae pv. oryzae on Rice

作者：Gao, Dongni; Li, Hui; Shao, Jiang; He, Lulu; Fu, Chen; Lai, Hongyu; Rothenberg, Dylan O'Neill; Xu, Xiaoli; Song, Gaopeng; Deng, Xin; Cui, Zi-Ning^*

来源：Journal of Agricultural and Food Chemistry, 2023, 71(24): 9291-9301.

DOI：10.1021/acs.jafc.3c00838

• ethyl-3-aryl-2-nitroacrylate
• synthesis
• typeIII secretion system (T3SS)
• inhibitors
• quorum quenching

Bacterial leaf blight (BLB) causedby Xanthomonasoryzae pv. oryzae (Xoo)is a highly destructivebacterial disease. Traditional prevention methods have utilized antibioticsto target bacterial growth, which has accelerated the emergence ofresistant strains. New prevention techniques are developing agentssuch as type III secretion system (T3SS) inhibitors that target bacterialvirulence factors without affecting bacterial growth. To explore novelT3SS inhibitors, a series of ethyl-3-aryl-2-nitroacrylate derivativeswere designed and synthesized. Preliminary screening of T3SS inhibitorswas based on the inhibition of the hpa1 gene promoterand showed no effect on bacterial growth. Compounds B9 and B10, obtained in the primary screening, significantlyinhibited the hypersensitive response (HR) in tobacco and the expressionof T3SS genes in the hrp cluster including key regulatorygenes. In vivo bioassays showed that T3SS inhibitorsobviously inhibited BLB and appeared to be more effective when combinedwith quorum quenching bacteria F20.

• 单位
  华南农业大学