Abstract：
In this study, 30 chalcone derivatives containing [1,2,4]-triazole-[4,3-a]-pyridine were designed and synthesized. The results of antibacterial activity showed that EC50 values of N26 against Xoo, Pcb was 36.41, 38.53 μg/mL, respectively, which were better than those of thiodiazole copper, whose EC50 values were 60.62, 106.75 μg/mL, respectively. The bacterial inhibitory activity of N26 against Xoo was verified by SEM. Antibacterial mechanism between N26 and Xoo was preliminarily explored, the experimental results showed that when the drug concentration was 100 mg/L, N26 had a good cell membrane permeability of Xoo, and it can inhibit the production of EPS content and extracellular enzyme content to disrupt the integrity of the Xoo biofilms achieving the effect of inhibiting Xoo. At 200 mg/L, N26 can protect and inhibit the lesions of post-harvested potatoes in vivo. The activities of N1-N30 against TMV were determined with half leaf dry spot method. The EC50 values of the curative and protective activity of N22 was 77.64 and 81.55 μg/mL, respectively, which were superior to those of NNM (294.27, 175.88 μg/mL, respectively). MST experiments demonstrated that N22 (Kd = 0.0076 ± 0.0007 μmol/L) had a stronger binding ability with TMV-CP, which was much higher than that of NNM (Kd = 0.7372 ± 0.2138 μmol/L). Molecular docking results showed that N22 had a significantly higher affinity with TMV-CP than NNM.
摘要：
在这项研究中,设计并合成了30种含[1,2,4]-三唑-[4,3-a]-吡啶的查耳酮衍生物。抗菌活性结果表明，N26对Xoo的EC50值，Pcb为36.41，38.53μg/mL，分别,比噻二唑铜更好，其EC50值分别为60.62,106.75μg/mL,分别。通过SEM验证了N26对Xoo的细菌抑制活性。初步探讨了N26与Xoo的抗菌机制,实验结果表明,当药物浓度为100mg/L时,N26具有良好的细胞膜通透性Xoo，能抑制EPS含量和胞外酶含量的产生，破坏Xoo生物膜的完整性，达到抑制Xoo的效果。在200mg/L时，N26可以保护和抑制马铃薯收获后的体内病变。用半叶干斑法测定N1-N30对TMV的活性。N22的治疗和保护活性的EC50值分别为77.64和81.55μg/mL,分别,优于NNM（294.27，175.88μg/mL，分别)。MST实验表明,N22(Kd=0.0076±0.0007μmol/L)与TMV-CP有较强的结合能力,远高于NNM(Kd=0.7372±0.2138μmol/L)。分子对接结果表明，N22与TMV-CP的亲和力明显高于NNM。
