A series of new 1,4-pentadien-3-one derivatives containing 1,2,4-triazole moiety were synthesized. The structures of the synthesized compounds were charactered via ¹H NMR, ¹³C NMR and HRMS. Antibacterial bioassays indicated that some of compounds showed potential antibacterial activities against Ralstonia solanacearum (Rs), Xanthomonas oryzae pv. Oryzae (Xoo) and Xanthomonas axonopodis pv. Citri (Xac). Compounds F₈ and F₁₇ showed good in vitro antibacterial activities against Rs, with the EC₅₀ values of 18.6 and 18.6 μg/mL, respectively, which were better than commercial agent bismerthiazol (55.2 μg/mL). Furthermore, compounds F₁₂ and F₁₅ showed good in vitro antibacterial activities against Xoo, with the EC₅₀ values of 10.9 and 17.5 μg/mL, which were better than commercial agent bismerthiazol (69.3 μg/mL). Moreover, compounds F₂, F₉, F₁₆ and F₁₇ showed good in vitro antibacterial activities against Xac, with the EC₅₀ values of 6.6, 5.4, 7.5 and 7.8 μg/mL, respectively, which were better than commercial agent bismerthiazol (54.9 μg/mL). The effect of compound F₉ on Xac bacterial cell membrane rupture was observed by scanning electron microscopy (SEM). In addition, antiviral bioassays indicated that some of compounds showed excellent protection activities against tobacco mosaic virus (TMV). Compounds F₅ and F₁₅ showed good protecting activity against TMV, with the EC₅₀ values of 108.3 and 105.4 μg/mL, respectively, which were better than commercial agent ningnanmycin (214.7 μg/mL). Microscale thermophoresis (MST) also showed that the binding of compound F₂ to TMV coat protein (TMV-CP) yielded a Kd value of 1.260 ± 0.654 μmol/L, which was very close to ningnanmycin (1.058 ± 0.286 μmol/L). Similarly, the molecular docking studies for F₂ and F₅ with TMV-CP (PDB code: 1EI7, ID: 4QGH) indicated that compounds F₂ and F₅ had partially interacted with TMV-CP.

合成了一系列含有1,2,4-三唑部分的新的1,4-戊二烯-3-酮衍生物。合成的化合物的结构通过¹ H NMR，¹³ C NMR和HRMS表征。抗菌生物测定表明，某些化合物显示针对潜在的抗菌活性青枯雷尔氏菌（卢比），水稻白叶枯病菌。菌（白叶枯病）和黄axonopodis PV。柠檬（Xac）。化合物F ₈和F ₁₇对EC具有良好的体外抗Rs抗菌活性。₅₀值分别为18.6和18.6μg/ mL，优于商业药物比美噻唑（55.2μg/ mL）。此外，化合物F ₁₂和F ₁₅对Xoo表现出良好的体外抗菌活性，EC ₅₀值为10.9和17.5μg/ mL，优于市售药物比美噻唑（69.3μg/ mL）。此外，化合物F ₂，F ₉，F ₁₆和F ₁₇在EC _50下显示出良好的体外抗Xac抗菌活性。分别为6.6、5.4、7.5和7.8μg/ mL的值，比市售药物比美噻唑（54.9μg/ mL）更好。通过扫描电子显微镜（SEM）观察到化合物F ₉对Xac细菌细胞膜破裂的作用。此外，抗病毒生物测定表明某些化合物对烟草花叶病毒（TMV）表现出出色的保护活性。化合物F ₅和F ₁₅表现出良好的针对TMV的保护活性，EC ₅₀值分别为108.3和105.4μg/ mL，优于商业制剂宁南霉素（214.7μg/ mL）。微型热泳（MST）还显示了化合物F ₂的结合TMV外壳蛋白（TMV-CP）的Kd值为1.260±0.654μmol/ L，非常接近宁南霉素（1.058±0.286μmol/ L）。同样，F ₂和F ₅与TMV-CP的分子对接研究（PDB代码：1EI7，ID：4QGH）表明，化合物F ₂和F ₅与TMV-CP部分相互作用。