Wang Pei-Yi, Zhou Lei, Zhou Jian, Wu Zhi-Bing, Xue Wei, Song Bao-An, Yang Song
State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals of Guizhou University, Guiyang 550025, China.
State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals of Guizhou University, Guiyang 550025, China.
Bioorg Med Chem Lett. 2016 Feb 15;26(4):1214-7. doi: 10.1016/j.bmcl.2016.01.029. Epub 2016 Jan 12.
By introducing the pyridinium group into 2,5-substituted-1,3,4-oxadiazole, a series of pyridinium-tailored 2,5-substituted-1,3,4-oxadiazole thioether/sulfoxide/sulfone derivatives were obtained, and their antibacterial activities were evaluated via turbidimeter test in vitro. The bioassays reveal that most of the target compounds exhibit better inhibition activities against pathogen Xanthomonas oryzae pv. oryzae, Ralstonia solanacearum, and Xanthomonas axonopodis pv. citri than positive controls bismerthiazol (CK1) or thiodiazole copper (CK2). Among them, I-8, I-10, I-12, II-10, II-12, III-10, and III-12 exert excellent inhibition activities against the three pathogenic bacteria with the half-maximal effective concentration (EC50) values ranging from 0.54 to 12.14 μg/mL. Our results demonstrate that pyridinium-tailored 1,3,4-oxadiazole thioether/sulfoxide/sulfone derivatives can serve as potential alternative bactericides for the management of plant bacterial diseases.
通过将吡啶鎓基团引入2,5-二取代-1,3,4-恶二唑，获得了一系列吡啶鎓修饰的2,5-二取代-1,3,4-恶二唑硫醚/亚砜/砜衍生物，并通过体外比浊法测试评估了它们的抗菌活性。生物测定表明，大多数目标化合物对水稻白叶枯病菌、青枯雷尔氏菌和柑橘溃疡病菌的抑制活性优于阳性对照叶枯唑（CK1）或噻菌铜（CK2）。其中，I-8、I-10、I-12、II-10、II-12、III-10和III-12对这三种病原菌具有优异的抑制活性，半数有效浓度（EC50）值在0.54至12.14μg/mL之间。我们的结果表明，吡啶鎓修饰的1,3,4-恶二唑硫醚/亚砜/砜衍生物可作为潜在的替代杀菌剂用于植物细菌性病害的防治。
