State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering; Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education; Research and Development Center for Fine Chemicals, Guizhou University, Guiyang, 550025, People's Republic of China.
Institute of Plant Protection and Soil Fertility, Hubei Academy of Agricultural Sciences, Wuhan, 430064, People's Republic of China.
Mol Divers. 2024 Apr;28(2):461-474. doi: 10.1007/s11030-022-10593-4. Epub 2023 Mar 25.
A series of chalcone derivatives containing 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole was designed and synthesized. Structures of all compounds were characterized by H NMR, C NMR, F NMR, and HRMS. The biological activities of the compounds were determined with the mycelial growth rate method, and further studies showed that some compounds had good antifungal activities at the concentration of 100 μg/mL. The EC value of compound L31 was 15.9 μg/mL against Phomopsis sp., which were better than that of azoxystrobin (EC value was 69.4 μg/mL). In addition, the mechanism of action of compound L31 shown that compound can affect mycelial growth by disrupting membrane integrity against Phomopsis sp., and that the higher the concentration of the compound is, the greater the disruption of membrane integrity is.
设计并合成了一系列含有 1,2,4-三唑并[3,4-b]-1,3,4-噻二唑的查尔酮衍生物。所有化合物的结构均通过 H NMR、C NMR、F NMR 和 HRMS 进行了表征。采用菌丝生长速率法测定了化合物的生物活性，进一步的研究表明，部分化合物在 100μg/mL 浓度下对病原菌具有良好的抑菌活性。化合物 L31 对辣椒疫霉的 EC 值为 15.9μg/mL，优于肟菌酯（EC 值为 69.4μg/mL）。此外，化合物 L31 的作用机制表明，化合物可以通过破坏细胞膜完整性来影响病原菌的菌丝生长，并且化合物的浓度越高，对细胞膜完整性的破坏越大。
