Wu Sikai, Shi Jing, Chen Jixiang, Hu Deyu, Zang Liansheng, Song Baoan
State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for Research and Development of Fine Chemicals, Guizhou University, Guiyang 550025, People's Republic of China.
J Agric Food Chem. 2021 Apr 28;69(16):4645-4654. doi: 10.1021/acs.jafc.1c01204. Epub 2021 Apr 19.
A series of novel 6-sulfonyl-1,2,4-triazolo[3,4-][1,3,4]thiadiazole derivatives were designed and synthesized. CoMFA models were established to analyze the quantitative structure-activity relationships on the basis of the EC values of the compounds. The models were used to design and synthesize compounds and with higher activities. The EC values of compound against pv. () and pv. () were 0.59 and 1.63 mg/L, respectively, which were higher than those of thiodiazole copper (90.43 and 97.93 mg/L) and bismerthiazol (68.37 and 75.59 mg/L). Moreover, protective activities of compound against bacterial leaf streak (BLS) and bacterial leaf blight (BLB) were 49.65% and 49.42%, respectively, which were superior to those of thiodiazole copper (44.28% and 41.51%) and bismerthiazol (38.89% and 40.09%). Protective activity of compound against BLS was closely related to the improvement of defense-related enzyme activities, chlorophyll content, and photosynthesis activation. This is consistent with the upregulated expression of defense responses and photosynthesis-related proteins.
设计并合成了一系列新型的6-磺酰基-1,2,4-三唑并[3,4-b][1,3,4]噻二唑衍生物。基于化合物的EC值建立了CoMFA模型以分析定量构效关系。这些模型用于设计和合成具有更高活性的化合物 和 。化合物 对水稻白叶枯病菌（Xanthomonas oryzae pv. oryzae）和水稻条斑病菌（Xanthomonas oryzae pv. oryzicola）的EC值分别为0.59和1.63 mg/L，高于噻菌铜（90.43和97.93 mg/L）和噻霉酮（68.37和75.59 mg/L）。此外，化合物 对水稻细菌性条斑病（BLS）和水稻白叶枯病（BLB）的保护活性分别为49.65%和49.42%，优于噻菌铜（44.28%和41.51%）和噻霉酮（38.89%和40.09%）。化合物 对BLS的保护活性与防御相关酶活性、叶绿素含量及光合作用活性的提高密切相关。这与防御反应和光合作用相关蛋白的表达上调一致。
