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Synthesis, Antibacterial Activity, and Mechanisms of Novel 6-Sulfonyl-1,2,4-triazolo[3,4-b][1,3,4]thiadiazole Derivatives
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2021-04-19 , DOI: 10.1021/acs.jafc.1c01204 Sikai Wu 1 , Jing Shi 1 , Jixiang Chen 1 , Deyu Hu 1 , Liansheng Zang 1 , Baoan Song 1
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2021-04-19 , DOI: 10.1021/acs.jafc.1c01204 Sikai Wu 1 , Jing Shi 1 , Jixiang Chen 1 , Deyu Hu 1 , Liansheng Zang 1 , Baoan Song 1
Affiliation
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A series of novel 6-sulfonyl-1,2,4-triazolo[3,4-b][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 EC50 values of the compounds. The models were used to design and synthesize compounds 32 and 33 with higher activities. The EC50 values of compound 33 against Xanthomonas oryzae pv. oryzae (Xoo) and Xanthomonas oryzae pv. oryzicola (Xoc) 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 33 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 33 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.
中文翻译：
新型6-磺酰基-1,2,4-三唑[3,4- b ] [1,3,4]噻二唑衍生物的合成，抗菌活性及机理
设计并合成了一系列新颖的6-磺酰基-1,2,4-三唑并[3,4- b ] [1,3,4]噻二唑衍生物。建立了CoMFA模型，以根据化合物的EC 50值分析定量的构效关系。该模型用于设计和合成具有较高活性的化合物32和33。化合物33对米黄单胞菌PV的EC 50值。米（Xoo）和黄单胞菌（Xanthomonas oryzae）。空心稗（XOC）分别为0.59和1.63 mg / L，分别高于硫代二唑铜（90.43和97.93 mg / L）和比美噻唑（68.37和75.59 mg / L）。此外，化合物33对细菌叶斑纹（BLS）和细菌叶枯病（BLB）的防护活性分别为49.65％和49.42％，优于硫代二唑铜（44.28％和41.51％）和比美噻唑（38.89％）。和40.09％）。化合物33对BLS的保护活性与防御相关酶活性，叶绿素含量和光合作用活化的提高密切相关。这与防御反应和光合作用相关蛋白的表达上调相一致。
更新日期：2021-04-29
中文翻译：
新型6-磺酰基-1,2,4-三唑[3,4- b ] [1,3,4]噻二唑衍生物的合成，抗菌活性及机理
设计并合成了一系列新颖的6-磺酰基-1,2,4-三唑并[3,4- b ] [1,3,4]噻二唑衍生物。建立了CoMFA模型，以根据化合物的EC 50值分析定量的构效关系。该模型用于设计和合成具有较高活性的化合物32和33。化合物33对米黄单胞菌PV的EC 50值。米（Xoo）和黄单胞菌（Xanthomonas oryzae）。空心稗（XOC）分别为0.59和1.63 mg / L，分别高于硫代二唑铜（90.43和97.93 mg / L）和比美噻唑（68.37和75.59 mg / L）。此外，化合物33对细菌叶斑纹（BLS）和细菌叶枯病（BLB）的防护活性分别为49.65％和49.42％，优于硫代二唑铜（44.28％和41.51％）和比美噻唑（38.89％）。和40.09％）。化合物33对BLS的保护活性与防御相关酶活性，叶绿素含量和光合作用活化的提高密切相关。这与防御反应和光合作用相关蛋白的表达上调相一致。
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