| 吴文能,费强.化学通报,2019,82(12):1115-1120. |
| 新型1,2,4-三唑硫醚取代乙酰胺类化合物的合成及抗菌活性 |
| Synthesis and Fungicidal Activity of 1, 2, 4-triazole Thioether Derivates Containing Acetamide Moiety |
| 投稿时间：2019-07-17 修订日期：2019-07-19 |
| DOI： |
| 中文关键词: 1, 2, 4-三唑 乙酰胺 合成 抑菌活性 |
| 英文关键词:1, 2, 4-triazole amides synthesis fungicidal activity |
| 基金项目:贵州省自然科学基金项目(黔科合基础[2016]1006)、中国博士后基金(2017M623070)、国家自然科学基金项目(21462010)、贵州中烟工业有限公司科技项目(GZZY/KJ/JS/2017CY011-1)、贵阳市科技局贵阳学院专项(GYU-KYZ[2018]01-01)资助 |
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| 中文摘要: |
| 以3, 4, 5-三甲氧苯甲酸为原料，将具有优良生物活性的1,2,4-三唑与酰胺结构有机结合，通过酯化、肼解、环化、醚化、水解、缩合等反应合成1, 2, 4-三唑硫醚乙酰胺类化合物6a-6m，其结构经1H NMR，13C NMR，MS和元素分析进行了结构确证。初步生物活性测试表明：化合物浓度在50 μg/mL时，化合物6a-6m对猕猴桃软腐病中的葡萄座腔菌、拟茎点霉菌（Phomopsis sp.）和灰霉菌（B. cinerea）表现一定的抑制活性，其中化合物6k和6l对葡萄座腔菌、拟茎点霉菌和灰霉菌的抑制活性在83.4%至91.3 %；化合物6k对葡萄座腔菌和拟茎点霉菌的EC50值为46.6 μg/mL和30.8 μg/mL，均优于对照药剂嘧霉胺(57.6 μg/mL 和 32.1 μg/mL)。以上生物活性表明，1, 2, 4-三唑硫醚乙酰胺类化合物具有较好的抑菌活性，为进一步开发高活性化合物奠定一定基础。 |
| 英文摘要: |
| 1,2,4-triazole thioether acetamide derivativeS 6a-6m were synthesized from 3,4,5-trimethoxybenzoic acid through esterification, hydrazinolysis, cyclization, etherification, hydrolysis and condensation, and their structures were confirmed by 1H NMR, 13C NMR, EMI-MS and elemental analysis. Preliminary bioactivity results indicated that compounds 6a-6m exhibited a certain inhibitory on B. dothidea, Phomopsis sp. and B. cinerea in kiwi soft rot at the concentration of 50 μg/mL. The Inhibition rate of compounds 6k and 6l against B. dothidea, Phomopsis sp. and B. cinerea were 83.4% to 91.3%. Meanwhile, the EC50 value of compound 6k against B. dothidea and Phomopsis sp. were 46.6 μg/mL and 30.8 μg/mL, respectively, superior that of the commercial agent pyrimethanil (57.6 μg/mL and 32.1 μg/mL). The biological activities indicate that 1,2,4-triazole thioether acetamides have good fungicidal activity and lays a foundation for further development of highly active compounds. |
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