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-triazoleamidessynthesisfungicidal 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

作者	单位	E-mail
吴文能	贵阳学院	wuwenneng123@126.com
费强	贵阳学院	fqorganic@163.com

摘要点击次数:1193 全文下载次数:0 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. 查看全文查看/发表评论下载PDF阅读器 相关附件：版权转让声明书 -->