环保型抑菌剂5,6,7,8-四氢-1,2,4-三唑并[4,2-a]吡嗪的合成  

Synthesis of environmental protection bacteriostatic agent 5,6,7,8-tetrahydro-1,2,4-triazolo[4,3-a]pyrazine

作　　者：罗维 李保庆 蔡慧华 LUO Wei;LI Bao-qing;CAI Hui-hua(Guangdong Polytechnic of Environmental Protection Engineering,Foshan 528216,Guangdong,China)

机构地区：[1]广东环境保护工程职业学院,广东佛山528216

出　　处：《农药》2022年第4期250-253,共4页Agrochemicals

基　　金：中小学生态环境教育科普宣教。

摘　　要：[目的]为寻找具有较高生物活性的5,6,7,8-四氢-1,2,4-三唑并[4,3-a]吡嗪类环保抑菌剂。[方法]以吡啶-2-甲酸、2-哌嗪酮以及取代苯甲酸为初始原料,经5步反应,合成了3个5,6,7,8-四氢-1,2,4-三唑并[4,3-a]吡嗪化合物8a~8c,其结构经1H NMR、元素分析及高分辨质谱确证且进行抑菌活性测定。[结果]目标化合物8b的抑菌活性较好,对大肠杆菌(Escherichia coli)和枯草芽孢杆菌(Bacillus subtilis)的MIC值均低于对照药剂阿米卡星。[结论]目标化合物8b可作为先导化合物进一步设计合成抑菌剂。[Aims] This study aims to find environmental protection bacteriostatic agent of 5,6,7,8-tetrahydro-1,2,4-triazolo [4,3-a]pyrazine with higher active bioactivity. [Methods] Three 5,6,7,8-tetrahydro-1,2,4-triazolo [4,3-a]pyrazine compounds 8a-8c were synthesized through five steps of reactions based on 2-picolinic acid, piperazin-2-one and substituted benzoic acid. The structures were confirmed by1H NMR, elemental analysis and HRMS. The fungicidal activities of these compounds were also evaluated. [Results] The compound 8b had better bacteriostatic activity, and the MIC values for Escherichia coli and Bacillus subtilis were lower than that of Amikacin. [Conclusions] The compound8b might be considered as a promising lead compound for further design and synthesis of agricultural fungicides.

关 键 词：5 6 7 8-四氢-1 2 4-三唑并[4 3-a]吡嗪 合成 抑菌活性 环保 

分 类 号：TQ460.3[化学工程—制药化工]