三唑并噻二唑衍生物的合成及抑菌活性

为了寻找高活性农药先导化合物，考虑到三唑并噻二唑衍生物具有广泛的生物活性，本文利用活性亚结构拼接原理，将活性基团分别引入1,2,4-均三唑并3,4-b]-1,3,4-噻二唑杂环的3位和6位，合成了未见文献报道的3,6-二取代均三唑并3,4-b]-1,3,4-噻二唑类化合物11个，并用IR、¹HNMR及元素分析测试技术对其进行了结构表征。抑菌活性生物测定结果表明，合成的大部分化合物对黄瓜灰霉病菌(Botrytis cinerea)均有较好的生长抑制作用，其中，化合物5ae、5ag和5bd的抑制率达到70%；化合物5ad、5cd、5ce的抑制率大于60%；5bd对水稻纹枯病菌(Pellicularia sasakii)抑制率大于60%，化合物5cg对西瓜炭疽病菌(Colletotrichum lagenarium)的抑制率为69%。

Synthesis and Fungicidal Activity of Triazolothiadiazole Derivatives

In order to find active pesticide leading compounds, thinking about that triazolothiadiazoles had various biological activities, this paper designed and synthesized 11 novel title compounds from 3-substituted-4-amino-5-mercapto-1,2,4-triazoles with heterocyclic carboxylic acid via cyclization in the presence of phosphoryl chloride by the princple of combination of active strucural moieties. The structures of the title compounds were characterized by melting point, IR, 1HNMR and elemental analysis. The results of bioassay experiments with 10 commonly used fungi showed that, all the title compounds had satisfactory fungicidal activity against Botrytis cinerea, the growth inhibition rate of compounds 5ae, 5ag, 5bd against Botrytis cinerea were up to 70% and for 5ad, 5cd, 5ce were more than 60%; compound 5bd exhibited fungicidal activity against Pellicularia sasakii with growth inhibition up to 60%, the growth inhibition rate of compound 5cg against Colletotrichum lagenarium was 69%.