新型N-芳基-2-((5-((4,6-二甲基嘧啶-2-基)硫甲基)-1,3,4-噻二唑-2-基)硫)乙酰胺类化合物的合成及杀菌活性

为寻找新型杂环活性化合物，通过活性亚结构拼接，以硫脲和乙酰丙酮为起始原料合成4，6-二甲基嘧啶-2-硫醇，随后经酯化、肼化、环化和缩合反应，设计并采用微波辅助合成了10个新型N-芳基-2-（（5-（（4，6-二甲基嘧啶-2-基）硫甲基）-1，3，4-噻二唑-2-基）硫）乙酰胺类化合物，其结构通过核磁共振氢谱和碳谱、红外光谱、质谱及元素分析确认。初步生物活性测试结果表明，在50 mg/L下，大部分目标化合物对植物病原真菌具有一定的抑制活性，其中化合物8h对黄瓜炭疽病菌Colletotrichum orbiculare的抑制率达77.3%。

Synthesis and fungicidal activity of novel N-aryl-2-((5-((4,6-dimethylpyrimidin-2-yl)thiomethyl)-1,3,4-thiadiazole-2-yl)thio)-acetamide compounds

In order to discover novel heterocyclic compounds with biological activities, ten novel N-aryl-2-((5-((4,6-dimethylpyrimidin-2-yl)thiomethyl)-1,3,4-thiadiazole-2-yl)thio) acetamide compounds were synthesized under microwave assisted condition via cyclization, esterification, hydrazination, cyclization and the condensation reactions. The structures of the title compounds were characterized by ¹H NMR, ¹³C NMR, IR, ESI-MS and elemental analysis. The preliminary bioassay results indicated that most of them showed inhibition activity against Colletotrichum orbiculare, Botrytis cinerea and Rhizoctonia solani at the concentration of 50 mg/L. The inhibition rate of compound 8h against C. orbiculare reached 77.3%.