N-(5-芳基-1,3,4-噁二唑-2-基)-N′-4-氟苯氧乙酰基硫脲的合成及抑菌活性

Synthesis and Fungicidal Activities of N-(5-Aryl-1,3,4-thiadiazol-2-yl)-N′-4-fluorobenzoxyacetylthioureas

摘要: 为了寻找更好的具有生物活性的化合物,从4-氟苯氧乙酸出发先合成酰基异硫氰酸酯,再与2-氨基-5-芳基-1,3,4-噁二唑反应合成了10个新的酰基硫脲类化合物,其结构经红外光谱、核磁共振氢谱、质谱和元素分析确认。采用平皿培养菌落生长速率法对6种病原菌进行了初步的生物活性测试,结果表明,在50mg/L浓度下,大部分化合物对黄瓜灰霉病菌Botrytis cinereapers、小麦赤霉病菌G ibberella zeae的抑制率达60%以上,其中Ⅱa、Ⅱc两个化合物对小麦赤霉病菌的抑制率达90%以上。

Abstract: In order to search compounds with better fungicidal activity,ten new N-(5-aryl-1,3,4-(thiadiazol)-2-yl)-N′-4-fluorobenzoxyacetylthioureas were synthesized from the start material of 4-fluorobenzoxyacetic acid.Their structures were confirmed by IR,MS,1H NMR and elemental analysis.The results of preliminary biological test showed that some of these compounds had good fungicidal activity. The inhibition rate of most compounds to Botrytis cinereapers and Gibberella zeae could reach 60% at the concentration of 50 mg/L.The inhibition rate of two compounds(Ⅱ_a and Ⅱ_c)to Gibberella zeae were 90%.