含葡萄糖取代基均三唑并[3,4-b]-1,3,4-噻二唑稠杂环化合物的合成及生物活性研究

Synthesis and Biological Activity of Glucopyranosyl Substituted Thiazolo-s-Triazoles

以2,3,4,6-四-O-乙酰基-β-D-吡喃葡萄糖基异硫氰酸酯为原料,与3-烷基/芳基-4-氨基-5-巯基-1,2,4-均三唑2a～2h反应制得了8个未见报道的3-烷基/芳基-6-(2′,3′,4′,6′-四-O-乙酰基-β-D-吡喃葡萄糖基)氨基均三唑并[3,4-b]-1,3,4-噻二唑化合物3a～3h,并经IR,1HNMR进行了结构表征.初步生物活性测试结果表明,目标化合物对黄瓜赤霉、棉花立枯、玉米大斑、苹果黑斑、花生褐斑和小麦赤霉6种植物原菌繁殖均有不同程度的抑制,化合物3g在50μg·L-1质量浓度时对小麦赤霉的防效达85%.

Eight novel glucopyranosyl substituted compounds: 3alkyl/aryl6(2′,3′,,4′,6′tetraOacetylβDglucopyranosyl)aminostrizolo1,3,4thiadiazoles were synthsized and identified by elemental analysis, IR and 1H NMR. Preliminary bioassay indicates that these compounds displayed varied fungicidal activities. The compound 3g showed a retardation of 85% against gibberellin at 50 μg·L-1 concentration.