摘要/Abstract

在吡唑环的3位引入叔醇结构，设计合成了一系列新颖的吡唑-4-甲酰胺类化合物，其结构经¹H NMR，¹³C NMR，HR-ESI-MS和X射线衍射表征确证.生物活性测试结果显示，部分化合物在100μg/mL时对瓜果腐霉菌和辣椒疫霉菌等测试植物病原菌显示了一定的杀菌活性，如N-（2-氟苯基）-3-（1-羟基环己基）-1，5-二甲基-1H-吡唑-4-甲酰胺（B₁）和N-（噻唑-2-基）-3-（1-羟基环己基）-1，5-二甲基-1H-吡唑-4-甲酰胺（B₁₀）对瓜果腐霉菌的EC₅₀分别为76.3和71.9μg/mL，化合物B₁₀对辣椒疫霉菌的EC₅₀分别为85.4μg/mL.
关键词: 吡唑-4-甲酰胺, 叔醇, 合成, 杀菌活性
A series of novel pyrazole-4-carboxamide compounds were designed and synthesized through introducing a tertiary alcohol moiety into the C-3 position of the pyrazole ring based on the chracteristics of pyrazole-4-carboxamide fungicides and natural products with a tertiary alcohol moiety. Their structures were characterized by ¹H NMR, ¹³C NMR, HR-ESI-MS data and X-ray diffraction. The preliminary bioassay results indicated that some of these compounds exhibit certain fungicidal activities against tested phytopathogens at the concentration of 100 µg/mL. N-(2-Fluorophenyl)-3-(1-hydroxycyclohexyl)-1,5-dimethyl-1H-pyrazole-4-carboxamide (B₁) and N-(thiazol-2-yl)-3-(1-hydroxycyclohexyl)-1,5-dimethyl-1H-pyrazole-4-carbo-xamide (B₁₀) have EC₅₀ values of 76.3 and 71.9 µg/mL against Pythium aphanidermatum. B₁₀ has an EC₅₀ value of 85.4 µg/mL against Phytophthora capsici, respectively.
Key words: pyrazole-4-carboxamide, tertiary alcohol moiety, synthesis, fungicidal activity


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