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为了进一步研究环烷基磺酰胺类化合物的杀菌活性与构效关系,在前期工作基础上,对先导化合物进一步展开研究,合成了15个未见文献报道的2-吡啶酰氨基环己烷基磺酰胺类化合物。首先以2-氧代环己烷基磺酰胺为原料,经过还原胺化后得到2-氨基环己烷基磺酰胺;再与取代吡啶甲酰氯反应,得到目标化合物。分别通过菌丝生长速率法与黄瓜活体叶片法测定了目标化合物对番茄灰霉病菌Botrytis cinerea及其他5种植物病原菌的杀菌活性。结果表明:目标化合物对番茄灰霉病菌表现出较好的抑制活性,其中化合物V-8在离体条件下对番茄灰霉病菌的EC_(50)值为1.41 mg/L,在500 mg/L下的活体防效为79.17%;此外,部分目标化合物在50 mg/L下,对水稻纹枯病菌、水稻稻瘟病菌、大豆根腐病菌、黄瓜绵腐病菌和辣椒疫霉的抑制率高于60%,其中,化合物V-7对黄瓜绵腐病菌的EC_(50)值为2.7 mg/L,其活性高于对照药剂多菌灵(EC_(50)值为4.4 mg/L),有进一步研究的价值。
In order to further study the bactericidal activity and the structure-activity relationship of the cycloalkylsulfonamides, further studies on the lead compounds were carried out based on the previous work, and 15 novel 2-picolinamidocyclohexanesulfones Amides. First 2-oxocyclohexyl sulfonamide as a raw material, after reductive amination to give 2-aminocyclohexyl sulfonamide; and then replaced with pyridine carbonyl chloride to give the target compound. The bactericidal activity of the target compound against Botrytis cinerea and five other plant pathogenic fungi were determined by mycelial growth rate and cucumber living leaf method respectively. The results showed that the target compounds showed good inhibitory activity against Botrytis cinerea, EC-50 value of compound V-8 was 1.41 mg / L against Botrytis cinerea in vitro. Under the conditions of 500 mg / L In addition, some of the target compounds at 50 mg / L, the inhibitory rate of Rhizoctonia solani, Magnaporthe grisea, Rhizoctonia solani, Toxoplasma gondii and Phytophthora capsici was high The EC 50 value of compound V-7 was 2.7 mg / L against M. gossypii and its activity was higher than that of the control drug carbendazim (EC 50 value 4.4 mg / L), with The value of further research.