2-吡啶酰氨基环己烷基磺酰胺的合成与杀菌活性

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Botrytiscinerea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ECsn值为1．41mg／L，在500mg／L下的活体防效为79．17％；此外，部分目...

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Bibliographic Details
Published in农药学学报 Vol. 19; no. 2; pp. 169 - 175
Main Author 王闽龙 曲圣极 纪明山 祁之秋 李兴海
Format Journal Article
LanguageChinese
Published 2017
Subjects
2-氨基环己烷基磺酰胺
取代吡啶酰胺
杀菌活性
构效关系
灰霉病菌
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Summary: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Botrytiscinerea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ECsn值为1．41mg／L，在500mg／L下的活体防效为79．17％；此外，部分目标化合物在50mg／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EC50值为2．7mg／L，其活性高于对照药剂多菌灵（EC50值为4．4mg／L），有进一步研究的价值。
Bibliography:In order to explore the fungicidal activity and structure-activity relationship of cycloalkylsulfonamides, 15 2-pyridinecarboxamide cyclohexylsulfonamides were synthesized and their activities against Botrytis cinerea were tested by in vitro mycelial growth rate method and in vivo leaf method. The title compounds were designed and synthesized by the reaction between pyridine formyl chloride and 2-amino cyclohexylsulfonamides, which was obtained from the reduction amination reaction using 2-oxocyclohexenylsulfonamides as the starting materials. The bioassay exhibited that all the compounds possessed fungicidal activities against B. cinerea and other five phytopathogenic fungi. Notably, compound V-8 showed good activity with the ECs0 value of 1.41 mg/L in vitro and the control efficiency of 79.17% in vivo against B. cinerea. Moreover, some of these compounds exhibited the inhibition rate of more than 60% against Rhizoctonia solani K/ihn, Pyricularia grisea, Pythium aphanidermatum, Fusarium oxysporium and Phytop
ISSN:1008-7303