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2-吡啶酰氨基环己烷基磺酰胺的合成与杀菌活性
  • ISSN号:1008-7303
  • 期刊名称:《农药学学报》
  • 时间:0
  • 分类:O626.3[理学—有机化学;理学—化学] S482.2[农业科学—农药学;农业科学—植物保护]
  • 作者机构:沈阳农业大学植物保护学院,沈阳110866
  • 相关基金:辽宁省自然科学基金(2015020766);辽宁省教育厅科学研究项目(LJNYB201611);国家自然科学基金(31101466).
中文摘要:

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。

英文摘要:

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 Phytophthora capsiei. Compound V-7, with the EC50 value of 2.7 mg/L, showed better activity than carbendazim (with the ECs0 value of 4.4 mg/L) against Pythium aphanidermatum. These promising compounds had great potentials for further research.

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期刊信息
  • 《农药学学报》
  • 北大核心期刊(2011版)
  • 主管单位:国家教育部
  • 主办单位:中国农业大学
  • 主编:王道全
  • 地址:北京市海淀区圆明园西路2号中国农业大学理学院
  • 邮编:100193
  • 邮箱:nyxuebao@263.net
  • 电话:010-62733003
  • 国际标准刊号:ISSN:1008-7303
  • 国内统一刊号:ISSN:11-3995/S
  • 邮发代号:2-949
  • 获奖情况:
  • 国内外数据库收录:
  • 俄罗斯文摘杂志,美国化学文摘(网络版),波兰哥白尼索引,美国剑桥科学文摘,英国动物学记录,中国中国科技核心期刊,中国北大核心期刊(2008版),中国北大核心期刊(2011版),中国北大核心期刊(2014版)
  • 被引量:8245