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2-苄硫基烟酰胺类衍生物的合成及生物活性

Synthesis and Bioactivity of 2-Benzylsulfanyl Nicotinamide Derivatives

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【作者】 朱宇春袁莉萍曹瑾沈晓霞吕冬华倪长春沈宙陈亮张一宾

【Author】 ZHU Yu-chun2,YUAN Li-ping1,CAO Jin1,SHEN Xiao-xia,LV Dong-huaNI Chang-chun1,SHEN Zhou1,CHEN Liang1,ZHANG Yi-bin1(1.Shanghai Pesticide Research Institute,Shanghai 200032,China;2.East China Universityof Science and Technology,Pharmaceutical Institute,Shanghai 200237,China)

【机构】 华东理工大学药学院上海市农药研究所

【摘要】 以2-苄硫基烟酸为原料,设计并合成了26个2-苄硫基烟酰胺类化合物,其化学结构经核磁共振氢谱和元素分析确证。初步的生物活性测定结果表明,该类化合物具有一定的杀虫及除草活性。其中C-9、C-10、C-11在50mg/L时对淡色库蚊Culex pipiens pallens的致死率达到100%;C-3、C-6、C-15在100mg/L对稗草Echinochloa crusgalliLink、马唐Digitaria sanguinalis、苋菜Ambrosia tricolorLinn的白化度大于80%。

【Abstract】 In search for novel pesticides with high effects,high selectivity and low toxicity,26 compounds belong to 2-benzylsulfanyl nicotinamide derivatives were designed and synthesized starting from 2-benzylsulfanyl nicotinic acid.Their chemical structures were confirmed by 1H NMR and elemental analysis.Preliminary bioassays showed that some compounds exhibited certain insecticidal and herbicidal activities.The mortality of Culex pipiens pallens from C-9,C-10 and C-11 at the concentration of 50 mg/L reached 100%.The albino rate of C-3,C-6,C-15 to Echinochloa crusgalli,Digitaria sanguinalis,Ambrosia tricolor and Brassica alboglabra at the concentration of 100 mg/L was above 80%.

【关键词】 烟酰胺衍生物合成生物活性
【Key words】 nicotinamidederivativesynthesisbioactivity
【基金】 国家重点基础研究发展规划(“973”计划)资助项目(2003CB114401)
  • 【文献出处】 农药学学报 ,Chinese Journal of Pesticide Science , 编辑部邮箱 ,2008年03期
  • 【分类号】O621.25
  • 【被引频次】3
  • 【下载频次】214
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