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一类新型大环内酯衍生物的合成及其生物活性研究

Study of Synthesis and Biological Activities of a Novel Macrolide Derivatives
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摘要 为了寻找高效、广谱的杀虫、杀菌剂,以去糖基或部分去糖基的多杀菌素为母体进行结构修饰,合成了8种大环内酯酰化衍生物,其结构经1H NMR,13C NMR和MS表征.对合成的化合物进行了生物活性测试.结果表明,这类化合物对鳞翅目、鞘翅目、双翅目、半翅目及线虫等害虫有较好的杀灭活性,其中化合物3e在100 mg/L浓度下对桃蚜的24 h杀灭率达到100%,化合物3f和3h在上药量为200μg时对假单胞菌有一定的抑制作用. Modification of molecular structure of pesticides is a common method to seek new efficient broad-spectrum insec-ticides. This study focused on modifying the structure of deglycosylated or partially deglycosylated spinosad. Eight new mac-rolide derivatives had been synthesized by acylation. Their structures were characterized by 1H NMR, 13C NMR and MS tech-niques. Their fungicidal and insecticidal activities were also evaluated. The results showed that all compounds synthesized had excellent insecticidal activities against lepidoptera, coleoptera, diptera, hemiptera and nematoda. Compound 3e at the concen-tration of 100 mg/L presented 100%insecticidal activity against hemiptera (e.g. Myzus persicae) and compounds 3f and 3h loading 200μg presented certain inhibition against pseudomonas.
出处 《有机化学》 SCIE CAS CSCD 北大核心 2014年第12期2543-2550,共8页 Chinese Journal of Organic Chemistry
基金 北京理工大学基础研究基金(No.20131042006)资助项目~~
关键词 大环内酯 酰化 杀虫活性 杀菌活性 macrolide acylate insecticidal activity fungicidal activity
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  • 1王登旭,王二兵,彭向前.泰利霉素的药理作用及临床应用[J].中国药物与临床,2005,5(7):524-525. 被引量:7
  • 2Farrell DJ, Sader HS, Castanheira M, et al. Antimicrobial characterisation of CEM-IO1 activity against respiratory tract pathogens, including muhidrug-resistant pneumocoecal serogroup 19A isolates [ J ]. In J Antimicrob Agents, 2010, 35(6~: 537-5d3_. 被引量:1
  • 3刘剑,杨明.泰利霉素研究进展[C]//四川省生理科学学会第八届学术交流会暨西部地区生理学学术研讨会.四川省生理科学学会第八届学术交流会暨西部地区生理学学术研讨会论文集.四川宜宾:[出版者不详],2007:87-89. 被引量:1
  • 4Rospide MF, Biedenbach D J, Jones RN. Comparative antimicrobial activity of ABT-773, a novel ketolide, tested against drug-resistant Gram-positive cocci and Haemophilus intIuenzae [ J ]. In J Antimicrob Agents, 2001, 17(6): 451- 455. 被引量:1
  • 5Johnson CN, Benjamin WH Jr, Gray BM, et al. In vitro activity of ABT-773, telithromyein and eight other antimierobials against erythromyein-resistant Streptococcus pneumoniae respiratory isolates of children [ J ]. In J Antimierob Agents, 2001, 18(6): 531-535. 被引量:1
  • 6Putnam SD, Sader HS, Farrell D J, et al. Antimicrobial eharaeterisation of solithromyein (CEM-101), a novel fluoroketolide: activity against staphylococci and enterocoeei [ J ]. In J Antimicrob Agents, 2011, 37(1): 39-45. 被引量:1
  • 7Putnam SD, Castanheira M, Moet GJ, et al. CEM-101, a novel fluoroketolide : Antimicrobial activity against a diverse collection of Gram-positive and Gram-negative bacteria [ J ].Diagn Microb Inlet Dis, 2010, 66(4): 393-401. 被引量:1
  • 8Farrell D J, Castanheira M, Sader HS, et al. The in vitro evaluation of solithromycin (CEM-101) against pathogens isolated in the United States and Europe (2009) [ J ]. J Infec, 2010, 61(6): 476-483. 被引量:1
  • 9Jiang LJ, Or YS. Pharmacokineyics of EDP-420 after muhiple oral doses in healthy aduh vohmteers and in a bioequivalenee study[J].Antimicrob Agents Chemother, 2009, 53(8): 3218-3225. 被引量:1
  • 10Linduska J. Foliar sprays to control ear-invading insects on sweet corn, 1997[J]. Arthrop Management Tests, 1998,23(1) :95-96. 被引量:1

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