期刊文献+

新型2-取代苯甲酰基-5-烷基环戊酮的设计、合成与生物活性研究 被引量:1

Design, Synthesis and Bioactivity of Novel 2-Aroyl-5-alkylcyclopentanone Derivatives
原文传递
导出
摘要 为了发现具有良好生物活性的新型先导化合物,在综合多种高活性化合物结构特点的基础上,设计合成了一系列含苯甲酰基乙烯醇结构的2-取代苯甲酰基-5-烷基-环戊酮类化合物.以己二酸二乙酯为原料,经6步反应制得目标产物,其结构经IR,1H NMR,X射线及元素分析或高分辨质谱确证,并对该类化合物合成方法进行了探讨.初步生测结果表明,部分化合物对油菜表现出明显的抑制活性,在100μg/mL浓度下对油菜的抑制率达到60%以上. To find new lead compounds with muti-bioactivities, a series of novel 2-aroyl-5-alkylcyclopentanone derivatives containing 2-bezoylenthenol were designed on the base of various commercial products. The target compounds were synthe- sized from diethyl adipate in 6 steps. Their structures were confirmed by IR, 1H NMR spectra, X-ray and elemental analysis or HRMS. The preliminary bioassay results indicated that some compounds showed obvious inhibition effects against Brassica campestris, and the herbicidal activities were more than 60% at 100 μg/mL.
出处 《有机化学》 SCIE CAS CSCD 北大核心 2013年第1期143-147,共5页 Chinese Journal of Organic Chemistry
基金 国家973计划(No.2010CB126103) 国家自然科学基金(Nos.20772066 21072108) "十二五"科技支撑计划(No.2011BAE06B05-3)资助项目~~
关键词 对羟基苯基丙酮酸双氧化酶 芳酰基乙烯醇 环戊酮 除草活性 4-hydroxyphenylpyruvate dioxygenase 2-bezoylenthenol cyclopropanone herbicidal activity
  • 相关文献

参考文献7

二级参考文献58

共引文献43

同被引文献17

  • 1宋宝安,刘新华,杨松,胡德禹,金林红,张玉涛.肟类衍生物的合成与农药生物活性的研究进展[J].有机化学,2005,25(5):507-525. 被引量:50
  • 2Boumendjel A.Aurones:A subclass of flavones with promising biological potential[J].Curr Med Chem,2003,10(23):2621-2630.
  • 3Haudecoeur R,Boumendjel A.Recent advances in the medicinal chemistry of aurones[J].Curr Med Chem,2012,19(18):2861-2875.
  • 4Okombi S,Rival D,Bonnet B,et al.Discovery of benzylidenebenzofuran-3 (2H)-one(aurones) as inhibitors of tyrosinase derived from human melanocytes[J].J Med Chem,2006,49(1):329-333.
  • 5Sim H M,Loh K Y,Yeo W K,et al.Aurones as modulators of ABCG2 and ABCB1:Synthesis and structureactivity relationships[J].Chem Med Chem,2011,6(4):713-724.
  • 6Cheng H M,Zhang L W,Liu Y X,et al.Design,synthesis and discovery of 5-hydroxyaurone derivatives as growth inhibitors against HUVEC and some cancer cell lines[J].Eur J Med Chem,2010,45 (12):5950-5957.
  • 7Anastasia D,Maya M,Christos A K,et al.Natural and synthetic 2'-hydroxy-chalcones and aurones:Synthesis,characterization and evaluation of the antioxidant and soybean lipoxygenase inhibitory activity[J].Bioorg Med Chem,2009,17 (23):8073-8085.
  • 8Venkateswarlu S,Panchagnula G K,Subbaraju G V.Synthesis and antioxidative activity of 3',4',6,7-tetrahydroxyaurone,a metabolite of Bidens frondosa[J].Biosci Biotechnol Biochem,2004,68 (10):2183-2185.
  • 9Harvey A L.Natural products in drug discovery[J].Drug Discov Today,2008,13(19):894-901.
  • 10Morimoto M,Fukumoto H,Nozoe T,et al.Synthesis and insect antifeedant activity of aurones against Spodoptera litura larvae[J].J Agiic Food Chem,2007,55(3):700-705.

引证文献1

相关作者

内容加载中请稍等...

相关机构

内容加载中请稍等...

相关主题

内容加载中请稍等...

浏览历史

内容加载中请稍等...
;
使用帮助 返回顶部