应用化学2017，Vol.34Issue(7)：783-788,6.DOI:10.11944/j.issn.1000-0518.2017.07.160440
溴代甲氧基二苯甲酮咪唑类化合物的合成及对过氧化氢致EA.hy 926细胞损伤的保护作用
Synthesis of Bromo-Methoxyl Benzophenone Imidazole Compounds and Their Protective Activities Against Hydrogen Peroxide Induced Injury in EA.hy 926 Cells
摘要
Abstract
To introduce the imidazole ring to the bromo-methoxyl benzophenone structures and find the target compounds with high protective activity on vacular endothelium cells, eight novel bromo-methoxyl benzophenone imidazole compounds were synthesized using 5-bromo-2-methylbenzoic acid as starting material via following reactions:acylating chlorination, Friedel acylation, bromination, radical substitution with N-bromosuccinimide(NBS) and nucleophilic substitution with substituted imidazoles.The structures of the target compounds were confirmed by proton and carbon nuclear magnetic resonance spectroscopy(1H and 13C NMR) and high resolution mass spectrometry(HRMS).Additionally, the protective effects of the target compounds against H2O2-induced EA.hy 926 cells injury were evaluated by methylthiazolyldiphenyl-tetrazolium bromide(MTT) assay and their structure-activity relationships were also preliminarily discussed.The in vitro results show that target compounds 6a, 6g and 6h exhibit significant cytoprotective activities and their half maximal inhibitory concentration(EC50) values are 1.9, 4.0 and 3.2 μmol/L, respectively, superior to the positive control Quercetin(EC50≈18 μmol/L).These results also suggest the potential application prospect of target compounds in the treatment of cardiovascular diseases.关键词
溴代甲氧基二苯甲酮/咪唑/EA.hy926细胞/保护活性Key words
bromo-methoxyl benzophenone/imidazole/EA.hy 926 cells/protective activity分类
化学化工引用本文复制引用
宋婷,孔德朋,王勤金,冯秀娥,李青山..溴代甲氧基二苯甲酮咪唑类化合物的合成及对过氧化氢致EA.hy 926细胞损伤的保护作用[J].应用化学,2017,34(7):783-788,6.基金项目
国家高技术研究发展计划("863"计划)(2013AA092903) （"863"计划）
国家自然科学基金(81473100) （81473100）
2014年度山西省煤基重点科技攻关项目(MJH2014-14) （MJH2014-14）
山西医科大学博士启动基金资助项目(B03201213) （B03201213）
Supported by the National High Technology Research and Development Plan("863" plan)(No.2013AA092903), the National Natural Science Foundation of China(No.81473100, Shanxi Province Coal-based Key Scientific and Technological Projects in 2014(No.MJH2014-14), Ph.D.Funded Start-up Funding of Shanxi Medical University(No.B03201213) （"863" plan）
