| 张圆琳,冯秀娥,高洁,李青山.化学通报,2014,77(5):452-456. |
| 新型卤代甲氧基二苯甲酮类化合物的合成及其对H2O2致人脐静脉内皮损伤的保护研究 |
| Synthesis of halogenated methoxy benzophenone derivatives and their cytoprotective activities against H2O2-induced injury in HUVECs |
| 投稿时间：2014-01-12 修订日期：2014-01-24 |
| DOI： |
| 中文关键词: 卤代甲氧基二苯甲酮 合成 人脐静脉内皮细胞 保护活性 |
| 英文关键词:halogenated methoxy benzophenone synthesis HUVECs cytoprotective activity |
| 基金项目:国家高技术研究发展计划（863计划） |
|
| 摘要点击次数: 3391 |
| 全文下载次数: 8 |
| 中文摘要: |
| 以甲氧基和卤素取代的苯甲酸为起始原料,经过羧酸酰基化、傅克酰基化、芳香环卤代等反应合成了系列新型卤代甲氧基二苯甲酮类化合物,通过考察其对H2O2诱导的人脐静脉内皮细胞(HUVECs)损伤的保护活性,完善了此类化合物的构效关系。共合成了12个目标化合物,其中8个为未见文献报道的新化合物,其结构经ESI-MS、1H-NMR、13C-NMR进行了表征和确认。体外活性实验表明,浓度为12.5μM时,化合物7a和9a对HUVECs有一定的保护活性,保护率超过50%。 |
| 英文摘要: |
| A series of novel halogenated methoxy benzophenone derivatives were designed and synthesized starting from methoxy and halogen substituted benzoic acids, followed by acylation of carboxylic acid, Friedel-Crafts acylation andShalogenation reaction. Their protective activities against H2O2-induced injury in human umbilical vein endothelial cell (HUVECs) were investigated to perfect the structure-activity relationships．Twelve target compounds were prepared including 8 new derivatives, and their structures were confirmed by ESI-MS, 1H-NMR and 13C-NMR. The results showed that the new compounds 7a and 9a exhibited high cytoprotective activities at 12.5μM, the protective rates were above 50 %. |
| 查看全文 查看/发表评论 下载PDF阅读器 |
| 关闭 |
|
|
|