环丙基修饰的新型氯硝柳胺类衍生物的合成及抗肺纤维化活性  

Cyclopropyl Modified Novel Niclosamide Derivatives:Design,Synthesis and Anti-pulmonary Fibrosis Activities

作　　者：韩英蕾 谭醉 邹胜[1] 黄晴菲[1] 叶庭洪 王启卫[1] HAN Ying-lei;TAN Zui;ZOU Sheng;HUANG Qing-fei;YE Ting-hong;WANG Qi-wei(Chengdu Institute of Organic Chemistry,Chinese Academy of Sciences,Chengdu 610041,China;University of Chinese Academy of Sciences,Beijing 100049,China;Laboratory of Liver Surgery,West China Hospital,Sichuan University,Chengdu 610041,China)

机构地区：[1]中国科学院成都有机化学研究所,四川成都610041 [2]中国科学院大学,北京100049 [3]四川大学华西医院肝脏外科研究室,四川成都610041

出　　处：《合成化学》2020年第7期614-619,共6页Chinese Journal of Synthetic Chemistry

基　　金：四川省科学技术厅杰出青年基金资助项目(2019JDJQ0010);中科院“西部之光”人才培养计划。

摘　　要：以氯硝柳胺为先导化合物,2-位羟基为修饰位点,乙酰基为连接子,设计并合成6个新的氯硝柳胺类衍生物(8a^8f),其结构经1 H NMR和HR-MS(ESI)表征。采用噻唑蓝(MTT)法考察目标化合物对小鼠成纤维细胞(3T3细胞)的体外抗肺纤维化活性。活性测试结果表明:环丙基修饰的化合物8a表现出比氯硝柳胺更好的抑制效果,具有一定的抗肺纤维化活性。New niclosamide derivatives(8a^8f)were designed and synthesized at the modification site of 2-OH using acetyl group as the linker,which were characterized by 1 H NMR and HR-MS(ESI).Then,the activities of anti-pulmonary fibrosis was evaluated in 3T3 cells by MTT assay,which indicated that the cyclopropyl functional compound 8a was more active than niclosamide against 3T3 cells.

关 键 词：氯硝柳胺 环丙基 抗肺纤维化 活性 噻唑蓝法 合成 

分 类 号：O621.3[理学—有机化学] O626[理学—化学]