5-羟基-1 H-吲哚-3-羧酸乙酯类化合物的合成及其抗流感病毒活性  

Synthesis and anti-influenza virus activity of ethyl 6-bromo-5-hydroxy-1 H-indole-3-carboxylate derivatives

作　　者：赵燕芳[1] 洪伟[1] 柴慧芳[1] 董金华[1] 宫平[1] 

机构地区：[1]沈阳药科大学制药工程学院,辽宁沈阳110016

出　　处：《中国药物化学杂志》2004年第4期219-224,共6页Chinese Journal of Medicinal Chemistry

基　　金：国家自然科学基金资助项目 (2 0 372 0 4 7)

摘　　要：目的设计合成 5 羟基 1H 吲哚 3 羧酸乙酯类化合物 ,评价其抗流感病毒和抗呼吸道合胞病毒活性。方法经IR、1H NMR和MS确证目标物结构 ,并经体外抗病毒试验进行活性筛选。结果与结论合成了 9个 5 羟基 1H 吲哚 3 羧酸乙酯类化合物 ,初步活性试验表明 ,具有一定的抑制流感病毒和呼吸道合胞病毒作用 ,其中 ,化合物Ⅷ1、Ⅷ2 、Ⅷ5的抗病毒活性与利巴韦林和阿比朵尔相当。Aim To design and synthesize a series of new ethyl 6-bromo-5-hydroxy-1 H -indole-3-carboxylate derivatives and evaluate their anti-influenza virus activity in vitro .Method Nine new compounds were synthesized and their structures were confirmed by IR, 1H-NMR and MS.They were tested for their anti-influenza virus activity in vitro in the cell culture experiments.The viruses were human influenza A3 in MDCK cells and respiratory syncytial virus in HeLa cells respectively.Results and Conclusion All the target compounds showed definite antiviral activity.Some of them,such as compounds Ⅷ 1,Ⅷ 2,Ⅷ 5 were comparable with ribavirin and arbidol.

关 键 词：药物化学 制备 化学合成 5-羟基-1H-吲哚-3-羧酸乙酯类化合物 抗流感病毒活性 

分 类 号：R914.5[医药卫生—药物化学]