6-溴-5-羟基吲哚-3-羧酸酯类衍生物的合成及其抗病毒活性

Syntheses and the in vitro antiviral activities of the derivatives of 6-bromo-5-hydroxyindole-3-carboxylic acid ethyl ester

目的设计合成 6 溴 5 羟基吲哚 3 羧酸酯类衍生物 ,并对其体外抗呼吸道病毒活性进行初步评价。方法以对苯醌、3 乙氨基 2 丁烯酸乙酯为起始原料 ,经多步反应合成目标化合物 ;并在MDCK和HeLa细胞内 ,采用细胞病变法 ,检测目标化合物对甲 3型流感病毒和呼吸道合胞病毒的抑制作用。结果与结论共制得 1 2个新化合物 ,经1H NMR、MS确证其结构。体外试验表明 ,目标化合物具有不同的抗病毒活性 ,其中Ⅵj 的体外抗病毒作用与阳性对照药金刚烷胺相当。

Aim To design and prepare some new derivatives of 6-bromo-5-hydroxyindole-3-carboxylic acid ethyl ester and to determine their antiviral activity in vitro . Method The target compounds were synthesized in several steps with the starting materials quinone and 3-ethylaminocrotonate,their antiviral activities in vitro against human influenza A3 and respiratory syncytial virus(RSV)were examined respectively in the MDCK cell culture and HeLa cell culture with virus cytopathic effect assay.Results and Conclusion The twelve derivatives of 6-bromo-5-hydroxyindole-3-carboxylic acid ethyl ester were synthesized whose structures were confirmed by 1H-NMR and MS.The pharmacological results show compoud Ⅵ_j has the same potent antiviral activity as the control drug amantadine.