5-羟基-6-溴-1H-吲哚-3-羧酸酯类衍生物的合成及其体外抗病毒活性  

Synthesis and in vitro antiviral activities of ethyl 6-bromo-5-hydroxy-1H-indole-3-carboxylates

作　　者：柴慧芳[1] 张珂良[1] 张维娜[1] 张思思[1] 许竞雄[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》2006年第5期264-269,共6页Chinese Journal of Medicinal Chemistry

基　　金：国家自然科学基金项目(20372047)

摘　　要：目的设计合成5-羟基-6-溴-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1H-NMR和MS确证目标化合物结构,并经体外抗病毒试验测定其抗病毒活性。结果与结论合成了11个未见文献报道的5-羟基-6-溴-1H-吲哚-3-羧酸乙酯类化合物。初步活性试验表明,11个目标化合物均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Ⅹ9的体外抗病毒作用与阳性对照药物金刚烷胺相当。Aim To design and synthesize a series of new ethyl 6-bromo-5-hydroxy-lH-indole-3-carboxylate derivatives, and to evaluate their antiviral activities in vitro. Methods Eleven new compounds were synthesized and their structures were confirmed by 1H-NMR and MS. Their in vitro anti-influenza A3 virus and anti-RSV activities were tested. Results and conclusion The target compounds all exhibited antiviral activities. Among them, the antiviral activity of compound X 9 was comparable to that of admantadine.

关 键 词：药物化学 化合物制备 化学合成 5-羟基-6-溴-1H-吲哚-3-羧酸酯 抗病毒活性 

分 类 号：R914.5[医药卫生—药物化学]