5-羟基-6-溴-1H-吲哚-3-羧酸酯类衍生物的合成及其抗乙肝病毒活性  

The synthesis and their antiviral activities against hepatitis B virus of 5-hydroxy-6-bromo-1H-indole-3-carboxylates

作　　者：柴慧芳[1] 赵燕芳[2] 宫平[2] 

机构地区：[1]贵阳中医学院,贵州贵阳550002 [2]沈阳药科大学制药工程学院,辽宁沈阳110016

出　　处：《贵州化工》2008年第4期20-23,共4页Guizhou Chemical Industry

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,评价其抗乙肝病毒活性。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7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,4个目标化合物具有不同程度抑制乙肝病毒进行DNA复制的作用,其IC50值均小于阳性对照拉米夫定(IC50:228.0μg/mL)。Aim： To design and synthesize 5 - hydroxy- 6 - bromo - 1H - indole - 3 -carboxylates, and to evaluate their antiviral activities against hepatitis B virus. Methods： Structures of target compounds were cortfirmed by 1H - NMR and MS, and their antiviral activities against hepatitis B virus were determined by in vitro tests. Results and conclusions： 11 5 - hydroxy - 6 - bromo - 1H - indole - 3 - carboxylate compounds unreported in literatures were synthesized. Pilot activity tests showed that 4 target compounds had substantially inhibitory effects on DNA replication of hepatitis B virus, and their IC50 values were all less than that of positive drug lamivudine （IC50： 228.0μg/ml）.

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 抗乙肝病毒活性 

分 类 号：TQ463.3[化学工程—制药化工]