摘要
目的设计合成一系列7-羟基喹啉-3-羧酸乙酯类化合物,并对其抗乙肝病毒活性进行初步评价。方法以香兰醛为起始原料,经7-9步反应合成目标化合物;测定目标化合物对HepG2.2.15细胞中乙肝病毒的抑制作用及其细胞毒性。结果与结论共合成12个新化合物,其结构经MS、IR和1H-NMR谱确证。体外活性测试表明,多数化合物显示出不同程度的乙肝病毒抑制活性,其中,化合物11a、12c的活性优于对照药拉米夫定。
Aim To design and synthesize a series of ethyl 7-hydroxyquinoline-3-carboxylate derivatives, and to evaluate their anti-HBV activities in vitro. Methods The target compounds were synthesized by 7 to 9 steps from vanillin. The abilities to inhibit replication of hepatitis B virus （HBV） and cytotoxicities of all compounds were evaluated in HepG2.2. I5 cells. Results and conclusion Twelve new compounds were synthesized and their structures were confirmed by MS, IR and ^1H-NMR. The results of the evaluation in vitro showed that most compounds exhibited HBV inhibitory activities. Among them, lla and 12c exhibited high activity than the positive control lamivudine.
出处
《中国药物化学杂志》
CAS
CSCD
2008年第5期329-334,共6页
Chinese Journal of Medicinal Chemistry
基金
国家自然科学基金项目(30672519)
