中文摘要：

目的设计、合成一系列含（3-芳杂基）喹啉结构的衍生物，并测定其体外抗乙肝病毒活性。方法以3-羟基-4-甲氧基苯甲醛为起始原料，经苄基保护、硝化、还原、环化、肼解反应得到关键中间体6-（苄氧基）-7-甲氧基-2-（（苯基硫代）甲基）喹啉-3-甲酰肼。该中间体经缩合（或酰化）、环合、脱保护、Mannich、氧化反应得到目标化合物。采用ELISA法和实时荧光定量PCR法测试了目标化合物的体外抗乙肝病毒活性。结果与结论合成的15个化合物均未见文献报道，其结构经MS、^1H—NMR、^13C-NMR确证；活性测试结果表明，多个目标化合物具有一定的体外抗乙肝病毒活性。

英文摘要：

Hepatitis B virus（HBV） is one of the most serious and prevalent health problems. Based on our previous work, a series of novel 3-heterocyclic quinoline derivatives were designed and synthesized and their anti-HBV activities were evaluated in the HepG 2.2.15 cell line. Using 3-hydroxy-4-methoxy benzaldehyde as the starting material, the key intermediate 6- （ benzyloxy ） -7-methoxy-2- （ （ phenylthio ） methyl ） quinoline- 3-carbohydrazide was synthesized via benzyl protecting reaction, nitrification, reduction, cyclization and hydrazinolysis. The target compounds were synthesized via condensation, cyclization, deprotection, Mannich reaction, and oxidation. The structures of the target compounds were confirmed by MS, ^1H-NMR and ^13C-NMR. Preliminary pharmacologic studies showed that two compounds （ 12g, 13j ） displayed excellent potency and selectivity towards HBV with IC50 values less than 5 μmol·L^-1.