新型6-羟基喹啉-3-羧酸乙酯的体外合成及抗乙型肝炎病毒活性评价
Synthesis and anti-hepatitis B virus evaluation of novel ethyl 6-hydroxyquinoline-3-carboxylates in vitro.
作者信息
Liu Yajing, Zhao Yanfang, Zhai Xin, Feng Xusheng, Wang Jinxin, Gong Ping
机构信息
Key Lab of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe District, Shenyang 110016, Liaoning, PR China.
出版信息
Bioorg Med Chem. 2008 Jul 1;16(13):6522-7. doi: 10.1016/j.bmc.2008.05.029. Epub 2008 May 17.
A series of non-nucleoside ethyl 6-hydroxyquinoline-3-carboxylate derivatives were prepared and evaluated in HepG2.2.15 cells. Most compounds inhibited the expression of viral antigens HBsAg or HBeAg at low concentration. Six compounds, 9f(3), 12b(6), 12f(6), 13b(2), 13b(6), and 13f(6), displayed excellent intracellular inhibitory activity and selectivity towards the replication of HBV DNA. Of these six initial hits, compound 13b(6) was the most active.
制备了一系列非核苷类6-羟基喹啉-3-羧酸乙酯衍生物，并在HepG2.2.15细胞中进行了评估。大多数化合物在低浓度下抑制病毒抗原HBsAg或HBeAg的表达。六种化合物，即9f(3)、12b(6)、12f(6)、13b(2)、13b(6)和13f(6)，对HBV DNA复制表现出优异的细胞内抑制活性和选择性。在这六个初始活性化合物中，化合物13b(6)活性最强。
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