乙基 6-溴-8-羟基咪唑并[1,2-a]吡啶-3-羧酸酯的合成及体外抗乙型肝炎病毒活性。
Synthesis and in-vitro anti-hepatitis B virus activity of ethyl 6-bromo-8-hydroxyimidazo[1,2-a]pyridine-3-carboxylates.
机构信息
Key Laboratory of Original New Drugs Design and Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, P.R. China.
出版信息
Arch Pharm (Weinheim). 2011 Mar;344(3):158-64. doi: 10.1002/ardp.201000045. Epub 2010 Dec 22.
A series of ethyl 6-bromo-8-hydroxyimidazo[1,2-a]pyridine-3-carboxylate derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in HepG2.2.15 cells. Nearly half of the tested compounds were proved to be highly effective in inhibiting the replication of HBV DNA with IC(50) values ranging from 1.3 to 9.1 µM. Among them, 10o and 10s were identified as the most promising compounds.
一系列的乙基 6-溴-8-羟基咪唑并[1,2-a]吡啶-3-羧酸酯衍生物被合成并在 HepG2.2.15 细胞中评估其抗乙型肝炎病毒 (HBV) 活性和细胞毒性。 测试的化合物中有近一半被证明具有高度抑制 HBV DNA 复制的活性，IC50 值范围为 1.3 到 9.1 μM。 其中，10o 和 10s 被鉴定为最有前途的化合物。
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