新型含 1,2,3-噻二唑的丙烯酰胺衍生物的合成及其作为乙型肝炎病毒复制抑制剂的抗病毒活性。
Synthesis and antiviral activity of new acrylamide derivatives containing 1,2,3-thiadiazole as inhibitors of hepatitis B virus replication.
机构信息
State Key Laboratory of Elemento-Organic Chemistry, National Pesticide Engineering Research Center (Tianjin), Nankai University, Tianjin 300071, China.
出版信息
Eur J Med Chem. 2010 May;45(5):1919-26. doi: 10.1016/j.ejmech.2010.01.032. Epub 2010 Jan 25.
A series of new acrylamide derivatives containing 1,2,3-thiadiazole were synthesized, characterized, and evaluated for their anti-hepatitis B virus (HBV) activities in vitro. The IC50 of compounds 9b (10.4 microg/mL), 9c (3.59 microg/mL) and 17a (9.00 microg/mL) of the inhibition on the replication of HBV DNA were higher than that of the positive control lamivudine (14.8 microg/mL). Compound 9d exhibited significant activity against secretion of HBeAg (IC50=12.26 microg/mL).
合成了一系列含 1,2,3-噻二唑的新型丙烯酰胺衍生物，对其进行了表征，并在体外评估了它们抗乙型肝炎病毒（HBV）的活性。化合物 9b（10.4μg/mL）、9c（3.59μg/mL）和 17a（9.00μg/mL）对 HBV DNA 复制的抑制作用的 IC50 均高于阳性对照拉米夫定（14.8μg/mL）。化合物 9d 对 HBeAg 的分泌表现出显著的活性（IC50=12.26μg/mL）。
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