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Synthesis and antiviral activity of new acrylamide derivatives containing 1,2,3-thiadiazole as inhibitors of hepatitis B virus replication

  作者 Dong, WL; Liu, ZX; Liu, XH; Li, ZM; Zhao, WG  
  选自 期刊  European Journal of Medicinal Chemistry;  卷期  2010年45-5;  页码  1919-1926  
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[摘要]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 mu g/mL), 9c (3.59 mu g/mL) and 17a (9.00 mu g/mL) of the inhibition on the replication of HBV DNA were higher than that of the positive control lamivudine (14.8 mu g/mL). Compound 9d exhibited significant activity against secretion of HBeAg (IC50 = 12.26 mu g/mL). (C) 2010 Elsevier Masson SAS. All rights reserved.

 
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