[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.