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

Abstract 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 IC 50 of compounds 9b (10.4 μg/mL), 9c (3.59 μg/mL) and 17a (9.00 μg/mL) of the inhibition on the replication of HBV DNA were higher than that of the positive control lamivudine (14.8 μg/mL). Compound 9d exhibited significant activity against secretion of HBeAg (IC 50  = 12.26 μg/mL).