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

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 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 (IC50 = 12.26 μg/mL).

Graphical abstractA series of new acrylamide derivatives containing 1,2,3-thiadiazole were synthesized, characterized and tested in vitro against HBV. Some of the new compounds display excellent activity against DNA reproduction and against HBeAg of HBV.Figure optionsDownload full-size imageDownload as PowerPoint slide