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

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

  • Eur J Med Chem. 2010 May;45(5):1919-26. doi: 10.1016/j.ejmech.2010.01.032.
Wei-Li Dong 1,  Zheng-Xiao Liu,  Xing-Hai Liu,  Zheng-Ming Li,  Wei-Guang Zhao
Affiliations

Affiliation

  • 1 State Key Laboratory of Elemento-Organic Chemistry, National Pesticide Engineering Research Center (Tianjin), Nankai University, Tianjin 300071, China.
PMID: 20149495 DOI: 10.1016/j.ejmech.2010.01.032
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 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).

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