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

Wei-Li Dong; Zheng-Xiao Liu; Xing-Hai Liu; Zheng-Ming Li; Wei-Guang Zhao

doi:10.1016/j.ejmech.2010.01.032

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. Epub 2010 Jan 25.

Authors

Wei-Li Dong¹, Zheng-Xiao Liu, Xing-Hai Liu, Zheng-Ming Li, Wei-Guang Zhao

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).

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Acrylamide / chemical synthesis
Acrylamide / chemistry
Acrylamide / pharmacology*
Antiviral Agents / chemical synthesis*
Antiviral Agents / chemistry
Antiviral Agents / pharmacology*
Cell Line
Cell Survival / drug effects
Crystallography, X-Ray
Hepatitis B virus / drug effects*
Hepatitis B virus / physiology*
Humans
Microbial Sensitivity Tests
Models, Molecular
Molecular Structure
Stereoisomerism
Thiadiazoles / chemistry*
Virus Replication / drug effects*

Substances

Antiviral Agents
Thiadiazoles
Acrylamide