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 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).
Dong
Wei-Li
WL
State Key Laboratory of Elemento-Organic Chemistry, National Pesticide Engineering Research Center (Tianjin), Nankai University, Tianjin 300071, China.
Liu
Zheng-Xiao
ZX
Liu
Xing-Hai
XH
Li
Zheng-Ming
ZM
Zhao
Wei-Guang
WG
D020106:Acrylamide / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D018360:Crystallography, X-Ray; D006515:Hepatitis B virus / Q000187:drug effects* / Q000502:physiology*; D006801:Humans; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D015394:Molecular Structure; D013237:Stereoisomerism; D013830:Thiadiazoles / Q000737:chemistry*; D014779:Virus Replication / Q000187:drug effects*
D000998:Antiviral Agents; D013830:Thiadiazoles; D020106:Acrylamide