151. Synthesis and anti-BVDV activity of novel δ-sultones in vitro: Implications for HCV therapies.
- Author
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Xu, Hai-Wei, Zhao, Ling-Jie, Liu, Huan-Fei, Zhao, Dan, Luo, Jiao, Xie, Xiao-Ping, Liu, Wen-Sheng, Zheng, Jia-Xin, Dai, Gui-Fu, Liu, Hong-Min, Liu, Long-Hua, and Liang, Yi-Bo
- Subjects
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DRUG synthesis , *SULTONES , *ANTIVIRAL agents , *BOVINE viral diarrhea virus , *HEPATITIS C treatment , *IN vitro studies , *DRUG development - Abstract
Abstract: In this study we report the synthesis and activity against bovine viral diarrhea virus (BVDV) of a novel series of bicycle δ-sultones containing γ-lactones. BVDV is responsible for major losses in cattle. Some of the synthesized δ-sultones showed pronounced anti-BVDV activity with EC50 values of 0.12–1.0μM and no significant cytotoxicity. Among them, the ortho bromosubstituted derivative 4f (EC50 =0.12μM) showed better antiviral activity than other derivatives and was 10 fold more that of than positive control ribavirin (EC50 =1.3μM). BVDV is also considered to be a valuable surrogate for the hepatitis C virus (HCV) in antiviral drug studies. The above results provided a novel candidate for the development of anti-HCV agents. [Copyright &y& Elsevier]
- Published
- 2014
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