title: Synthesis and anti-BVDV activity of novel δ-sultones in vitro: implications for HCV therapies.
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.
authors.affiliation: New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, KeXue DaDao, Zheng zhou, Henan Province 450001, PR China.
authors.forename: Hai-Wei
authors.initials: HW
authors.lastname: Xu
authors.affiliation: New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, KeXue DaDao, Zheng zhou, Henan Province 450001, PR China.
authors.forename: Ling-Jie
authors.initials: LJ
authors.lastname: Zhao
authors.affiliation: School of Life Sciences, Zhengzhou University, No. 100, KeXue DaDao, Zheng zhou, Henan Province 450001, PR China.
authors.forename: Huan-Fei
authors.initials: HF
authors.lastname: Liu
authors.affiliation: School of Life Sciences, Zhengzhou University, No. 100, KeXue DaDao, Zheng zhou, Henan Province 450001, PR China.
authors.forename: Dan
authors.initials: D
authors.lastname: Zhao
authors.affiliation: New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, KeXue DaDao, Zheng zhou, Henan Province 450001, PR China.
authors.forename: Jiao
authors.initials: J
authors.lastname: Luo
authors.affiliation: New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, KeXue DaDao, Zheng zhou, Henan Province 450001, PR China.
authors.forename: Xiao-Ping
authors.initials: XP
authors.lastname: Xie
authors.affiliation: New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, KeXue DaDao, Zheng zhou, Henan Province 450001, PR China.
authors.forename: Wen-Sheng
authors.initials: WS
authors.lastname: Liu
authors.affiliation: New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, KeXue DaDao, Zheng zhou, Henan Province 450001, PR China.
authors.forename: Jia-Xin
authors.initials: JX
authors.lastname: Zheng
authors.affiliation: School of Life Sciences, Zhengzhou University, No. 100, KeXue DaDao, Zheng zhou, Henan Province 450001, PR China. Electronic address: daiguifu@zzu.edu.cn.
authors.forename: Gui-Fu
authors.initials: GF
authors.lastname: Dai
authors.affiliation: New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, KeXue DaDao, Zheng zhou, Henan Province 450001, PR China. Electronic address: liuhm@zzu.edu.cn.
authors.forename: Hong-Min
authors.initials: HM
authors.lastname: Liu
authors.affiliation: College of Chemistry and Molecular Engineering, Zhengzhou University, No. 100, KeXue DaDao, Zheng zhou, Henan Province 450001, PR China.
authors.forename: Long-Hua
authors.initials: LH
authors.lastname: Liu
authors.affiliation: New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, KeXue DaDao, Zheng zhou, Henan Province 450001, PR China.
authors.forename: Yi-Bo
authors.initials: YB
authors.lastname: Liang
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002417:Cattle; D001908:Diarrhea Viruses, Bovine Viral / Q000187:drug effects*; D004195:Disease Models, Animal; D015195:Drug Design; D016174:Hepacivirus / Q000187:drug effects*
chemical_list: D000998:Antiviral Agents
keywords: Anti-BVDV; Anti-HCV; CSIC reaction; Lactone; Sultone; Synthesis