title: The discovery and characterization of a novel scaffold as a potent hepatitis C virus inhibitor.
abstract: HCV infections are a major global health concern. Although direct acting antiviral agents have significantly improved the response rate of anti-HCV therapy, they also suffer from drug resistance, unfavorable pharmacokinetic profiles and high costs. Thus, it is still highly desirable to develop new anti-HCV therapeutics. Herein a novel anti-HCV benzothiazole scaffold was discovered by phenotypic screening. Further target characterization and structural optimization studies revealed that the benzothiazole-disulfoamide derivatives were potent anti-HCV molecules with good selectivity and acted by targeting NS5A.
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China. shengcq@hotmail.com.
authors.forename: Na
authors.initials: N
authors.lastname: Liu
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China. shengcq@hotmail.com.
authors.forename: Shiping
authors.initials: S
authors.lastname: Zhu
authors.affiliation: The First Department of Hepatic Surgery, Eastern Hepatobiliary Hospital, Second Military Medical University, 225 Changhai Road, Shanghai 200438, China.
authors.forename: Xianghua
authors.initials: X
authors.lastname: Zhang
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China. shengcq@hotmail.com.
authors.forename: Xunkui
authors.initials: X
authors.lastname: Yin
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China. shengcq@hotmail.com.
authors.forename: Guoqiang
authors.initials: G
authors.lastname: Dong
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China. shengcq@hotmail.com.
authors.forename: Jianzhong
authors.initials: J
authors.lastname: Yao
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China. shengcq@hotmail.com.
authors.forename: Zhenyuan
authors.initials: Z
authors.lastname: Miao
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China. shengcq@hotmail.com.
authors.forename: Wannian
authors.initials: W
authors.lastname: Zhang
authors.affiliation: Shanghai Public Health Clinical Center, Fudan University, Caolang Road 2901, Shanghai 201508, China. zhangxiaonan@shaphc.org.
authors.forename: Xiaonan
authors.initials: X
authors.lastname: Zhang
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China. shengcq@hotmail.com.
authors.forename: Chunquan
authors.initials: C
authors.lastname: Sheng
mesh_terms: D000998:Antiviral Agents / Q000494:pharmacology*; D055808:Drug Discovery; D016174:Hepacivirus / Q000187:drug effects*
chemical_list: D000998:Antiviral Agents