title: Design and synthesis of imidazo[1,2-α][1,8]naphthyridine derivatives as anti-HCV agents via direct C-H arylation.
abstract: RO8191 represents a newly identified small-molecule IFN-α-substitute, which displays potent anti-HCV activity. In this communication, we reported the design and synthesis of two series of imidazo[1,2-α][1,8]naphthyridine derivatives, as RO8191 analogues, via a direct C-H arylation approach. Notably, by adjusting the reaction conditions, we could achieve the two series of analogues via regioselective single- and double-arylations, respectively. The anti-HCV activities of the synthesized compounds were evaluated within the HCV cell culture system, and the preliminary results showed that some of them displayed promising anti-HCV activities.
authors.affiliation: The Comprehensive AIDS Research Center, and The Department of Pharmacology and Pharmaceutical Sciences, School of Medicine, Tsinghua University, Beijing 100084, China. yefengtang@tsinghua.edu.cn.
authors.forename: Shengdian
authors.initials: S
authors.lastname: Huang
authors.forename: Jie
authors.initials: J
authors.lastname: Qing
authors.forename: Shuo
authors.initials: S
authors.lastname: Wang
authors.forename: Huan
authors.initials: H
authors.lastname: Wang
authors.forename: Linqi
authors.initials: L
authors.lastname: Zhang
authors.forename: Yefeng
authors.initials: Y
authors.lastname: Tang
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D060326:Chemistry Techniques, Synthetic; D015195:Drug Design; D016174:Hepacivirus / Q000187:drug effects*; D007093:Imidazoles / Q000737:chemistry*; D009287:Naphthyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000998:Antiviral Agents; D007093:Imidazoles; D009287:Naphthyridines