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Discovery of Imidazo[1,2-α][1,8]naphthyridine Derivatives as Potential HCV Entry Inhibitor

Huan Wang, Shuo Wang, Lili Cheng, Ligong Chen, Yongguang Wang, Jie Qing, Shengdian Huang, Yuanhao Wang, Xiaoqiang Lei, Yunfei Wu, Zhilong Ma, Linqi Zhang, Yefeng Tang

ACS Med Chem Lett. 2015 Jul 27;6(9):977-81.

PMID: 26396683

Abstract:

RO8191 represents a newly discovered small-molecule IFN-like agent that displays potent anti-HCV activity. With it as lead, a series of compounds bearing an imidazo[1,2-α][1,8]naphthyridine core and an amide bond-linked side chain were designed and synthesized. These compounds were evaluated on HCV cell culture system (HCVcc-hRluc-JFH1), and some of them exhibited remarkable anti-HCV activity (EC50 = 0.017-0.159 μM) and low toxicity (CC50 > 25 μM). Moreover, it was revealed that these newly identified anti-HCV agents exert their antiviral effect through a distinct mechanism of action from that of RO8191 by targeting the viral entry process. Thus, our study provides a starting point for the development of potential HCV entry inhibitor.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP691868889 RO8191 RO8191 691868-88-9 Price
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