2-Arylthio-5-iodo pyrimidine derivatives as non-nucleoside HBV polymerase inhibitors

Publication date: Available online 17 February 2018
Source:Bioorganic & Medicinal Chemistry
Author(s): Jie Wang, Liang Zhang, Jianxiong Zhao, Yu Zhang, Qingchuan Liu, Chao Tian, Zhili Zhang, Junyi Liu, Xiaowei Wang
In this study, a series of 2-arylthio-5-iodo pyrimidine derivatives, as non-nucleoside hepatitis B virus inhibitors, were evaluated and firstly reported as potential anti-HBV agents. To probe the mechanism of active agents, DHBV polymerase was isolated and a non-radioisotopic assay was established for measuring HBV polymerase. The biological results demonstrated that 2-arylthio-5-iodo pyrimidine derivatives targeted HBV polymerase. In addition, pharmacophore models were constructed for future optimization of lead compounds. Further study will be performed for the development of non-nucleoside anti-HBV agents.

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