2-Arylthio-5-iodo pyrimidine derivatives as non-nucleoside HBV polymerase inhibitors |
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| Authors: | Jie Wang Liang Zhang Jianxiong Zhao Yu Zhang Qingchuan Liu Chao Tian Zhili Zhang Junyi Liu Xiaowei Wang |
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| Affiliation: | 1. Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, 100191, China;2. Beijing Weijian Jiye Institute of Biotechnology, 100041, China |
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| Abstract: | 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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| Keywords: | Anti-HBV agents Non-nucleoside inhibitors of HBV polymerase 2-Arylthio pyrimidine derivatives Non-radioisotopic enzyme assay Pharmacophore models |
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