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.

中文翻译：

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2-芳硫基-5-碘嘧啶衍生物作为非核苷HBV聚合酶抑制剂

在这项研究中，评估了一系列2-芳硫基-5-碘嘧啶衍生物，作为非核苷乙型肝炎病毒抑制剂，并首次报道其为潜在的抗HBV药物。为了探究活性剂的作用机理，分离了DHBV聚合酶并建立了非放射性同位素测定法来测量HBV聚合酶。生物学结果表明2-芳硫基-5-碘嘧啶衍生物靶向HBV聚合酶。此外，还建立了药效团模型以用于将来对前导化合物的优化。非核苷类抗HBV药物的开发将进行进一步的研究。