Small-molecule inhibitors for the treatment of hepatitis B virus documented in patents.
Small-molecule inhibitors for the treatment of hepatitis B virus documented in patents.
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DOI：
10.2174/1389557511313050012
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发表时间：
2013-03
期刊：
影响因子：
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通讯作者：
Chang-An Geng;Li-Jun Wang;R. Guo;Ji-Jun Chen
中科院分区：
文献类型：
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作者：
Chang-An Geng;Li-Jun Wang;R. Guo;Ji-Jun Chen
乙型肝炎病毒（HBV）感染是世界范围内严重的健康问题，目前的治疗方法包括疫苗、免疫调节剂、干扰素和核苷类似物，远远不能令人满意。为了寻找新的抗hbv药物，大量的研究已经揭示了大量具有不同骨架和抗hbv活性的小分子化合物。虽然已经发表了一些关于抗hbv进展的综述，但它们主要集中在期刊文章中报道的结果。本文综述了近年来（2001年至2010年）申请的小分子抗hbv抑制剂的结构特征和抗hbv特性。这些小分子在结构上主要分为核苷类似物（环核苷和无环核苷）和非核苷（天然和合成的化合物）两类，在体外具有抑制HBsAg和HBeAg分泌和HBV DNA复制的活性，在体内具有抗dhbv DNA的活性。特别是结构多样、作用机制新颖的非核苷类，为抗HBV药物的发现提供了丰富的候选药物，有望作为HBV感染的辅助治疗药物。本文将为了解当前的抗hbv研究和开发新的抗hbv药物提供有价值的信息。
Hepatitis B virus (HBV) infection is a serious health problem worldwide, and the current treatment methods including vaccines, immunomodulators, interferons and nucleoside analogs are far from satisfactory. For the search of new anti-HBV agents, much investigation has revealed a large number of small-molecule compounds with various skeletons and promising anti-HBV activities. Although some reviews on anti-HBV progress have been published, they are mainly concentrated on the results reported in journal articles. This review provides an overview of the structural features and anti-HBV properties of the small-molecule anti-HBV inhibitors claimed in recent patents (from 2001 to 2010). These small-molecules can be structurally classified as two main types, nucleoside analogs (cyclic and acyclic nucleosides) and non-nucleosides (natural and synthesized compounds), which are declared with the activity inhibiting the secretion of HBsAg and HBeAg and HBV DNA replication in vitro, as well as anti-DHBV DNA in vivo. Especially, the non-nucleosides with diverse skeletons and novel mechanism offer prolific candidates for anti-HBV drug discovery, which are preferred to be used as adjuvant therapy for HBV infection. This paper will provide valuable information for understanding the current anti-HBV investigation and developing new anti-HBV agents.