State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Heilongtan, Kunming 650201, Yunnan, P.R. China.
Mini Rev Med Chem. 2013 Apr 1;13(5):749-76. doi: 10.2174/1389557511313050012.
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.
乙型肝炎病毒（HBV）感染是一个全球性的严重健康问题，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等，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许多具有不同骨架和有前途的抗 HBV 活性的小分子化合物。尽管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上。本综述概述了近年来（2001 年至 2010 年）专利中声称的小分子抗 HBV 抑制剂的结构特征和抗 HBV 特性。这些小分子可以分为两类主要类型，核苷类似物（环和非环核苷）和非核苷（天然和合成化合物），它们被宣布具有抑制 HBsAg 和 HBeAg 分泌以及体外 HBV DNA 复制以及体内抗 DHBV DNA 的活性。特别是，具有不同骨架和新颖机制的非核苷类化合物为抗 HBV 药物发现提供了丰富的候选物，它们更适合作为 HBV 感染的辅助治疗药物。本文将为了解当前抗 HBV 研究和开发新的抗 HBV 药物提供有价值的信息。
