title: Small-molecule inhibitors for the treatment of hepatitis B virus documented in patents.
abstract: 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.
authors: 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.
authors: Chang-An
authors: CA
authors: Geng
authors: Li-Jun
authors: LJ
authors: Wang
authors: Rui-Hua
authors: RH
authors: Guo
authors: Ji-Jun
authors: JJ
authors: Chen
mesh_terms: D000998:Antiviral Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D001688:Biological Products / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D006509:Hepatitis B / Q000188:drug therapy*; D006514:Hepatitis B Surface Antigens / Q000378:metabolism; D006513:Hepatitis B e Antigens / Q000378:metabolism; D006515:Hepatitis B virus / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D009705:Nucleosides / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D054852:Small Molecule Libraries / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D014779:Virus Replication / Q000187:drug effects
chemical_list: D000998:Antiviral Agents; D001688:Biological Products; D006514:Hepatitis B Surface Antigens; D006513:Hepatitis B e Antigens; D009705:Nucleosides; D054852:Small Molecule Libraries