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Mini-Reviews in Medicinal Chemistry
ISSN (Print): 1389-5575
ISSN (Online): 1875-5607
Epub Full Text Article
DOI: 10.2174/13895575113139990056      Price:  $95

Small-Molecule Inhibitors for the Treatment of Hepatitis B Virus Documented in Patents

Author(s): Chang-An Geng, Li-Jun Wang, Rui-Hua Guo and Ji-Jun Chen
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 nonnucleosides 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.
Hepatitis B virus (HBV), small-molecule inhibitors, nucleoside analogs, non-nucleosides, natural products, synthesized compounds, chemical modification, patents
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