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Mini-Reviews in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

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

Volume 13, Issue 5, 2013

Page: [749 - 776] Pages: 28

DOI: 10.2174/1389557511313050012

Price: $65

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 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.

Keywords: Hepatitis B virus (HBV), small-molecule inhibitors, nucleoside analogs, non-nucleosides, natural products, synthesized compounds, chemical modification, patents


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