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: Chang-An Geng, Li-Jun Wang, Rui-Hua Guo, Ji-Jun Chen
• Journal: Mini reviews in medicinal chemistry (Mini Rev Med Chem) Vol. 13 Issue 5 Pg. 749-76 (Apr 01 2013) ISSN: 1875-5607 [Electronic] Netherlands
• PMID: 23317498 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review)

Chemical References

• Antiviral Agents
• Biological Products
• Hepatitis B Surface Antigens
• Hepatitis B e Antigens
• Nucleosides
• Small Molecule Libraries

Topics

• Antiviral Agents (chemistry, pharmacology, therapeutic use)
• Biological Products (chemistry, pharmacology, therapeutic use)
• Hepatitis B (drug therapy)
• Hepatitis B Surface Antigens (metabolism)
• Hepatitis B e Antigens (metabolism)
• Hepatitis B virus (drug effects, metabolism)
• Humans
• Nucleosides (chemistry, pharmacology, therapeutic use)
• Small Molecule Libraries (chemistry, pharmacology, therapeutic use)
• Virus Replication (drug effects)