Antiviral agents 3. Discovery of a novel small molecule non-nucleoside inhibitor of hepatitis B virus (HBV)

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1644-8. doi: 10.1016/j.bmcl.2011.01.109.

Ian T Crosby ¹, David G Bourke, Eric D Jones, Tyrone P Jeynes, Susan Cox, Jonathan A V Coates, Alan D Robertson

Affiliations

Affiliation

1 Medicinal Chemistry and Drug Action, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia. ian.crosby@monash.edu

PMID: 21333535 DOI: 10.1016/j.bmcl.2011.01.109

Abstract

The discovery of a small molecule non-nucleoside inhibitor of Hepatitis B Virus is described. During our work on conocurvone derived naphthoquinone 'trimers' for the treatment of HIV, we discovered a potent inhibitor 9 of Hepatitis B Virus in an Antiviral screen. During attempts to resynthesis 9 for proof of concept studies, we altered the synthesis in order to attempt to reduced side reactions and difficult to remove by-products. As a result we discovered a small molecule 19 that also was a potent inhibitor of HBV. Importantly, this small molecule inhibitor of Hepatitis B Virus is also an inhibitor of Hepatitis B Virus resistant to 3TC, a bench MARK of nucleoside analogues active in the treatment of Hepatitis B Virus. The development of 19 as an agent to treat HBV infections is discussed.

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