Synthesis and biological evaluation of 1H-benzimidazol-5-ols as potent HBV inhibitors

Yanfang Zhao; Yajing Liu; Dong Chen; Zengquan Wei; Wenzhao Liu; Ping Gong

doi:10.1016/j.bmcl.2010.10.099

Synthesis and biological evaluation of 1H-benzimidazol-5-ols as potent HBV inhibitors

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7230-3. doi: 10.1016/j.bmcl.2010.10.099. Epub 2010 Oct 26.

Authors

Yanfang Zhao¹, Yajing Liu, Dong Chen, Zengquan Wei, Wenzhao Liu, Ping Gong

Affiliation

¹ Key Lab of Structure-Based Drug Design & Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang, PR China.

PMID: 21074429
DOI: 10.1016/j.bmcl.2010.10.099

Abstract

A new series of 1-methyl-1H-benzimidazol-5-ol derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in the HepG2.2.15 cell line. Some of the analogues in this series displayed inhibitory activity superior to lamivudine. Of them, compound 13b was the most potent one, showing an IC(50) value of 7.8 μM and a SI value of 13.0.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antiviral Agents / chemical synthesis*
Antiviral Agents / chemistry
Antiviral Agents / toxicity
Benzimidazoles / chemical synthesis
Benzimidazoles / chemistry*
Benzimidazoles / toxicity
Cell Line, Tumor
DNA Replication / drug effects
Hepatitis B virus / drug effects*
Humans
Lamivudine / toxicity
Structure-Activity Relationship

Substances

Antiviral Agents
Benzimidazoles
Lamivudine