Design and synthesis of novel benzimidazole derivatives as inhibitors of hepatitis B virus

Yu Luo; Jia-Ping Yao; Li Yang; Chun-Lan Feng; Wei Tang; Gui-Feng Wang; Jian-Pin Zuo; Wei Lu

doi:10.1016/j.bmc.2010.05.076

Design and synthesis of novel benzimidazole derivatives as inhibitors of hepatitis B virus

Bioorg Med Chem. 2010 Jul 15;18(14):5048-55. doi: 10.1016/j.bmc.2010.05.076. Epub 2010 Jun 1.

Authors

Yu Luo¹, Jia-Ping Yao, Li Yang, Chun-Lan Feng, Wei Tang, Gui-Feng Wang, Jian-Pin Zuo, Wei Lu

Affiliation

¹ Department of Chemistry, East China Normal University, 3663 North Zhongshan Road, Shanghai 200062, PR China.

PMID: 20639110
DOI: 10.1016/j.bmc.2010.05.076

Abstract

A series of novel benzimidazole derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in the HepG2.2.15 cell line. The preliminary SAR was discussed. Compound 12a, with IC50<0.41 microM and SI>81.2, was the most promising compound and selected as the benchmark compound for further optimization.

Publication types

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

MeSH terms

Antiviral Agents / chemical synthesis
Antiviral Agents / chemistry*
Antiviral Agents / pharmacology*
Benzimidazoles / chemical synthesis
Benzimidazoles / chemistry*
Benzimidazoles / pharmacology*
Cell Line, Tumor
Cell Survival / drug effects
Hepatitis B / drug therapy*
Hepatitis B virus / drug effects*
Humans
Structure-Activity Relationship

Substances

Antiviral Agents
Benzimidazoles