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

Bioorganic & Medicinal Chemistry Letters
2010.0

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.

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