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

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 IC50 value of 7.8 μM and a SI value of 13.0.

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