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

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 μM and SI >81.2, was the most promising compound and selected as the benchmark compound for further optimization.