Synthesis and anti-Hepatitis B virus activity of a novel class of thiazolylbenzimidazole derivatives

Recently, heterocyclic benzimidazole derivatives have been investigated and validated as a promising class of antiviral agents. In this paper, a series of novel thiazolylbenzimidazole derivatives was synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity on the HepG2.2.15 cell line. Afterwards, the preliminary structure-activity relationship (SAR) was discussed. Compound 8b, with IC₅₀â=â1. 1ââμM and SIâ>â90.9, was the most promising compound and could be selected as a benchmark compound for further investigation. A series of novel benzimidazole analogues was prepared and assessed for their anti-HBV activity and cytotoxicity in vitro. The preliminary structure-activity relationships (SAR) were discussed. Compound 8b showed good antiviral activities and high selectivity. Further studies of SAR based on 8b are ongoing.