Design, Synthesis and Evaluation of Novel 4-(4-Chlorobenzyl)-6-methylpyridazin-3(2H)-one Derivatives as Hepatitis B Virus Inhibitors

摘要

22 Novel pyridazin-3-ones have been designed for anti-hepatitis B virus (HBV) activity by structural modificationes of 3711 which is capsid assembly modulator. Structure of the target compounds were confirmed by elemental analysis and spectroscopic data including X-ray studies. Among them, the compound having piperazine moiety showed notable inhib- itory activity on secretion of HBV DNA and HBeAg which is comparable to that of AT-130. The preliminary structure-activity relationeships (SARs) of the newly synthesized pyridazin-3-one analogues were summarized, which may help researchers to discover more potent anti-HBV agents bearing pyridazine-3-one scaffold.