Design And Synthesis Of 1H-Benzo[d]Imidazol-5-Ol Derivatives

In this paper, the biological characteristics of the hepatitis B virus, and the development of the anti-HBV drugs were introduced briefly. The design and synthesis of 1H-benzo[d]imidazol-5-ol derivatives were introduced in details.Based on the structure-activity relationship studies of the former research, Arbidol was took as lead compound, and the indole ring was replaced with the benzimidazole ring, which had been reported to have antiviral activities in many literatures. Thus 1H-benzo[d]imidazol-5-ol derivatives were designed, and modifications and optimizations were made at 1-position 2-position 4-position and 6-position, in order to investigate the effects of the steric effect the electronic effect and the hydrophobicity on antiviral activities.The synthetic route was confirmed in the experiments. Starting from 4-nitrophenol or 2-fluoro-4-nitrophenol, the target compounds were synthesized through two different routs. Also, the reaction conditions were optimized during the experiments.Total 30 target compounds that had never been reported in literatures were designed and synthesized, their structures were confirmed by MS and ~1H-NMR. The pharmacological evaluation of the target compounds is underway.