Design, Synthesis And Antiviral Evaluation Of Novel N-6 Substituent Adenosine Analogues

Antiviral agents play an important role in the treatment of viral diseases. However, due to the continuous emergence of new viruses and virus resistance increasing, the current antiviral drugs can not cure all the viral diseases. Therefore, finding new antiviral drugs is important for human health.In our work, a series of novel N-6 substituent adenosine analogues were synthesized and their antiviral activities were tested against Coxsackie virus B3 (CVB3) and Herpes simplex virus type 1 (HSV-1) in HEp-2 cells. All the compounds were identified by 1H NMR,13C NMR, HRMS(ESI or EI). All the analogues antiviral activities were tested against Coxsackie virus B3 (CVB3) and Herpes simplex virus type 1 (HSV-1)in HEp-2 cells. All the compounds showed low inhibitory activity against HSV-1, but most compounds exhibit inhibitory activity against CVB3, nine analogues showed high antiviral activity on CVB3, especially, one derivative showed promising activities against CVB3 with IC50 at low concentrations and higher selectivity index, better than the commercialized medicine, Ribavirin.The above work confirmed that the N-6 piperazine adenosine analogues have antiviral activity on CVB3, and have the potential to become antiviral agents.