Perylenyltriazoles inhibit reproduction of enveloped viruses

摘要

Abstract 1-Substituted 4-perylen-2(3)-yl-1,2,3-triazoles, easily accessible by ‘click’ reaction and combining in one molecule a polyaromatic unit and a nitrogen heterocycle, were found to strongly inhibit the reproduction of enveloped viruses. 5-[4-(Perylen-3-yl)-1,2,3-triazol-1-yl]-uridine and 2-[1-(2-hydroxyethyl)-1,2,3-triazol-4-yl]perylene show EC 50 of 0.031 and 0.023?μM, respectively, against tick-borne encephalitis virus (TBEV). Remarkably, the nucleoside unit appears to be not essential for antiviral activity. These results provide deeper understanding of structural basis of activity for this new class of antivirals. Graphical abstract 4-Perylenyl-1,2,3-triazoles, easily accessible by ‘click’ reaction and combining in one molecule the polyaromatic unit and the nitrogen heterocycle, were found to have potent activity against enveloped viruses. Display Omitted Highlights ? 1-Substituted 4-(perylen-2(3)-yl)-1,2,3-triazoles were prepared using ‘click’ chemistry approach. ? Perylenyltriazoles have high activity against enveloped viruses. ? Nucleoside part of the molecule is not essential for antiviral activity. ? The discovered antiviral perylenyltriazole scaffold pave the way to new antivirals.