Synthesis and antiviral activities of quinazolinamine-coumarin conjugates toward chikungunya and hepatitis C viruses

Development of new drugs with broad-spectrum to combat RNA viruses would be beneficial to mankind but faces a great challenge. We designed and efficiently synthesized a series of quinazolin-4-amine-SCH2-coumarin conjugated compounds. Our data of the virus-cell-based assay show five new conjugates inhibit chikungunya virus with EC50 values as potent as 1.96 mu M and two conjugates inhibit hepatitis C virus with EC50 values as low as 16.6 mu M. These conjugates possess a xylene substituent at the C-4 amino group of quinazoline and a t-butyl substituent at the C-6' position of coumarin. (c) 2022 Elsevier Masson SAS. All rights reserved.

Automated summary

The development of new drugs with broad-spectrum activity against RNA viruses is of great significance for mankind, but it is also faced with significant challenges. In this study, a series of quinazolin-4-amine-SCH2-coumarin conjugated compounds were designed and synthesized, and their anti-viral activities against chikungunya virus and hepatitis C virus were evaluated using virus-cell-based assays.