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

Abstract

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 μM and two conjugates inhibit hepatitis C virus with EC₅₀ values as low as 16.6 μM. 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.