首页|Synthesis and antiviral activities of quinazolinamine-coumarin conjugates toward chikungunya and hepatitis C viruses
Synthesis and antiviral activities of quinazolinamine-coumarin conjugates toward chikungunya and hepatitis C viruses
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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.
Quinazolin-4-amineCoumarinChikungunya virusHepatitis C virusBroad-spectrumStructure-activity relationshipANTI-HCV AGENTSMEDICINAL CHEMISTRYDIMROTH REARRANGEMENTINHIBITING AGENTSDRUG DISCOVERYDERIVATIVESSPECTRUMPOTENTREPLICATIONDESIGN
Kapoor, Mohit、Gupta, Nitesh K.、Tsay, Shwu-Chen、Huang, Wen-Chieh、Tan, Kui-Thong、Hu, Yu-Chen、Hwu, Jih Ru、Lyssen, Pieter、Neyts, Johan