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

Jih Ru Hwu, Mohit Kapoor, Nitesh K. Gupta, Shwu-Chen Tsay, Wen-Chieh Huang, Kui-Thong Tan, Yu-Chen Hu, Pieter LyssenJohan Neyts
European Journal of Medicinal Chemistry, 卷.232, 114164
03/2022

摘要

Broad-spectrum Chikungunya virus Coumarin Hepatitis C virus Quinazolin-4-amine Structure–activity relationship Pharmacology Drug Discovery Organic Chemistry
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–SCH 2 –coumarin conjugated compounds. Our data of the virus-cell-based assay show five new conjugates inhibit chikungunya virus with EC 50 values as potent as 1.96 μM and two conjugates inhibit hepatitis C virus with EC 50 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.

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