4.7 Article

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

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 232, Issue -, Pages -

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2022.114164

Keywords

Quinazolin-4-amine; Coumarin; Chikungunya virus; Hepatitis C virus; Broad-spectrum; Structure-activity relationship

Funding

  1. Ministry of Science and Technology (MOST) [110-2113-M-007-011, 110-2634-F-007-023]
  2. Ministry of Education [110QR001I5, 109QR001I5]
  3. European Commission SILVER project within the 7th Framework Programme as Cooperation Project [260644]

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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.
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.

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