Synthesis, characterization, cytotoxicity, and antiviral activity of new coumarin analogues against coronavirus

Abstract

Coronaviruses have emerged as a global health challenge, with the recent outbreak of SARS-CoV-2 affecting more than 600 million individuals worldwide. While vaccination remains a central preventive approach, addressing SARS-CoV-2 involves antiviral drugs, monoclonal antibodies, and corticosteroids. Research indicates that coumarin exhibits potent antiviral properties. Therefore, this study aimed to investigate the antiviral properties of newly synthesized coumarin analogues (NCA) against coronaviruses. The study involved the synthesis of NCAs through esterification, hydrazination, imination, and cyclo-condensation reactions, followed by their characterization using FTIR, NMR, and Mass Spectrometry. Cell viability analysis was conducted using HEK-293 cells, and the viral replication inhibition activity of NCAs against OC43 was assessed using plaque assays. The antiviral activity of NCAs against the Infectious Bronchitis Virus (IBV) was evaluated based on mortality rate, lesion development, and viral RNA load suppression. The study successfully synthesized NCAs and elucidated their structures. The viral plaque assay demonstrated the ability of NCAs to effectively inhibit viral replication. Analysis of viral RNA by qRTPCR confirmed a decrease in OC43 viral load following NCA treatment. Immunofluorescence assays also showed a reduction in SARS-CoV-2 infection in the presence of NCAs. Evaluation of cytotoxicity using HEK-293 cells indicated that NCAs exhibited a favourable safety profile while effectively inhibiting IBV viral replication. These findings highlight the promising antiviral activities of NCAs against coronavirus replication and infection.

Keywords

• Coronavirus
• SARS-CoV-2
• Infectious Bronchitis Virus
• OC43
• Antiviral
• Coumarin derivatives