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Identification of sulphonamide-tethered N-((triazol-4-yl)methyl)isatin derivatives as inhibitors of SARS-CoV-2 main protease

ElNaggar, Mai H, Elgazar, Abdullah A, Gamal, Ghada, Hamed, Shimaa M, Elsayed, Zainab M, El-Ashrey, Mohamed K, Abood, Amira, El Hassab, Mahmoud A, Soliman, Ahmed M, El-Domany, Ramadan A, and others. (2023) Identification of sulphonamide-tethered N-((triazol-4-yl)methyl)isatin derivatives as inhibitors of SARS-CoV-2 main protease. Journal of enzyme inhibition and medicinal chemistry, 38 (1). Article Number 2234665. ISSN 1475-6374. (doi:10.1080/14756366.2023.2234665) (KAR id:102199)

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SARS-CoV-2 pandemic in the end of 2019 led to profound consequences on global health and economy. Till producing successful vaccination strategies, the healthcare sectors suffered from the lack of effective therapeutic agents that could control the spread of infection. Thus, academia and the pharmaceutical sector prioritise SARS-CoV-2 antiviral drug discovery. Here, we exploited previous reports highlighting the anti-SARS-CoV-2 activities of isatin-based molecules to develop novel triazolo-isatins for inhibiting main protease (Mpro) of the virus, a crucial enzyme for its replication in the host cells. Particularly, sulphonamide showed promising inhibitory activity with an IC = 0.249 µM. Additionally, inhibited viral cell proliferation with an IC of 4.33 µg/ml, and was non-toxic to VERO-E6 cells (CC50 = 564.74 µg/ml) displaying a selectivity index of 130.4. analysis of disclosed its ability to interact with key residues in the enzyme active site, supporting the obtained findings.

Item Type: Article
DOI/Identification number: 10.1080/14756366.2023.2234665
Uncontrolled keywords: Humans, Isatin, Sulfonamides - pharmacology, main protease, SARS-CoV-2, FRET assay and moleuclar docking, Isatin derivatives, Sulfanilamide, click chemistry, COVID-19
Subjects: Q Science > QH Natural history > QH301 Biology
Divisions: Divisions > Division of Natural Sciences > Biosciences
SWORD Depositor: JISC Publications Router
Depositing User: JISC Publications Router
Date Deposited: 26 Jul 2023 15:13 UTC
Last Modified: 26 Jul 2023 15:14 UTC
Resource URI: (The current URI for this page, for reference purposes)
ElNaggar, Mai H:
Elgazar, Abdullah A:
Abood, Amira:
Supuran, Claudiu T:
Eldehna, Wagdy M:
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