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Identification of p -aminobenzylamine derivatives as dual non-covalent inhibitors of the transmembrane host proteases TMPRSS2 and HAT proteases with anti-viral potential

Year: 2025
Type: article
Abstract: -aminobenzylamine derivatives acting as potent dual TMPRSS2/HAT non-covalent inhibitors. In SARS-CoV-2 infection assays in lung epithelial cells, four compounds demonstrated significant antiviral activity without cytotoxicity at tested doses. Drug-likeness profiling confirmed compliance with Lipinski's and Veber's rules, as well as favourable solubility and microsomal stability. These findings highlight a novel chemical series with potential as broad-spectrum antivirals targeting host proteases.
DOI: 10.1039/d5md00680e
Authors: Hélène Carvaillo, Ashok Dussol, Nancy Chaaya, Sara Kadri, Feryel Soualmia, Nicolas Masurier, Chahrazade El Amri
Institutions: École Nationale Supérieure de Chimie de Montpellier, Centre National de la Recherche Scientifique, Université de Montpellier, Institut des Biomolécules Max Mousseron, Inserm, Sorbonne Université, Institut de Biologie Paris-Seine, Développement Adaptation et Vieillissement
Language: English
Field: Medicine
Open Access status: hybrid
Funders: Infrastructures en Biologie Santé et Agronomie, European Cooperation in Science and Technology, Agence Nationale de la Recherche, Institut National de la Santé et de la Recherche Médicale, Centre National de la Recherche Scientifique, Université de Montpellier, Sorbonne Université
OpenAlex ID: W4415620913
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