Poster (Scientific congresses and symposiums)
EXPLORING COUMARIN DERIVATIVES AS NOVEL ANTIVIRAL AGENTS TARGETING TMPRSS2: A MULTIDISCIPLINARY APPROACH FOR RESPIRATORY VIRAL DISEASE TREATMENT
Lesenfants, Cindy; Leroy, Charline; Goffin, Eric et al.
2023MedChem 2023
Editorial reviewed
 

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Keywords :
SARS-CoV-2; TMPRSS2; Serine protease; coumarinic compounds; In vitro assay
Abstract :
[en] The recent emergence of the new coronavirus, SARS-CoV-2, which triggered a global pandemic of severe acute respiratory syndrome, has highlighted the need to develop new antiviral treatments. In this context, the human serine protease TMPRSS2, implicated in the entry mechanism of several viruses, including specific strains of influenza and coronaviruses, has emerged as a target of significant interest. Preliminary in vitro and in silico results from our chemical library suggest that appropriately substituted coumarin derivatives could present a promising solution. Our main objective is to prepare coumarin derivatives substituted with a basic functional group and a leaving group at the 6-position of the coumarin ring. To guide our synthesis, tests using isolated enzymes will be conducted, providing essential insights into the selectivity and activity of these compounds. Furthermore, a comprehensive assessment of the cytotoxicity of these compounds will play a crucial role in guiding our synthesis. Finally, these new compounds will undergo testing against several viral strains to assess their antiviral activity. This multidisciplinary approach aims to identify promising antiviral agents that would significantly expand the options available for the treatment of respiratory diseases. These compounds could also play a fundamental role in the prevention and management of future pandemics.
Research center :
CIRM - Centre Interdisciplinaire de Recherche sur le Médicament - ULiège [BE]
Disciplines :
Pharmacy, pharmacology & toxicology
Author, co-author :
Lesenfants, Cindy  ;  Université de Liège - ULiège > Département de pharmacie > Chimie pharmaceutique
Leroy, Charline ;  Université de Liège - ULiège > Département de pharmacie
Goffin, Eric ;  Université de Liège - ULiège > Département de pharmacie > Chimie pharmaceutique
Colson, Thomas  ;  Université de Liège - ULiège > Département de pharmacie > Chimie pharmaceutique
Chaaya, Nancy;  Sorbonne Université [FR] > Biological Adaptation and Ageing
Garigliany, Mutien-Marie  ;  Université de Liège - ULiège > Département de morphologie et pathologie (DMP) > Pathologie générale et autopsies
Chavatte, Philippe;  ULille - University of Lille [FR] > Institute for Translational Research in Inflammation
Reboud-Ravaux, Michèle;  Sorbonne Université [FR] > Biological Adaptation and Ageing
Pirotte, Bernard ;  Université de Liège - ULiège > Département de pharmacie
El Amri, Chahrazade;  Sorbonne Université [FR] > Biological Adaptation and Ageing
Francotte, Pierre  ;  Université de Liège - ULiège > Département de pharmacie > Chimie pharmaceutique
Language :
English
Title :
EXPLORING COUMARIN DERIVATIVES AS NOVEL ANTIVIRAL AGENTS TARGETING TMPRSS2: A MULTIDISCIPLINARY APPROACH FOR RESPIRATORY VIRAL DISEASE TREATMENT
Publication date :
08 December 2023
Event name :
MedChem 2023
Event place :
Bruxelles, Belgium
Event date :
8 décembre 2023
Audience :
International
Peer reviewed :
Editorial reviewed
Funders :
Fondation Léon Fredericq [BE]
F.R.S.-FNRS - Fonds de la Recherche Scientifique [BE]
Available on ORBi :
since 11 December 2023

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