Fiche publication
Date publication
avril 2022
Journal
Molecules (Basel, Switzerland)
Auteurs
Membres identifiés du Cancéropôle Est :
Dr DEJAEGERE Annick
,
Dr STOTE Roland
Tous les auteurs :
Bergin JCJ, Tan KK, Nelson AK, Amarandei CA, Hubscher-Bruder V, Brandel J, Voinarovska V, Dejaegere A, Stote RH, Tétard D
Lien Pubmed
Résumé
Two analogues of tolcapone where the nitrocatechol group has been replaced by a 1-hydroxy-2(1)-pyridinone have been designed and synthesised. These compounds are expected to have a dual mode of action both beneficial against Parkinson's disease: they are designed to be inhibitors of catechol -methyl transferase, which contribute to the reduction of dopamine in the brain, and to protect neurons against oxidative damage. To assess whether these compounds are worthy of biological assessment to demonstrate these effects, measurement of their pa and stability constants for Fe(III), in silico modelling of their potential to inhibit COMT and blood-brain barrier scoring were performed. These results demonstrate that the compounds may indeed have the desired properties, indicating they are indeed promising candidates for further evaluation.
Mots clés
1-hydroxy-2(1H)-pyridinone, Parkinson’s disease, catechol O-methyl transferase
Référence
Molecules. 2022 04 28;27(9):
