Design, synthesis and biological activity of benzo[b]tiophen-3-ol derivatives as monoamine oxidase (hMAO) inhibitors for neurodegenerative disorders.

Anno
2021
Proponente Paola Chimenti - Professore Associato
Sottosettore ERC del proponente del progetto
LS7_4
Componenti gruppo di ricerca
Componente Categoria
Gianluca Ferrigno Dottorando/Assegnista/Specializzando componente non strutturato del gruppo di ricerca
Abstract

Monoamine oxidases, (MAOs) have been widely recognised as important pharmacological targets for the treatment of mood disorders (anxiety, depression) and neurodegeneration (Parkinson's disease, PD) as the results of their effects on monoamine metabolism and level. The products deriving from hMAO enzymatic activity are aldehydes and the ammonium ion, while the by-product hydrogen peroxide is formed in order to regenerate the catalytically active form of the FAD cofactor. Although aldehydes do not appear to accumulate in the healthy brain, some studies have shown that elevated concentration of these products may exert cytotoxic effects. MAO-mediated oxidative stress has been associated with different neurodegenerative pathologies as well as cardiomyopathies. This suggests that reducing the activity of the hMAOs could be useful in order to protect cell. Aims of this project are: a) to design new irreversible and reversible MAO inhibitors as therapeutic tools for neurodegenerative phatologies b) to perform a virtual screening for identifying new inhibitors.

ERC
LS7_4, LS5_7, PE5_17
Keywords:
CHIMICA FARMACEUTICA, SCOPERTA E DESIGN DI FARMACI, CROMATOGRAFIA, CHIMICA COMPUTAZIONALE, METODOLOGIE SINTETICHE

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