Design, synthesis and biological evaluation of light-driven on-off multitarget AChE and MAO-B inhibitors.
Journal
RSC medicinal chemistry
ISSN: 2632-8682
Titre abrégé: RSC Med Chem
Pays: England
ID NLM: 101759460
Informations de publication
Date de publication:
20 Jul 2022
20 Jul 2022
Historique:
received:
11
02
2022
accepted:
19
05
2022
entrez:
4
8
2022
pubmed:
5
8
2022
medline:
5
8
2022
Statut:
epublish
Résumé
Neurodegenerative diseases are multifactorial disorders characterized by protein misfolding, oxidative stress, and neuroinflammation, finally resulting in neuronal loss and cognitive dysfunctions. Nowadays, an attractive strategy to improve the classical treatments is the development of multitarget-directed molecules able to synergistically interact with different enzymes and/or receptors. In addition, an interesting tool to refine personalized therapies may arise from the use of bioactive species able to modify their activity as a result of light irradiation. To this aim, we designed and synthesized a small library of cinnamic acid-inspired isomeric compounds with light modulated activity able to inhibit acetylcholinesterase (AChE) and monoamine oxidase B (MAO-B), with remarkable selectivity over butyrylcholinesterase (BChE) and MAO-A, which have been investigated as the enzyme targets related to Alzheimer's disease (AD). The inhibitory activities were evaluated for the pure
Identifiants
pubmed: 35923722
doi: 10.1039/d2md00042c
pii: d2md00042c
pmc: PMC9298480
doi:
Types de publication
Journal Article
Langues
eng
Pagination
873-883Informations de copyright
This journal is © The Royal Society of Chemistry.
Déclaration de conflit d'intérêts
There are no conflicts to declare.
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