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Title: N-1,2,3-triazole-isatin derivatives for cholinesterase and β-amyloid aggregation inhibition: A comprehensive bioassay study
Authors: Marques, Carolina S.
López, Óscar
Bagetta, Donatella
Carreiro, Elisabete P.
Petralla, Sabrina
Bartolini, Manuela
Hoffmann, Matthias
Alcaro, Stefano
Monti, Barbara
Bolognesi, Maria Laura
Decker, Michael
Fernández-Bolaños, José
Burke, Anthony J.
Keywords: isatin
β-amyloid inhibition
Issue Date: 10-Mar-2020
Publisher: Elsevier Inc.
Abstract: Our goal was the evaluation of a series of N-1,2,3-triazole-isatin derivatives for multi-target activity which included cholinesterase (ChE) inhibition and β-amyloid (Aβ) peptide anti-aggregation. The compounds have shown considerable promise as butyrylcholinesterase (BuChE) inhibitors. Although the inhibition of eel acet- ylcholinesterase (eeAChE) was weak, the inhibitions against equine BuChE (eqBuChE) and human BuChE (hBuChE) were more significant with a best inhibition against eqBuChE of 0.46 μM. In some cases, these mo- lecules gave better inhibitions for hBuChE than eqBuChE. For greater insights into their mode of action, mole- cular docking studies were carried out, followed by STD-NMR validation. In addition, some of these compounds showed weak Aβ anti-aggregation activity. Hepatotoxicity studies showed that they were non-hepatoxic and neurotoxicity studies using neurite out- growth experiments led to the conclusion that these compounds are only weakly neurotoxic.
Type: article
Appears in Collections:LAVQ-REQUIMTE - Publicações - Artigos em Revistas Internacionais Com Arbitragem Científica

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