Artículo
N-1,2,3-triazole-isatin derivatives for cholinesterase and β-amyloid aggregation inhibition: A comprehensive bioassay study
Autor/es | Marques, Carolina S.
López López, Óscar Bagetta, Donatella Carreiro, Elisabete P. Petralla, Sabrina Bartolini, Manuela Hoffmann, Matthias Alcaro, Stefano Monti, Barbara Bolognesi, Maria Laura Decker, Michael Fernández-Bolaños Guzmán, José María Burke, Anthony J. |
Departamento | Universidad de Sevilla. Departamento de Química orgánica |
Fecha de publicación | 2020-05 |
Fecha de depósito | 2024-02-05 |
Publicado en |
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Resumen | 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 ... 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 acetylcholinesterase (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 molecules gave better inhibitions for hBuChE than eqBuChE. For greater insights into their mode of action, molecular 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 outgrowth experiments led to the conclusion that these compounds are only weakly neurotoxic. |
Agencias financiadoras | Fundação para a Ciência e a Tecnologia (FCT) Ministerio de Economía y Competitividad (MINECO). España Junta de Andalucía Deutsche Forschungsgemeinschaft / German Research Foundation (DFG) |
Identificador del proyecto | Pest-OE/QUI/UI0619/2019
CTQ2016-78703-P FQM134 DFG DE 1546/6-3 |
Cita | Marques, C.S., López López, Ó., Bagetta, D., Carreiro, E.P., Petralla, S., Bartolini, M.,...,Burke, A.J. (2020). N-1,2,3-triazole-isatin derivatives for cholinesterase and β-amyloid aggregation inhibition: A comprehensive bioassay study. Bioorganic Chemistry, 98, 103753. https://doi.org/10.1016/j.bioorg.2020.103753. |
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