2. Academic Validation
  3. N-1,2,3-triazole-isatin derivatives for cholinesterase and β-amyloid aggregation inhibition: A comprehensive bioassay study

N-1,2,3-triazole-isatin derivatives for cholinesterase and β-amyloid aggregation inhibition: A comprehensive bioassay study

  • Bioorg Chem. 2020 May;98:103753. doi: 10.1016/j.bioorg.2020.103753.
Carolina S Marques 1,  Óscar López 2,  Donatella Bagetta 3,  Elisabete P Carreiro 1,  Sabrina Petralla 4,  Manuela Bartolini 4,  Matthias Hoffmann 5,  Stefano Alcaro 6,  Barbara Monti 4,  Maria Laura Bolognesi 4,  Michael Decker 5,  José G Fernández-Bolaños 2,  Anthony J Burke 7
Affiliations

Affiliations

  • 1 LAQV-REQUIMTE, University of Évora, Institute for Research and Advanced Studies, Rua Romão Ramalho, 59, 7000 Évora, Portugal.
  • 2 Departamento de Química Orgánica, Facultad de Química, Universidad de Sevilla, Apartado 1203, E-41071 Seville, Spain.
  • 3 Net4Science Academic Spin-Off, University "Magna Græcia" of Catanzaro, Campus Universitario "S.Venuta", Catanzaro, Italy.
  • 4 Department of Pharmacy and Biotechnology, Alma Mater Studiorum, University of Bologna, via Belmeloro 6/via Selmi 3, 40126 Bologna, Italy.
  • 5 Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy and Food Chemistry, Julius Maximilian University Würzburg, Am Hubland, D-97074 Würzburg, Germany.
  • 6 Net4Science Academic Spin-Off, University "Magna Græcia" of Catanzaro, Campus Universitario "S.Venuta", Catanzaro, Italy; Department of "Scienze della Salute", University "Magna Græcia" of Catanzaro, Campus Universitario "S. Venuta", Catanzaro, Italy.
  • 7 LAQV-REQUIMTE, University of Évora, Institute for Research and Advanced Studies, Rua Romão Ramalho, 59, 7000 Évora, Portugal; Chemistry Department, School of Science and Technology, University of Évora, Rua Romão Ramalho 59, 7000-671 Évora, Portugal. Electronic address: ajb@uevora.pt.
PMID: 32200328 DOI: 10.1016/j.bioorg.2020.103753
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 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.

Keywords

1,2,3-triazole; Butyrylcholinesterase; Hepatotoxicity; Isatin; Neurotoxicity; Oxindole; β-amyloid inhibition.

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