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    Design, synthesis and biochemical evaluation of novel multi-target inhibitors as potential anti-Parkinson agents

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    Date
    2018
    Author
    Carradori, Simone
    Petzer, Anél
    Petzer, Jacobus P.
    Ortuso, Francesco
    Bagetta, Donatella
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    Abstract
    New 4-(3-nitrophenyl)thiazol-2-ylhydrazone derivatives are proposed as dual-target-directed monoamine oxidase B (MAO-B) and acetylcholinesterase (AChE) inhibitors, as well as antioxidant agents, for the treatment of neurodegenerative disorders such as Parkinson's disease. Rational molecular design, target recognition and predicted pharmacokinetic properties have been evaluated by means of molecular modelling. Based on these properties, compounds were synthesized and evaluated in vitro as MAO-B and AChE inhibitors, and compared to the activities at their corresponding isozymes, monoamine oxidase A (MAO-A) and butyrylcholinesterase (BuChE), respectively. Anti-oxidant properties, potentially useful in the treatment of neurodegenerative disorders, have been also investigated in vitro. Among the evaluated compounds, three inhibitors may be considered as promising dual inhibitors of MAO-B and AChE, in vitro. MAO-B inhibition was also shown to be competitive and reversible for compound 19
    URI
    http://hdl.handle.net/10394/26436
    https://www.sciencedirect.com/science/article/pii/S0223523417308528
    https://doi.org/10.1016/j.ejmech.2017.10.050
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