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    Exploring 4-substituted-2-thiazolylhydrazones from 2-, 3-, and 4-acetylpyridine as selective and reversible hMAO-B inhibitors

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    Date
    2013
    Author
    Chimenti, Paola
    Petzer, Anél
    Petzer, Jacobus P.
    Carradori, Simone
    D’Ascenzio, Melissa
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    Abstract
    A series of 4-substituted-2-thiazolylhydrazone derivatives have been synthesized and tested in vitro for their human monoamine oxidase (hMAO) A and B inhibitory activity. Our findings confirmed that the substitution at C4 of the thiazole ring was important to obtain highly potent and selective hMAO-B inhibitors with IC50 values in the nanomolar range. Moreover, these derivatives were endowed with a reversible mechanism of enzyme inhibition. Molecular modelling studies were performed to rationalize the recognition of all inhibitors with respect to hMAO-A and -B isoforms.
    URI
    http://hdl.handle.net/10394/13844
    https://www.sciencedirect.com/science/article/pii/S0223523413003413
    https://doi.org/10.1016/j.ejmech.2013.05.032
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