Exploring 4-substituted-2-thiazolylhydrazones from 2-, 3-, and 4-acetylpyridine as selective and reversible hMAO-B inhibitors
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Elsevier
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.
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Chimenti, P. et al. 2013. Exploring 4-substituted-2-thiazolylhydrazones from 2-, 3-, and 4-acetylpyridine as selective and reversible hMAO-B inhibitors. European journal of medicinal chemistry, 66:221-227. [https://doi.org/10.1016/j.ejmech.2013.05.032]