Exploring 4-substituted-2-thiazolylhydrazones from 2-, 3-, and 4-acetylpyridine as selective and reversible hMAO-B inhibitors
| dc.contributor.author | Chimenti, Paola | |
| dc.contributor.author | Petzer, Anél | |
| dc.contributor.author | Petzer, Jacobus P. | |
| dc.contributor.author | Carradori, Simone | |
| dc.contributor.author | D’Ascenzio, Melissa | |
| dc.contributor.researchID | 12264954 - Petzer, Anél | |
| dc.contributor.researchID | 10727388 - Petzer, Jacobus Petrus | |
| dc.date.accessioned | 2015-05-20T12:52:37Z | |
| dc.date.available | 2015-05-20T12:52:37Z | |
| dc.date.issued | 2013 | |
| dc.description.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. | en_US |
| dc.identifier.citation | 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] | en_US |
| dc.identifier.issn | 0223-5234 | |
| dc.identifier.issn | 1768-3254 (Online) | |
| dc.identifier.uri | http://hdl.handle.net/10394/13844 | |
| dc.identifier.uri | https://www.sciencedirect.com/science/article/pii/S0223523413003413 | |
| dc.identifier.uri | https://doi.org/10.1016/j.ejmech.2013.05.032 | |
| dc.language.iso | en | en_US |
| dc.publisher | Elsevier | en_US |
| dc.subject | Monoamine oxidase | en_US |
| dc.subject | Acetylpyridine | en_US |
| dc.subject | Reversibility | en_US |
| dc.subject | Molecular modelling | en_US |
| dc.subject | Thiazole | en_US |
| dc.title | Exploring 4-substituted-2-thiazolylhydrazones from 2-, 3-, and 4-acetylpyridine as selective and reversible hMAO-B inhibitors | en_US |
| dc.type | Article | en_US |