期刊
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
卷 34, 期 1, 页码 1511-1525出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756366.2019.1653864
关键词
MAO-B inhibitors; benzothiophene; molecular modelling; rat cortex synaptosomes; antioxidant activity; Parkinson's disease
资金
- Progetto di Ricerca Ateneo La Sapienza (Italy) [2014-C26A14AC5L]
- POR FESR LAZIO 2014/2020 - REGIONE LAZIO - Avviso pubblico LIFE 2020
- National Research Foundation of South Africa [85642, 96180]
A series of benzo[b]thiophen-3-ols were synthesised and investigated as potential human monoamine oxidase (hMAO) inhibitors in vitro as well as ex vivo in rat cortex synaptosomes by means of evaluation of 3,4-dihydroxyphenylacetic acid/dopamine (DOPAC/DA) ratio and lactate dehydrogenase (LDH) activity. Most of these compounds possessed high selectivity for the MAO-B isoform and a discrete antioxidant and chelating potential. Molecular docking studies of all the compounds underscored potential binding site interactions suitable for MAO inhibition activity, and suggested structural requirements to further improve the activity of this scaffold by chemical modification of the aryl substituents. Starting from this heterocyclic nucleus, novel lead compounds for the treatment of neurodegenerative disease could be developed.
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