Benzo[b]tiophen-3-ol derivatives as effective inhibitors of human monoamine oxidase: design, synthesis, and biological activity
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Date
2019
Journal Title
Journal ISSN
Volume Title
Publisher
TAYLOR & FRANCIS LTD
Access Rights
info:eu-repo/semantics/openAccess
Abstract
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.
Description
Keywords
MAO-B inhibitors, Benzothiophene, Molecular modelling, Rat cortex synaptosomes, Antioxidant activity, Parkinson's disease
Journal or Series
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
WoS Q Value
Q1
Scopus Q Value
Q1
Volume
34
Issue
1
Citation
Guglielmi, P., Secci, D., Petzer, A., Bagetta, D., Chimenti, P., Rotondi, G., Ferrante, C., Recinella, L.,Leone, S., Alcaro, S., Zengin, G., Petzer, J. P., Ortuso, F., Carradori, S. (2019). Benzo [b] Tiophen-3-ol Derivatives as Effective Inhibitors of Human Monoamine Oxidase: Design, Synthesis, and Biological Activity. Journal of Enzyme Inhibition and Medicinal Chemistry, 34(1), 1511-1525.
