Benzo[b]tiophen-3-ol derivatives as effective inhibitors of human monoamine oxidase: design, synthesis, and biological activity

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Küçük Resim

Tarih

2019

Dergi Başlığı

Dergi ISSN

Cilt Başlığı

Yayıncı

TAYLOR & FRANCIS LTD

Erişim Hakkı

info:eu-repo/semantics/openAccess

Özet

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.

Açıklama

Anahtar Kelimeler

MAO-B inhibitors, Benzothiophene, Molecular modelling, Rat cortex synaptosomes, Antioxidant activity, Parkinson's disease

Kaynak

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

WoS Q Değeri

Q1

Scopus Q Değeri

Q1

Cilt

34

Sayı

1

Künye

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.