Scopus
🔓 Açık Erişim
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 · Ocak 2019
Makale Bilgileri
DergiJournal of Enzyme Inhibition and Medicinal Chemistry
Yayın TarihiOcak 2019
Cilt / Sayfa34 · 1511-1525
Scopus ID2-s2.0-85071029361
Erişim🔓 Açık Erişim
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.
Yazarlar (14)
1
Paolo Guglielmi
2
Daniela Secci
3
Anél Petzer
4
Donatella Bagetta
5
Paola Chimenti
6
Giulia Rotondi
7
Claudio Ferrante
8
Lucia Recinella
9
Sheila Leone
10
Stefano Alcaro
ORCID: 0000-0002-0437-358X
11
Gokhan Zengin
ORCID: 0000-0001-6548-7823
12
Jacobus P. Petzer
13
Francesco Ortuso
ORCID: 0000-0001-6235-8161
14
Simone Carradori
Anahtar Kelimeler
antioxidant activity
benzothiophene
MAO-B inhibitors
molecular modelling
Parkinson’s disease
rat cortex synaptosomes
Kurumlar
North-West University
Potchefstroom South Africa
Sapienza Università di Roma
Rome Italy
Selçuk Üniversitesi
Selçuklu Turkey
Università degli studi Magna Graecia di Catanzaro
Catanzaro Italy
University of G. d'Annunzio Chieti and Pescara
Chieti Italy
Metrikler
18
Atıf
14
Yazar
6
Anahtar Kelime