Dimethoxyindoles based thiosemicarbazones as multi-target agents; synthesis, crystal interactions, biological activity and molecular modeling.
Antioxidant
Cholinesterase inhibitor
Dimethoxyindoles
Molecular modelling
Thiosemicarbazones
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
03 2022
03 2022
Historique:
received:
19
08
2021
revised:
05
01
2022
accepted:
25
01
2022
pubmed:
6
2
2022
medline:
14
6
2022
entrez:
5
2
2022
Statut:
ppublish
Résumé
Alzheimer's disease (AD) is known as one of the most devastating neurodegenerative disease diagnosed for the old-aged people and cholinesterase inhibitors (ChEI) can be used as an effective palliative treatment for AD. A range of novel monomeric and dimeric indole based thiosemicarbazone derivatives 17-28 was synthesized in order to target cholinesterases (ChE). Biological importance of the targeted compounds 17-28 was investigated by employing the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes along with three different antioxidant property determination assays, namely DPPH free radical scavenging, ABTS cationic radical decolarization, and CUPRAC cupric reducing antioxidant capacity. The compounds 18 and 19 displayed the best inhibitor activity against BChE with IC
Identifiants
pubmed: 35121556
pii: S0045-2068(22)00052-9
doi: 10.1016/j.bioorg.2022.105647
pii:
doi:
Substances chimiques
Antioxidants
0
Cholinesterase Inhibitors
0
Thiosemicarbazones
0
Acetylcholinesterase
EC 3.1.1.7
Butyrylcholinesterase
EC 3.1.1.8
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
105647Informations de copyright
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