Investigating 1,2,3,4,5,6-hexahydroazepino[4,3-b]indole as scaffold of butyrylcholinesterase-selective inhibitors with additional neuroprotective activities for Alzheimer's disease.
Amyloid beta-Peptides
/ metabolism
Azepines
/ chemical synthesis
Butyrylcholinesterase
/ chemistry
Catalytic Domain
Cell Line, Tumor
Cholinesterase Inhibitors
/ chemical synthesis
Dose-Response Relationship, Drug
Drug Design
Free Radical Scavengers
/ chemical synthesis
Humans
Indoles
/ chemical synthesis
Molecular Docking Simulation
Molecular Structure
Neuroprotective Agents
/ chemical synthesis
Peptide Fragments
/ metabolism
Protein Binding
/ drug effects
Protein Multimerization
/ drug effects
Structure-Activity Relationship
Acetylcholinesterase
Alzheimer's disease
Amyloid-β aggregation
Azepino[4,3-b]indole
Butyrylcholinesterase
Neuroprotection
Journal
European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510
Informations de publication
Date de publication:
01 Sep 2019
01 Sep 2019
Historique:
received:
09
03
2019
revised:
13
05
2019
accepted:
23
05
2019
pubmed:
4
6
2019
medline:
26
7
2019
entrez:
4
6
2019
Statut:
ppublish
Résumé
Due to the role of butyrylcholinesterase (BChE) in acetylcholine hydrolysis in the late stages of the Alzheimer's disease (AD), inhibitors of butyrylcholinesterase (BChE) have been recently envisaged, besides acetylcholinesterase (AChE) inhibitors, as candidates for treating mild-to-moderate AD. Herein, synthesis and AChE/BChE inhibition activity of some twenty derivatives of 1,2,3,4,5,6-hexahydroazepino[4,3-b]indole (HHAI) is reported. Most of the newly synthesized HHAI derivatives achieved the inhibition of both ChE isoforms with IC
Identifiants
pubmed: 31158754
pii: S0223-5234(19)30479-9
doi: 10.1016/j.ejmech.2019.05.062
pii:
doi:
Substances chimiques
Amyloid beta-Peptides
0
Azepines
0
Cholinesterase Inhibitors
0
Free Radical Scavengers
0
Indoles
0
Neuroprotective Agents
0
Peptide Fragments
0
amyloid beta-protein (1-40)
0
amyloid beta-protein (1-42)
0
Butyrylcholinesterase
EC 3.1.1.8
Types de publication
Journal Article
Langues
eng
Pagination
414-424Informations de copyright
Copyright © 2019 Elsevier Masson SAS. All rights reserved.