3-Aryl Coumarin Derivatives Bearing Aminoalkoxy Moiety as Multi-Target-Directed Ligands against Alzheimer's Disease.
Acetylcholinesterase
/ chemistry
Alzheimer Disease
/ drug therapy
Amyloid beta-Peptides
/ chemistry
Animals
Apoptosis
/ drug effects
Binding Sites
Butyrylcholinesterase
/ chemistry
Catalytic Domain
Cholinesterase Inhibitors
/ chemistry
Coumarins
/ chemistry
Humans
Hydrogen Peroxide
/ toxicity
Inhibitory Concentration 50
Kinetics
Ligands
Molecular Docking Simulation
Neuroprotective Agents
/ chemistry
PC12 Cells
Rats
Structure-Activity Relationship
3-phenylcoumarin
Alzheimer's disease
cholinesterase
neuroprotective activity
synthesis design
β-amyloid
Journal
Chemistry & biodiversity
ISSN: 1612-1880
Titre abrégé: Chem Biodivers
Pays: Switzerland
ID NLM: 101197449
Informations de publication
Date de publication:
May 2019
May 2019
Historique:
received:
26
08
2018
accepted:
25
02
2019
pubmed:
9
4
2019
medline:
1
6
2019
entrez:
9
4
2019
Statut:
ppublish
Résumé
Two series of novel coumarin derivatives, substituted at 3 and 7 positions with aminoalkoxy groups, are synthesized, characterized, and screened. The effect of amine substituents and the length of cross-linker are investigated in acetyl- and butyrylcholinesterase (AChE and BuChE) inhibition. Target compounds show moderate to potent inhibitory activities against AChE and BuChE. 3-(3,4-Dichlorophenyl)-7-[4-(diethylamino)butoxy]-2H-chromen-2-one (4y) is identified as the most potent compound against AChE (IC
Identifiants
pubmed: 30957958
doi: 10.1002/cbdv.201800436
doi:
Substances chimiques
Amyloid beta-Peptides
0
Cholinesterase Inhibitors
0
Coumarins
0
Ligands
0
Neuroprotective Agents
0
Hydrogen Peroxide
BBX060AN9V
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
e1800436Subventions
Organisme : Research Council of Tehran University of Medical Sciences
ID : 34462-45-01-96
Informations de copyright
© 2019 Wiley-VHCA AG, Zurich, Switzerland.