Synthesis and Biological Activity of Some Benzochromenoquinolinones: Tacrine Analogs as Potent Anti-Alzheimer's Agents.
Acetylcholinesterase
/ metabolism
Alzheimer Disease
/ drug therapy
Amyloid beta-Peptides
/ antagonists & inhibitors
Animals
Antioxidants
/ chemical synthesis
Biphenyl Compounds
/ antagonists & inhibitors
Butyrylcholinesterase
/ metabolism
Cholinesterase Inhibitors
/ chemical synthesis
Dose-Response Relationship, Drug
Electrophorus
Horses
Kinetics
Molecular Docking Simulation
Molecular Structure
Neurons
/ drug effects
Neuroprotective Agents
/ chemical synthesis
PC12 Cells
Peptide Fragments
/ antagonists & inhibitors
Picrates
/ antagonists & inhibitors
Quinolones
/ chemical synthesis
Rats
Structure-Activity Relationship
Alzheimer's disease
BACE1
benzochromenoquinolinones
cholinesterase
docking study
inhibitors
neuroprotective activity
tacrine
Journal
Chemistry & biodiversity
ISSN: 1612-1880
Titre abrégé: Chem Biodivers
Pays: Switzerland
ID NLM: 101197449
Informations de publication
Date de publication:
Apr 2019
Apr 2019
Historique:
received:
20
09
2018
accepted:
04
02
2019
pubmed:
6
2
2019
medline:
29
5
2019
entrez:
6
2
2019
Statut:
ppublish
Résumé
Alzheimer's disease (AD) is a well-known neurodegenerative disorder affecting millions of old people worldwide and the corresponding epidemiological data emphasize the importance of the disease. As AD is a multifactorial illness, various single target directed drugs that have reached clinical trials have failed. Therefore, various factors associated with outset of AD have been considered in targeted drug discovery. In this work, various benzochromenoquinolinones were synthesized and evaluated for their cholinesterase and BACE1 inhibitory activities as well as neuroprotective and metal-chelating properties. Among the synthesized compounds, 14-amino-13-(3-nitrophenyl)-2,3,4,13-tetrahydro-1H-benzo[6,7]chromeno[2,3-b]quinoline-7,12-dione (6m) depicted the best inhibitory activity toward acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with IC
Identifiants
pubmed: 30720917
doi: 10.1002/cbdv.201800488
doi:
Substances chimiques
Amyloid beta-Peptides
0
Antioxidants
0
Biphenyl Compounds
0
Cholinesterase Inhibitors
0
Neuroprotective Agents
0
Peptide Fragments
0
Picrates
0
Quinolones
0
amyloid beta-protein (23-35)
0
1,1-diphenyl-2-picrylhydrazyl
DFD3H4VGDH
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
e1800488Subventions
Organisme : Research Council of Tehran University of Medical Sciences
ID : 95-03-96-33001
Informations de copyright
© 2019 Wiley-VHCA AG, Zurich, Switzerland.