Selective Pseudo-irreversible Butyrylcholinesterase Inhibitors Transferring Antioxidant Moieties to the Enzyme Show Pronounced Neuroprotective Efficacy In Vitro and In Vivo in an Alzheimer's Disease Mouse Model.
Acetylcholinesterase
/ metabolism
Alzheimer Disease
/ drug therapy
Animals
Antioxidants
/ chemical synthesis
Biphenyl Compounds
/ antagonists & inhibitors
Butyrylcholinesterase
/ deficiency
Cell Survival
/ drug effects
Cells, Cultured
Cholinesterase Inhibitors
/ chemical synthesis
Chromans
/ chemical synthesis
Cinnamates
/ chemical synthesis
Disease Models, Animal
Dose-Response Relationship, Drug
Humans
Male
Melatonin
/ chemical synthesis
Mice
Molecular Structure
Neuroprotective Agents
/ chemical synthesis
Picrates
/ antagonists & inhibitors
Structure-Activity Relationship
Journal
Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531
Informations de publication
Date de publication:
08 07 2021
08 07 2021
Historique:
pubmed:
22
6
2021
medline:
8
9
2021
entrez:
21
6
2021
Statut:
ppublish
Résumé
A series of multitarget-directed ligands (MTDLs) was designed by functionalizing a pseudo-irreversible butyrylcholinesterase (BChE) inhibitor. The obtained hybrids were investigated in vitro regarding their
Identifiants
pubmed: 34152756
doi: 10.1021/acs.jmedchem.1c00534
doi:
Substances chimiques
Antioxidants
0
Biphenyl Compounds
0
Cholinesterase Inhibitors
0
Chromans
0
Cinnamates
0
Neuroprotective Agents
0
Picrates
0
cinnamic acid
140-10-3
1,1-diphenyl-2-picrylhydrazyl
DFD3H4VGDH
Acetylcholinesterase
EC 3.1.1.7
Butyrylcholinesterase
EC 3.1.1.8
Melatonin
JL5DK93RCL
6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid
S18UL9710X
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM