Biological evaluation and molecular docking of novel 1,3,4-thiadiazole-resorcinol conjugates as multifunctional cholinesterases inhibitors.
Acetylcholinesterase
/ chemistry
Amyloid beta-Peptides
/ chemistry
Antioxidants
/ chemistry
Binding Sites
Butyrylcholinesterase
/ chemistry
Catalytic Domain
Cell Line
Cell Survival
/ drug effects
Cholinesterase Inhibitors
/ chemistry
Humans
Kinetics
Molecular Docking Simulation
Protein Aggregates
/ drug effects
Resorcinols
/ chemistry
Thiadiazoles
/ chemistry
1,3,4-Thiadiazole
Acetylcholinesterase
Antioxidant
Beta amyloid
Butyrylcholinesterase
Cytotoxicity
Inhibitor
Molecular docking
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
02 2021
02 2021
Historique:
received:
23
07
2020
revised:
24
11
2020
accepted:
28
12
2020
pubmed:
15
1
2021
medline:
9
9
2021
entrez:
14
1
2021
Statut:
ppublish
Résumé
Two series of novel 1,3,4-thiadiazole-resorcinol conjugates were efficiently synthesized and evaluated as cholinesterases inhibitors. N-Butyl- and N-chlorophenyl-5-amino-1,3,4-thiadiazol-2-yl)benzene-1,3-diols were identified as the most promising compounds of low nanomolar activity against AChE (IC
Identifiants
pubmed: 33444983
pii: S0045-2068(20)31915-5
doi: 10.1016/j.bioorg.2020.104617
pii:
doi:
Substances chimiques
Amyloid beta-Peptides
0
Antioxidants
0
Cholinesterase Inhibitors
0
Protein Aggregates
0
Resorcinols
0
Thiadiazoles
0
1,3,4-thiadiazole
14IAC3GH7G
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
104617Informations de copyright
Copyright © 2020. Published by Elsevier Inc.