Dual targeting of acetylcholinesterase and tau aggregation: Design, synthesis and evaluation of multifunctional deoxyvasicinone analogues for Alzheimer's disease.
Acetylcholinesterase
/ metabolism
Alzheimer Disease
/ drug therapy
Cholinesterase Inhibitors
/ chemical synthesis
Dose-Response Relationship, Drug
Drug Design
Humans
Molecular Structure
Neuroprotective Agents
/ chemical synthesis
Protein Aggregates
/ drug effects
Quinazolines
/ chemical synthesis
Structure-Activity Relationship
tau Proteins
/ antagonists & inhibitors
Acetylcholinesterase
Alzheimer’s disease
Deoxyvasicinone derivatives
Tau aggregation
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
11 2021
11 2021
Historique:
received:
29
05
2021
revised:
18
08
2021
accepted:
08
09
2021
pubmed:
26
9
2021
medline:
5
1
2022
entrez:
25
9
2021
Statut:
ppublish
Résumé
Development of multitargeted ligands have demonstrated remarkable efficiency as potential therapeutics for Alzheimer's disease (AD). Herein, we reported a new series of deoxyvasicinone analogues as dual inhibitor of acetylcholinesterase (AChE) and tau aggregation that function as multitargeted ligands for AD. All the multitargeted ligands 11(a-j) and 15(a-g) were designed, synthesized, and validated by
Identifiants
pubmed: 34562674
pii: S0045-2068(21)00731-8
doi: 10.1016/j.bioorg.2021.105354
pii:
doi:
Substances chimiques
Cholinesterase Inhibitors
0
Neuroprotective Agents
0
Protein Aggregates
0
Quinazolines
0
tau Proteins
0
2,3-trimethylene-4-quinazolone
530-53-0
Acetylcholinesterase
EC 3.1.1.7
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
105354Informations de copyright
Copyright © 2021 Elsevier Inc. All rights reserved.