Novel multi target-directed ligands targeting 5-HT
Alzheimer Disease
/ drug therapy
Animals
Antioxidants
/ chemical synthesis
Biphenyl Compounds
/ antagonists & inhibitors
COS Cells
Cell Line, Tumor
Cell Proliferation
/ drug effects
Cell Survival
/ drug effects
Chlorocebus aethiops
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Humans
Ligands
Molecular Structure
Picrates
/ antagonists & inhibitors
Reactive Oxygen Species
/ analysis
Receptors, Serotonin, 5-HT4
/ metabolism
Serotonin 5-HT4 Receptor Agonists
/ chemical synthesis
Structure-Activity Relationship
5-HT(4) receptor
Alzheimer's disease
Antioxidant
MTDL
Phenol
Journal
European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510
Informations de publication
Date de publication:
15 Nov 2019
15 Nov 2019
Historique:
received:
31
05
2019
revised:
19
07
2019
accepted:
05
08
2019
pubmed:
17
8
2019
medline:
22
11
2019
entrez:
17
8
2019
Statut:
ppublish
Résumé
Facing the complexity of Alzheimer's disease (AD), it is now currently admitted that a therapeutic pleiotropic intervention is needed to alter its progression. Among the major hallmarks of the disease, the amyloid pathology and the oxidative stress are closely related. We propose in this study to develop original Multi-Target Directed Ligands (MTDL) able to impact at the same time Aβ protein accumulation and toxicity of Reactive Oxygen Species (ROS) in neuronal cells. Such MTDL were obtained by linking on a central piperidine two scaffolds of interest: a typical aminochlorobenzophenone present in numerous 5-HT
Identifiants
pubmed: 31419776
pii: S0223-5234(19)30730-5
doi: 10.1016/j.ejmech.2019.111596
pii:
doi:
Substances chimiques
Antioxidants
0
Biphenyl Compounds
0
Ligands
0
Picrates
0
Reactive Oxygen Species
0
Serotonin 5-HT4 Receptor Agonists
0
Receptors, Serotonin, 5-HT4
158165-40-3
1,1-diphenyl-2-picrylhydrazyl
DFD3H4VGDH
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
111596Informations de copyright
Copyright © 2019 Elsevier Masson SAS. All rights reserved.