Design, synthesis and biological evaluation of rasagiline-clorgyline hybrids as novel dual inhibitors of monoamine oxidase-B and amyloid-β aggregation against Alzheimer's disease.
Alzheimer Disease
/ drug therapy
Amyloid beta-Peptides
/ antagonists & inhibitors
Animals
Cell Line, Tumor
Cell Survival
/ drug effects
Clorgyline
/ chemistry
Dose-Response Relationship, Drug
Drug Design
Humans
Indans
/ chemistry
Male
Models, Molecular
Molecular Structure
Monoamine Oxidase
/ metabolism
Monoamine Oxidase Inhibitors
/ chemical synthesis
Neuroprotective Agents
/ chemical synthesis
Peptide Fragments
/ antagonists & inhibitors
Protein Aggregates
/ drug effects
Rats
Rats, Sprague-Dawley
Structure-Activity Relationship
Alzheimer’s disease
Amyloid-β
Monoamine oxidase
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 Sep 2020
15 Sep 2020
Historique:
received:
28
01
2020
revised:
13
04
2020
accepted:
15
05
2020
pubmed:
12
7
2020
medline:
2
4
2021
entrez:
12
7
2020
Statut:
ppublish
Résumé
A series of rasagiline-clorgyline hybrids was designed, synthesized and investigated in vitro for their inhibition of monoamine oxidase and amyloid-β aggregation. Most of compounds were found to be selective and highly potent hMAO-B inhibitors showing IC
Identifiants
pubmed: 32652406
pii: S0223-5234(20)30446-3
doi: 10.1016/j.ejmech.2020.112475
pii:
doi:
Substances chimiques
Amyloid beta-Peptides
0
Indans
0
Monoamine Oxidase Inhibitors
0
Neuroprotective Agents
0
Peptide Fragments
0
Protein Aggregates
0
amyloid beta-protein (1-42)
0
rasagiline
003N66TS6T
Monoamine Oxidase
EC 1.4.3.4
Clorgyline
LYJ16FZU9Q
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
112475Informations de copyright
Copyright © 2020 Elsevier Masson SAS. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of competing interest The authors declare no competing financial interest.