Tryptophan-derived butyrylcholinesterase inhibitors as promising leads against Alzheimer's disease.
Alzheimer Disease
/ drug therapy
Butyrylcholinesterase
/ metabolism
Cell Line, Tumor
Cell Survival
/ drug effects
Cholinesterase Inhibitors
/ chemical synthesis
Crystallography, X-Ray
Dose-Response Relationship, Drug
Humans
Models, Molecular
Molecular Structure
Structure-Activity Relationship
Tryptophan
/ chemistry
Journal
Chemical communications (Cambridge, England)
ISSN: 1364-548X
Titre abrégé: Chem Commun (Camb)
Pays: England
ID NLM: 9610838
Informations de publication
Date de publication:
26 Mar 2019
26 Mar 2019
Historique:
pubmed:
14
3
2019
medline:
11
4
2019
entrez:
14
3
2019
Statut:
ppublish
Résumé
We have identified tryptophan-based selective nanomolar butyrylcholinesterase (BChE) inhibitors. They are defined according to their chemical modularity, novel binding mode revealed by five solved crystal structures with human BChE, low cytotoxicity, and predicted permeability of the blood-brain barrier. Altogether, these factors indicate their potential as unique lead compounds for symptomatic therapy against Alzheimer's disease.
Substances chimiques
Cholinesterase Inhibitors
0
Tryptophan
8DUH1N11BX
Butyrylcholinesterase
EC 3.1.1.8
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM