Synthesis and evaluation of catecholamine derivatives as amyloid-beta aggregation inhibitors.
Bioorg Med Chem Lett
; 107: 129788, 2024 Jul 15.
Article
in En
| MEDLINE
| ID: mdl-38740144
ABSTRACT
Effectively inhibition of amyloid ß (Aß) aggregation is considered an important method for treatment of the Alzheimer's disease. Herein, inspired by the ability of trans-clovamide to effectively inhibit Aß aggregation, we synthesized a series of structurally related catecholamine derivatives and tested them as Aß aggregation inhibitors using the Thioflavin T assay. The results show that they demonstrated a higher inhibitory rate against Aß aggregation. Furthermore, these compounds exhibited high water solubilities and low cytotoxicities. Additionally, transmission electron microscopy images and dynamic light scattering of their Aß aggregations were observed. Docking simulations revealed that the catechol moiety of the synthesized compounds can form hydrogen bonds with the key regions of Aß and thereby inhibit Aß aggregation.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Catecholamines
/
Amyloid beta-Peptides
/
Molecular Docking Simulation
/
Protein Aggregates
Limits:
Humans
Language:
En
Journal:
Bioorg Med Chem Lett
/
Bioorg. med. chem. lett
/
Bioorganic & medicinal chemistry letters
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2024
Document type:
Article
Affiliation country:
Japón
Country of publication:
Reino Unido