Anticholinesterase activity of ß-carboline-1, 3, 5-triazine hybrids
Braz. J. Pharm. Sci. (Online)
; 58: e19958, 2022. tab, graf
Article
in English
| LILACS
| ID: biblio-1383955
Responsible library:
BR40.1
Localization: BR40.1
ABSTRACT
Abstract The ß-carboline-1,3,5-triazine hydrochlorides 8-13 were evaluated in vitro against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). The analysed compounds were selective to BuChE, with IC50 values in the range from 1.0-18.8 µM being obtained. The N-{2-[(4,6-dihydrazinyl-1,3,5-triazin-2-yl)amino]ethyl}-1-phenyl-ß-carboline-3-carboxamide (12) was the most potent compound and kinetic studies indicate that it acts as a competitive inhibitor of BuChE. Molecular docking studies show that 12 strongly interacts with the residues of His438 (residue of the catalytic triad) and Trp82 (residue of catalytic anionic site), confirming that this compound competes with the same binding site of the butyrylthiocholine
Full text:
Available
Collection:
International databases
Database:
LILACS
Main subject:
Triazines
/
In Vitro Techniques
Language:
English
Journal:
Braz. J. Pharm. Sci. (Online)
Journal subject:
Farmacologia
/
Teraputica
/
Toxicologia
Year:
2022
Document type:
Article
Affiliation country:
Brazil
Institution/Affiliation country:
Federal Technological University of Paraná/BR
/
State University of Maringá/BR