Anticholinesterase activity of ß-carboline-1, 3, 5-triazine hybrids
Braz. J. Pharm. Sci. (Online)
;
58: e19958, 2022. tab, graf
Article
Dans Anglais
| LILACS
| ID: biblio-1383955
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
Texte intégral:
Disponible
Indice:
LILAS (Amériques)
Sujet Principal:
Triazines
/
Techniques in vitro
langue:
Anglais
Texte intégral:
Braz. J. Pharm. Sci. (Online)
Thème du journal:
Farmacologia
/
Teraputica
/
Toxicologia
Année:
2022
Type:
Article
Pays d'affiliation:
Brésil
Institution/Pays d'affiliation:
Federal Technological University of Paraná/BR
/
State University of Maringá/BR
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