Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 1 de 1
Filtrar
Más filtros










Base de datos
Intervalo de año de publicación
1.
Bioorg Chem ; 109: 104670, 2021 04.
Artículo en Inglés | MEDLINE | ID: mdl-33588241

RESUMEN

In this study, we reported the discovery of pyridazine based 1,2,3-triazole derivatives as inhibitors of α-glucosidase. All target compounds exhibited significant inhibitory activities against yeast and rat α-glucosidase enzymes compared to positive control, acarbose. The most potent compound 6j, ethyl 3-(2-(1-(4-nitrobenzyl)-1H-1,2,3-triazol-4-yl)ethyl)-5,6-diphenylpyridazine-4-carboxylate exhibited IC50 values of 58, and 73 µM. Docking studies indicated the responsibility of hydrophobic and hydrogen bonding interactions in the ligand-enzyme complex stability. The in-vitro safety against the normal cell line was observed by toxicity evaluation of the selected compounds.


Asunto(s)
Piridazinas/farmacología , Triazoles/farmacología , Sitios de Unión , Línea Celular , Diseño de Fármacos , Inhibidores de Glicósido Hidrolasas/química , Humanos , Modelos Moleculares , Estructura Molecular , Unión Proteica , Conformación Proteica , Piridazinas/química , Saccharomyces cerevisiae/enzimología , Relación Estructura-Actividad , Triazoles/química , alfa-Glucosidasas/metabolismo
SELECCIÓN DE REFERENCIAS
DETALLE DE LA BÚSQUEDA
...