Synthesis, in vitro alpha-glucosidase inhibitory potential of benzimidazole bearing bis-Schiff bases and their molecular docking study.
Bioorg Chem
; 94: 103394, 2020 01.
Article
en En
| MEDLINE
| ID: mdl-31699396
ABSTRACT
Voglibose and acarbose are distinguished α-glucosidase inhibitors used for controlling of diabetes mellitus. Unfortunately, these distinguished and clinically used inhibitors have also numerous side effects. Subsequently, there is still needed to develop safer therapy. Despite of a broad spectrum of biological importance of benzimidazole, it is occasionally evaluated for α-glucosidase activity. Current study deals with the synthesis and biological screening of benzimidazole bearing bis-Schiff bases (1-19) for their α-glucosidase inhibitory activity. All analogues exhibited excellent to good inhibitory potential (IC50â¯=â¯2.20⯱â¯0.1to 88.60⯱â¯1.70⯵M) when compared with standard drug acarbose (IC50â¯=â¯38.45⯱â¯0.80⯵M). A structure activity relationship has been established on the basis of electronic effects and position of different substituents present on phenyl ring. In order to rationalize the binding interactions of most active analogues with the active site of α-glucosidase enzyme, molecular docking study was conducted.
Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Bencimidazoles
/
Alfa-Glucosidasas
/
Simulación del Acoplamiento Molecular
/
Inhibidores de Glicósido Hidrolasas
Límite:
Humans
Idioma:
En
Revista:
Bioorg Chem
Año:
2020
Tipo del documento:
Article