Synthesis and biological evaluation of 1,6-bis-triazole-2,3,4-tri-O-benzyl-α-d-glucopyranosides as a novel α-glucosidase inhibitor in the treatment of Type 2 diabetes.
Bioorg Med Chem Lett
; 50: 128331, 2021 10 15.
Article
en En
| MEDLINE
| ID: mdl-34418573
ABSTRACT
A novel series of 1,6-bis-triazole-benzyl-α-glucoside derivatives (7a-7ee) were designed, synthesized and evaluated for inhibitory activity against α-glucosidase. Most of the synthesized compounds exhibited good activity with IC50 ranging from 3.73 µM to 53.34 µM and are more potent than the standard drug acarbose (IC50 = 146.25 ± 0.40 µM). SARs study showed the ester and menthol moiety play an important role in the inhibitory activity. The molecular docking model of the potent compounds 7f, 7z, 7cc and 7dd showed good binding energy and interacts well with amino acid residues around the active site of the enzyme, which confirmed the in vitro activity results.
Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Diabetes Mellitus Tipo 2
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Inhibidores de Glicósido Hidrolasas
/
Glucanos
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Hipoglucemiantes
Límite:
Humans
Idioma:
En
Año:
2021
Tipo del documento:
Article