Design and synthesis of new fused carbazole-imidazole derivatives as anti-diabetic agents: In vitro α-glucosidase inhibition, kinetic, and in silico studies.
Bioorg Med Chem Lett
; 29(5): 713-718, 2019 03 01.
Article
en En
| MEDLINE
| ID: mdl-30661823
ABSTRACT
Twenty three fused carbazole-imidazoles 6a-w were designed, synthesized, and screened as new α-glucosidase inhibitors. All the synthesized fused carbazole-imidazoles 6a-w were found to be more active than acarbose (IC50â¯=â¯750.0⯱â¯1.5⯵M) against yeast α-glucosidase with IC50 values in the range of 74.0⯱â¯0.7-298.3⯱â¯0.9⯵M. Kinetic study of the most potent compound 6v demonstrated that this compound is a competitive inhibitor for α-glucosidase (Ki valueâ¯=â¯75⯵M). Furthermore, the in silico studies of the most potent compounds 6v and 6o confirmed that these compounds interacted with the key residues in the active site of α-glucosidase.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Carbazoles
/
Inhibidores de Glicósido Hidrolasas
/
Hipoglucemiantes
/
Imidazoles
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2019
Tipo del documento:
Article