Design, synthesis, in vitro, and in silico studies of novel diarylimidazole-1,2,3-triazole hybrids as potent α-glucosidase inhibitors.
Bioorg Med Chem
; 27(23): 115148, 2019 12 01.
Article
em En
| MEDLINE
| ID: mdl-31679980
ABSTRACT
In this work, new derivatives of diarylimidazole-1,2,3-triazole 7a-p were designed, synthesized, and evaluated for their in vitro α-glucosidase inhibitory activity. All compounds showed potent inhibitory activity in the range of IC50â¯=â¯90.4-246.7⯵M comparing with acarbose as the standard drug (IC50â¯=â¯750.0⯵M). Among the synthesized compounds, compounds 7b, 7c, and 7e were approximately 8 times more potent than acarbose. The kinetic study of those compounds indicated that they acted as the competitive inhibitors of α-glucosidase. Molecular docking studies were also carried out for compounds 7b, 7c, and 7e using modeled α-glucosidase to find the interaction modes responsible for the desired inhibitory activity.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Triazóis
/
Inibidores de Glicosídeo Hidrolases
Limite:
Humans
Idioma:
En
Ano de publicação:
2019
Tipo de documento:
Article