Biscoumarin-1,2,3-triazole hybrids as novel anti-diabetic agents: Design, synthesis, in vitro α-glucosidase inhibition, kinetic, and docking studies.
Bioorg Chem
; 92: 103206, 2019 11.
Article
em En
| MEDLINE
| ID: mdl-31445191
ABSTRACT
A novel series of biscoumarin-1,2,3-triazole hybrids 6a-n was prepared and evaluated for α-glucosidase inhibitory potential. All fourteen derivatives exhibited excellent α-glucosidase inhibitory activity with IC50 values ranging between 13.0⯱â¯1.5 and 75.5⯱â¯7.0⯵M when compared with the acarbose as standard inhibitor (IC50â¯=â¯750.0⯱â¯12.0⯵M). Among the synthesized compounds, compounds 6c (IC50â¯=â¯13.0⯱â¯1.5⯵M) and 6g (IC50â¯=â¯16.4⯱â¯1.7⯵M) exhibited the highest inhibitory activity against α-glucosidase and were non-cytotoxic towards normal fibroblast cells. Kinetic study revealed that compound 6c inhibits the α-glucosidase in a competitive mode. Furthermore, molecular docking investigation was performed to find interaction modes of the biscoumarin-1,2,3-triazole derivatives.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Triazóis
/
Cumarínicos
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Alfa-Glucosidases
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Simulação de Acoplamento Molecular
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Inibidores de Glicosídeo Hidrolases
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Hipoglicemiantes
Limite:
Humans
/
Infant
Idioma:
En
Revista:
Bioorg Chem
Ano de publicação:
2019
Tipo de documento:
Article
País de afiliação:
Irã