Design and synthesis of novel quinazolinone-1,2,3-triazole hybrids as new anti-diabetic agents: In vitro α-glucosidase inhibition, kinetic, and docking study.
Bioorg Chem
; 83: 161-169, 2019 03.
Article
en En
| MEDLINE
| ID: mdl-30366316
ABSTRACT
A novel series of quinazolinone-1,2,3-triazole hybrids 10a-p were designed, synthesized, and evaluated for their in vitro α-glucosidase inhibitory activity leading to efficient anti-diabetic agents. All synthesized compounds exhibited good inhibitory activity against yeast α-glucosidase (IC50 values in the range of 181.0-474.5⯵M) even much more potent than standard drug acarbose (IC50â¯=â¯750.0). Among them, quinazolinone-1,2,3-triazoles possessing 4-bromobenzyl moiety connected to 1,2,3-triazole ring (10g and 10p) demonstrated the most potent inhibitory activity towards α-glucosidase. Compound 10g inhibited α-glucosidase in a competitive manner with Ki value of 117⯵M. Furthermore, the binding modes of the most potent compounds 10g and 10p in the α-glucosidase active site was studied through in silico docking studies. Also, lack of cytotoxicity of compounds 10g and 10p was confirmed via MTT assay.
Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Triazoles
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Alfa-Glucosidasas
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Quinazolinonas
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Simulación del Acoplamiento Molecular
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Inhibidores de Glicósido Hidrolasas
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Hipoglucemiantes
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Antineoplásicos
Límite:
Humans
Idioma:
En
Revista:
Bioorg Chem
Año:
2019
Tipo del documento:
Article
País de afiliación:
Irán