Synthesis, in vitro evaluation and molecular docking studies of thiazole derivatives as new inhibitors of α-glucosidase.
Bioorg Chem
; 62: 15-21, 2015 Oct.
Article
em En
| MEDLINE
| ID: mdl-26162519
ABSTRACT
A series of thiazole derivatives 1-21 were prepared, characterized by EI-MS and (1)H NMR and evaluated for α-glucosidase inhibitory potential. All twenty one derivatives showed good α-glucosidase inhibitory activity with IC50 value ranging between 18.23±0.03 and 424.41±0.94µM when compared with the standard acarbose (IC50, 38.25±0.12µM). Compound (8) (IC50, 18.23±0.03µM) and compound (7) (IC50=36.75±0.05µM) exhibited outstanding inhibitory potential much better than the standard acarbose (IC50, 38.25±0.12µM). All other analogs also showed good to moderate enzyme inhibition. Molecular docking studies were carried out in order to find the binding affinity of thiazole derivatives with enzyme. Studies showed these thiazole analogs as a new class of α-glucosidase inhibitors.
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Base de dados:
MEDLINE
Assunto principal:
Fenóis
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Tiazóis
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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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Hidrazinas
Idioma:
En
Ano de publicação:
2015
Tipo de documento:
Article