Synthesis, in-vitro evaluation, molecular docking, and kinetic studies of pyridazine-triazole hybrid system as novel α-glucosidase inhibitors.
Binding Sites
Cell Line
Drug Design
Glycoside Hydrolase Inhibitors
/ chemistry
Humans
Models, Molecular
Molecular Structure
Protein Binding
Protein Conformation
Pyridazines
/ chemistry
Saccharomyces cerevisiae
/ enzymology
Structure-Activity Relationship
Triazoles
/ chemistry
alpha-Glucosidases
/ metabolism
Anti-diabetic drug
Click reaction
Pyridazine
Triazole
α-Glucosidase inhibitor
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
04 2021
04 2021
Historique:
received:
12
07
2020
revised:
18
01
2021
accepted:
20
01
2021
pubmed:
16
2
2021
medline:
9
10
2021
entrez:
15
2
2021
Statut:
ppublish
Résumé
In this study, we reported the discovery of pyridazine based 1,2,3-triazole derivatives as inhibitors of α-glucosidase. All target compounds exhibited significant inhibitory activities against yeast and rat α-glucosidase enzymes compared to positive control, acarbose. The most potent compound 6j, ethyl 3-(2-(1-(4-nitrobenzyl)-1H-1,2,3-triazol-4-yl)ethyl)-5,6-diphenylpyridazine-4-carboxylate exhibited IC
Identifiants
pubmed: 33588241
pii: S0045-2068(21)00046-8
doi: 10.1016/j.bioorg.2021.104670
pii:
doi:
Substances chimiques
Glycoside Hydrolase Inhibitors
0
Pyridazines
0
Triazoles
0
alpha-Glucosidases
EC 3.2.1.20
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
104670Informations de copyright
Copyright © 2021 Elsevier Inc. All rights reserved.