Exploring antidiabetic potential of adamantyl-thiosemicarbazones via aldose reductase (ALR2) inhibition.
Adamantane
/ chemistry
Aldehyde Reductase
/ antagonists & inhibitors
Chromatography, Thin Layer
Dose-Response Relationship, Drug
Hypoglycemic Agents
/ chemical synthesis
Inhibitory Concentration 50
Magnetic Resonance Spectroscopy
Molecular Docking Simulation
Molecular Structure
Protein Binding
Thiosemicarbazones
/ chemical synthesis
Adamantyl methyl ketone
Adamantyl-thiosemicarbazone
Aldose reductase (ALR2)
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
11 2019
11 2019
Historique:
received:
17
06
2019
revised:
05
08
2019
accepted:
01
09
2019
pubmed:
22
9
2019
medline:
23
10
2020
entrez:
22
9
2019
Statut:
ppublish
Résumé
The role of aldose reductase (ALR2) in diabetes mellitus is well-established. Our interest in finding ALR2 inhibitors led us to explore the inhibitory potential of new thiosemicarbazones. In this study, we have synthesized adamantyl-thiosemicarbazones and screened them as aldehyde reductase (ALR1) and aldose reductase (ALR2) inhibitors. The compounds bearing phenyl 3a, 2-methylphenyl 3g and 2,6-dimethylphenyl 3m have been identified as most potent ALR2 inhibitors with IC
Identifiants
pubmed: 31541804
pii: S0045-2068(19)30975-7
doi: 10.1016/j.bioorg.2019.103244
pii:
doi:
Substances chimiques
Hypoglycemic Agents
0
Thiosemicarbazones
0
AKR1B1 protein, human
EC 1.1.1.21
Aldehyde Reductase
EC 1.1.1.21
Adamantane
PJY633525U
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
103244Informations de copyright
Copyright © 2019 Elsevier Inc. All rights reserved.