Article detail · 2025
Discovery of Hydrazine Clubbed Thiazoles as Potential Antidiabetic Agents: Synthesis, Biological Evaluation, and Molecular Docking Studies
- Year
- 2025
- ISSN
0272-4391- Type
- article
Data source split
- YÖKSİS YÖKSİS article record
- OpenAlex OpenAlex enrichment (abstract, citations, topics)
Abstract
English (OpenAlex)
ABSTRACT In this study, hydrazine clubbed thiazole derivatives (3a–3j) were obtained by Hantzsch thiazole synthesis and characterized by MS, 1H NMR, and 13C NMR. The inhibitory potentials of the derivatives against diabetes‐related enzymes such as aldose reductase (AR), α‐glycosidase (α‐GLY), and α‐amylase (α‐AMY) were experimentally determined, and the results were supported by molecular docking. The results showed that the derivatives (3a–3j) displayed varied degree of potential inhibitory activity, with KI values covering the following ranges: 5.47 ± 0.53 to 23.89 ± 1.46 nM for AR and 1.76 ± 0.01 to 24.81 ± 0.15 μM for α‐GLY, and with IC50 values 4.94–28.17 μM for α‐AMY, as compared to standard epalrestat and acarbose (KI: 34.53 ± 2.52 nM for AR and 23.53 ± 2.72 μM for α‐GLY, respectively). The selective activity of these derivatives on antidiabetic enzymes may be important for the treatment of diabetes and may lead to the development of alternative new compounds for this purpose.
Topics
- Enzyme function and inhibition
- Click Chemistry and Applications
- Aldose Reductase and Taurine
Primary topic Enzyme function and inhibition