Discovery of Hydrazine Clubbed Thiazoles as Potential Antidiabetic Agents: Synthesis, Biological Evaluation, and Molecular Docking Studies

Kaya B., Tahtacı H., ÇİFTCİ B., Duran H. E., Necip A., IŞIK M., ...Daha Fazla

Drug Development Research, cilt.86, sa.1, 2025 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 86 Sayı: 1
  • Basım Tarihi: 2025
  • Doi Numarası: 10.1002/ddr.70060
  • Dergi Adı: Drug Development Research
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier, BIOSIS, Biotechnology Research Abstracts, CAB Abstracts, Chemical Abstracts Core, EMBASE, International Pharmaceutical Abstracts, Veterinary Science Database
  • Anahtar Kelimeler: ADME, aldose reductase, alpha-amylase, alpha-glucosidase, antidiabetic, molecular docking, thiazole
  • Bilecik Şeyh Edebali Üniversitesi Adresli: Evet

Özet

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.