Design, synthesis, and antidiabetic activity of new furan-clubbed 1,2,3-triazole derivatives as α -glucosidase inhibitors
Year: 2026
Type: article
Abstract: Aim The study aims to design, synthesize, and evaluate novel furan-clubbed 1,2,3-triazole derivatives as potential α-glucosidase inhibitors for the management of diabetes mellitus.Materials and methods Ten furan-clubbed-1,2,3-triazole derivatives PD(1–10) were synthesized and characterized through sophisticated instrumentation techniques, including FT-IR, 1H NMR, 13C NMR, and LC-MS. The compounds were assessed in vitro for their ability to inhibit the α-glucosidase enzyme. The in vivo antidiabetic effect of the best molecules was evaluated using STZ-nicotinamide induced diabetic mouse model. The observed results were further supported by molecular docking against α-glucosidase (PDB ID: 3L4U) and histopathological examinationsResults The results of in vitro studies showed that the test compound PD-10 exhibited the strongest α-glucosidase inhibition (IC50 = 13.82 μM), outperforming acarbose (IC50 = 32.03 μM), followed by PD-1 and PD-6. Further, the in vivo antidiabetic evaluation of the best compounds adjudged compound PD-10 as the best molecule among the series. Docking analyses indicated a significant binding affinity of PD-10 (−4.34 kcal/mol).Conclusions The research highlights PD-10 as a promising α-glucosidase inhibitor with strong in vitro and in vivo antidiabetic effects, supported by favorable molecular docking interactions, and emphasizes its potential for development as an antidiabetic lead for further studies and evaluations.
Source: Future Medicinal Chemistry
Institution: Indo Soviet Friendship College of Pharmacy
Language: English
Subfield: Endocrinology, Diabetes and Metabolism
Field: Medicine
Domain: Health Sciences
Open Access status: green
Award: G3817326202
OpenAlex ID: W7154718014