Future medicinal chemistry · 2026
Design, synthesis, and antidiabetic activity of new furan-clubbed 1,2,3-triazole derivatives as α-glucosidase inhibitors.
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Devi Priya, Maity Subhadip, Singh Aastha, Mehan Sidharth, Singh Gurpreet, Asati Vivek
Аннотация
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 examinations.
RESULTS: 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.
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 examinations.
RESULTS: 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.