biostudies-literatureWang Lthe Henan Science and Technology ProgramInnovative Research Team of the Active Ingredients and Efficacy Correlation Evaluation System with Dabie Mountain Traditional Chinese Medicine in Xinyang Agriculture and Forestry UniversityXinyang Agriculture and Forestry University Youth Fund ProjectHenan Science and Technology ProgramXinyang Agriculture and Forestry University National Research Project Cultivation Fund ProjectNatural Science Foundation of Henan5062https://www.ebi.ac.uk/biostudies/studies/S-EPMC11547804biostudies-literatureUnknown29(21)1-deoxynojirimycin (DNJ) is a well-known α-glucosidase inhibitor. A series of phenyltriazole-deoxynojirimycin hybrids containing C4 and C6 (4 and 6 methylenes, respectively) linkers were synthesized. These novel compounds were assessed for preliminary glucosidase inhibition and cytotoxicity tests in vitro. Among them, compounds 12-14 and 16-20 (IC50: 105 ± 9-11 ± 1 μM) were more active than deoxynojirimycin (DNJ, IC50 = 155 ± 15 μM). The kinetics of enzyme inhibition measured by using Lineweaver-Burk plots indicated that compounds 18 and 19 were competitive inhibitors. In addition, a molecular docking study of α-glucosidase revealed that the interaction modes and the orientations of compound 18 andMolecules (Basel, Switzerland)Synthesis and Evaluation of Phenyltriazole-Deoxynojirimycin Hybrids as Potent α-Glucosidase Inhibitors.PMC11547804242102320266No. QN2022021 and No. QN2022023pyjj20230101XNKJTD-008No. 242102320266 and No. 232102320294QN2022023232300420065No. pyjj20230101No.232300420065QN2022021232102320294Zhu NGuo LGuo XLuo WBai XZhao YWang LfalseSynthesis and Evaluation of Phenyltriazole-Deoxynojirimycin Hybrids as Potent α-Glucosidase Inhibitors.1-deoxynojirimycin (DNJ) is a well-known α-glucosidase inhibitor. A series of phenyltriazole-deoxynojirimycin hybrids containing C4 and C6 (4 and 6 methylenes, respectively) linkers were synthesized. These novel compounds were assessed for preliminary glucosidase inhibition and cytotoxicity tests in vitro. Among them, compounds 12-14 and 16-20 (IC50: 105 ± 9-11 ± 1 μM) were more active than deoxynojirimycin (DNJ, IC50 = 155 ± 15 μM). The kinetics of enzyme inhibition measured by using Lineweaver-Burk plots indicated that compounds 18 and 19 were competitive inhibitors. In addition, a molecular docking study of α-glucosidase revealed that the interaction modes and the orientations of compound 18 and2024-01-01T00:00:00Z2024 Oct2026-04-08T19:46:26.383Z2025-04-19T17:30:19.507ZS-EPMC115478043951970510.3390/molecules29215062