{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Wang L"],"funding":["the Henan Science and Technology Program","Innovative Research Team of the Active Ingredients and Efficacy Correlation Evaluation System with Dabie Mountain Traditional Chinese Medicine in Xinyang Agriculture and Forestry University","Xinyang Agriculture and Forestry University Youth Fund Project","Henan Science and Technology Program","Xinyang Agriculture and Forestry University National Research Project Cultivation Fund Project","Natural Science Foundation of Henan"],"pagination":["5062"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC11547804"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["29(21)"],"pubmed_abstract":["1-deoxynojirimycin (DNJ) is a well-known α-glucosidase inhibitor. A series of phenyltriazole-deoxynojirimycin hybrids containing C<sub>4</sub> and C<sub>6</sub> (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 <b>12</b>-<b>14</b> and <b>16</b>-<b>20</b> (IC<sub>50</sub>: 105 ± 9-11 ± 1 μM) were more active than deoxynojirimycin (DNJ, IC<sub>50</sub> = 155 ± 15 μM). The kinetics of enzyme inhibition measured by using Lineweaver-Burk plots indicated that compounds <b>18</b> and <b>19</b> were competitive inhibitors. In addition, a molecular docking study of α-glucosidase revealed that the interaction modes and the orientations of compound <b>18</b> and"],"journal":["Molecules (Basel, Switzerland)"],"pubmed_title":["Synthesis and Evaluation of Phenyltriazole-Deoxynojirimycin Hybrids as Potent α-Glucosidase Inhibitors."],"pmcid":["PMC11547804"],"funding_grant_id":["242102320266","No. QN2022021 and No. QN2022023","pyjj20230101","XNKJTD-008","No. 242102320266 and No. 232102320294","QN2022023","232300420065","No. pyjj20230101","No.232300420065","QN2022021","232102320294"],"pubmed_authors":["Zhu N","Guo L","Guo X","Luo W","Bai X","Zhao Y","Wang L"],"additional_accession":[]},"is_claimable":false,"name":"Synthesis and Evaluation of Phenyltriazole-Deoxynojirimycin Hybrids as Potent α-Glucosidase Inhibitors.","description":"1-deoxynojirimycin (DNJ) is a well-known α-glucosidase inhibitor. A series of phenyltriazole-deoxynojirimycin hybrids containing C<sub>4</sub> and C<sub>6</sub> (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 <b>12</b>-<b>14</b> and <b>16</b>-<b>20</b> (IC<sub>50</sub>: 105 ± 9-11 ± 1 μM) were more active than deoxynojirimycin (DNJ, IC<sub>50</sub> = 155 ± 15 μM). The kinetics of enzyme inhibition measured by using Lineweaver-Burk plots indicated that compounds <b>18</b> and <b>19</b> were competitive inhibitors. In addition, a molecular docking study of α-glucosidase revealed that the interaction modes and the orientations of compound <b>18</b> and","dates":{"release":"2024-01-01T00:00:00Z","publication":"2024 Oct","modification":"2026-04-08T19:46:26.383Z","creation":"2025-04-19T17:30:19.507Z"},"accession":"S-EPMC11547804","cross_references":{"pubmed":["39519705"],"doi":["10.3390/molecules29215062"]}}