(2019) New thiosemicarbazide-1,2,3-triazole hybrids as potent α-glucosidase inhibitors: Design, synthesis, and biological evaluation. Journal of Molecular Structure. pp. 192-200. ISSN 00222860 (ISSN)
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Abstract
A new series of thiosemicarbazide-1,2,3-triazole hybrids 10a-o has been synthesized, characterized by 1 H NMR, 13 C NMR, and screened for their in vitro α-glucosidase inhibitory activity. All of the synthesized compounds displayed excellent α-glucosidase inhibitory activity with IC 50 values in the range of 75.0 ± 0.5 to 253.0 ± 0.5 μM, as compared to the standard drug acarbose (IC 50 = 750.0 ± 1.5 μM). Among the synthesized compounds, compound 10h (IC 50 = 75.0 ± 0.5)with 4-methoxy group at phenyl part of thiosemicarbazide moiety and 2,6-dichloro substituents at benzyl moiety was found to be the most potent compound. Kinetic analysis revealed that compound 10h is a competitive inhibitor for α-glucosidase. Docking study of compound 10h in the active site of α-glucosidase showed that this compound interacted with residues His239, His279, Glu304, Gly306, and Arg312. © 2019 Elsevier B.V.
| Item Type: | Article |
|---|---|
| Keywords: | 1,2,3-Triazole Molecular docking Thiosemicarbazide α-Glucosidase inhibitor Molecular structure Alpha glucosidase Biological evaluation Glucosidase inhibitors Inhibitory activity Potent compounds Thiosemicarbazides Structure (composition) |
| Subjects: | QV Pharmacology |
| Divisions: | Faculty of Pharmacy and Pharmaceutical Sciences > گروه شیمی دارویی |
| Page Range: | pp. 192-200 |
| Journal or Publication Title: | Journal of Molecular Structure |
| Journal Index: | Scopus |
| Volume: | 1192 |
| Identification Number: | https://doi.org/10.1016/j.molstruc.2019.04.082 |
| ISSN: | 00222860 (ISSN) |
| Depositing User: | Zahra Otroj |
| URI: | http://eprints.mui.ac.ir/id/eprint/10772 |
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