دورية أكاديمية
Synthesis, in vitro inhibitory activity, kinetic study and molecular docking of novel N-alkyl–deoxynojirimycin derivatives as potential α-glucosidase inhibitors
| العنوان: | Synthesis, in vitro inhibitory activity, kinetic study and molecular docking of novel N-alkyl–deoxynojirimycin derivatives as potential α-glucosidase inhibitors |
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| المؤلفون: | Ping Lin, Jia-Cheng Zeng, Ji-Guang Chen, Xu-Liang Nie, En Yuan, Xiao-Qiang Wang, Da-Yong Peng, Zhong-Ping Yin |
| المصدر: | Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 35, Iss 1, Pp 1879-1890 (2020) |
| بيانات النشر: | Taylor & Francis Group, 2020. |
| سنة النشر: | 2020 |
| المجموعة: | LCC:Therapeutics. Pharmacology |
| مصطلحات موضوعية: | 1-deoxynojirimycin derivatives, α-glucosidase, inhibitor, structure–activity relationship, docking study, Therapeutics. Pharmacology, RM1-950 |
| الوصف: | A series of novel N-alkyl-1-deoxynojirimycin derivatives 25 ∼ 44 were synthesised and evaluated for their in vitro α-glucosidase inhibitory activity to develop α-glucosidase inhibitors with high activity. All twenty compounds exhibited α-glucosidase inhibitory activity with IC50 values ranging from 30.0 ± 0.6 µM to 2000 µM as compared to standard acarbose (IC50 = 822.0 ± 1.5 µM). The most active compound 43 was ∼27-fold more active than acarbose. Kinetic study revealed that compounds 43, 40, and 34 were all competitive inhibitors on α-glucosidase with Ki of 10 µM, 52 µM, and 150 µM, respectively. Molecular docking demonstrated that the high active inhibitors interacted with α-glucosidase by four types of interactions, including hydrogen bonds, π–π stacking interactions, hydrophobic interactions, and electrostatic interaction. Among all the interactions, the π–π stacking interaction and hydrogen bond played a significant role in a various range of activities of the compounds. |
| نوع الوثيقة: | article |
| وصف الملف: | electronic resource |
| اللغة: | English |
| تدمد: | 1475-6366 1475-6374 14756366 |
| العلاقة: | https://doaj.org/toc/1475-6366Test; https://doaj.org/toc/1475-6374Test |
| DOI: | 10.1080/14756366.2020.1826941 |
| الوصول الحر: | https://doaj.org/article/3ca7608a036348e0a87d91e7c3d39694Test |
| رقم الانضمام: | edsdoj.3ca7608a036348e0a87d91e7c3d39694 |
| قاعدة البيانات: | Directory of Open Access Journals |
Full Text Finder | تدمد: | 14756366 14756374 |
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| DOI: | 10.1080/14756366.2020.1826941 |