In Vitro and in Vivo Antidiabetics Study of New Oxadiazole Derivatives Along with Molecular Docking Study.

Autor: Taha, Muhammad, Salahuddin, Mohammed, Almandil, Noor Barak, Farooq, Rai Khalid, Rahim, Fazal, Uddin, Nizam, Nawaz, Muhammad, Alhibshi, Amani H., Anouar, El Hassane, Khan, Khalid Mohammed
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Zdroj: Polycyclic Aromatic Compounds; 2023, Vol. 43 Issue 8, p6911-6926, 16p
Abstrakt: There is an excellent approach to design antidiabetic drugs based on inhibitors of α-glucosidase. These inhibitors control the sugar level in blood of diabetic patients to avoid complications on patient health. In current study we designed a new series of oxadiazole based derivatives (1–20). All synthesized analogues were characterized through 1H-NMR, 13C-NMR, HREI-MS and evaluated against α-glucosidase inhibitory potential and analogues 1, 4, 16, 17, and 19 showed excellent activity ranging 1.10–8.60 μM. The analogues 2, 3, 5, 6, 10, 14, and 18 showed 4 to 2 folds better activities ranging 10.10–21.30 μM than standard drug standard acarbose (IC50 = 38.40 ± 0.80 μM). The analogues 11, 13, and 20 showed activities ranging 34.30–34.60 μM better than standard. The analogues 7, 12, and 15 showed weak activities. The analogues 8 and 9 found completely inactive. The binding interactions of these active derivatives were confirmed through molecular docking. The docked analogues, and the α-glucosidase exhibited negative bending energies. The inhibition of α-glucosidase via tested analogues were thermodynamically favored. Based on these results, analog 1 was evaluated against STZ induced diabetic rats and found potent at a dose of 200 mg/kg. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index
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