New Quinoline Analogues: As Potential Diabetics Inhibitors and Molecular Docking Study
| Autor: | Muhammad Taha, Mohammed Salahuddin, Fazal Rahim, Syahrul Imran, Shafqat Hussain, Nizam Uddin, Khalid Mohammed Khan |
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| Rok vydání: | 2023 |
| Předmět: | |
| Zdroj: | Polycyclic Aromatic Compounds. :1-23 |
| ISSN: | 1563-5333 1040-6638 |
| Popis: | The 7-quinolinyl bearing 1,3,4-thiadiazole-2-amine analogues were synthesized (1–17) and based on the literature these analog were screened in vitro for their α-amylase and α-glucosidase inhibitory profile. All analogues showed moderate to good inhibitory potentials ranging between 0.80 ± 0.05 µM to 40.20 ± 0.70 µM and 1.20 ± 0.10 µM to 43.30 ± 0.80 µM against α-amylase and α-glucosidase. Among the series, analogues 2 (IC50 = 2.10 ± 0.10 µM), (IC50 = 2.40 ± 0.10 µM), 3 (IC50 = 0.80 ± 0.05 µM), (IC50 = 1.20 ± 0.10 µM) and 4 (IC50 = 1.50 ± 0.10 µM), (IC50 = 1.90 ± 0.10 µM) with flouro substitution at phenyl ring of the 1,3,4-thiadiazole ring were identified to be the most potent inhibitors against α-amylase and α-glucosidase enzymes. The structure of all the newly synthetics analogues were confirmed by using different types of spectroscopic techniques such as HREI-MS, 1H- and 13C-NMR spectroscopy. To find structure-activity relationship, molecular docking studies were carry out to understand the binding mode of active inhibitors with active site of enzymes and results supported the experimental data. Due to the most potent inhibitory activity of analogue 4 among all the synthesized compound, it was screened against streptozotocin induced diabetic animal model. |
| Databáze: | OpenAIRE |
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