AI Article Synopsis
- Researchers synthesized various derivatives of oxadiazoles to investigate their potential as α-glucosidase inhibitors, continuing their exploration of heterocyclic compounds.
- The synthesized 1,3,4-oxadiazole derivatives were characterized using techniques like NMR and mass spectrometry and were found to have varying levels of α-glucosidase inhibitory activity.
- Among the tested compounds, most showed good inhibition compared to the standard acarbose, with compound 14 demonstrating the strongest activity (IC50 = 0.80 ± 0.1 μM) while compound 7 was less effective (IC50 = 45.1 ± 1.7 μM); molecular docking studies further elucidated the interactions between the active compounds
Article Abstract
Background: In the recent past, we have synthesized and reported different derivatives of oxadiazoles as potential α-glucosidase inhibitors, keeping in mind, the pharmacological aspects of oxadiazole moiety and in continuation of our ongoing research on the chemistry and bioactivity of new heterocyclic compounds.
Methods: 1,3,4-Oxadiazole derivatives (1-14) have been synthesized and characterized by different spectroscopic techniques such as 1H-, 13C-NMR and HREI-MS.
Results: The synthetic derivatives were screened for α-glucosidase inhibitory potential. All compounds exhibited good inhibitory activity with IC50 values ranging between 0.80 ± 0.1 to 45.1 ± 1.7 μM in comparison with the standard acarbose having IC50 value 38.45 ± 0.80 μM.
Conclusion: Thirteen compounds 1-6 and 8-14 showed potential inhibitory activity as compared to the standard acarbose having IC50 value 38.45 ± 0.80 μM, however, only one compound 7 (IC50 = 45.1 ± 1.7 μM) was found to be less active. Compound 14 (IC50 = 0.80 ± 0.1 μM) showed promising inhibitory activity among all synthetic derivatives. Molecular docking studies were also conducted for the active compounds to understand the ligand-enzyme binding interactions.
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| http://dx.doi.org/10.2174/1573406415666190612150447 | DOI Listing |
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