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Synthesis, In vitro α-Glucosidase Inhibitory Potential and Molecular Docking Studies of 2-Amino-1,3,4-Oxadiazole Derivatives

Author(s):

Hayat Ullah, Fazal Rahim*, Muhammad Taha, Raffaqat Hussain, Abdul Wadood, Mohsan Nawaz, Zainul Wahab, Kanwal and Khalid Mohammed Khan   Pages 1 - 11 ( 11 )

Abstract:


Background: In the recent past, we had 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.

Method: 1,3,4-Oxadiazole derivatives (1-14) have been synthesized and characterized by different spectroscopic techniques such as 1H-, 13C-NMR and HREI-MS.

Result: 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 values 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.

Keywords:

Synthesis, 1, 3, 4-oxadiazole, ?-glucosidase, in viro, SAR, molecular docking study

Affiliation:

Department of Chemistry, Hazara University, Mansehra-21300, Department of Chemistry, Hazara University, Mansehra-21300, Department of Clinical Pharmacy, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box 31441, Dammam, Department of Chemistry, Hazara University, Mansehra-21300, Department of Biochemistry, Abdul Wali Khan University Mardan, Mardan-23200, Department of Chemistry, Hazara University, Mansehra-21300, Department of Conservation Sciences, Hazara University, Mansehra-21300, H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270



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