Preparation of Novel 3,4,5-Triaryl-1,2,4-Oxadiazole Derivatives: Molecular Docking and Α-Glucosidase Assessment

Preparation of Novel 3,4,5-Triaryl-1,2,4-Oxadiazole Derivatives: Molecular Docking and Α-Glucosidase Assessment Publisher

Roustaei S¹ ; Saeedian Moghadam E² ; Faramarzi MA³ ; Amini M^{2, 4}

Show Affiliations

1. Department of Radiopharmacy, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, 1417614411, Iran
2. Drug Design and Development Research Center, The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, Tehran, 1417614411, Iran
3. Department of Pharmaceutical Biotechnology, Faculty of Pharmacy and Biotechnology Research Center, Tehran University of Medical Sciences, Tehran, 1417614411, Iran
4. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, 1417614411, Iran

Source: ChemistrySelect Published:2024

Abstract

Diabetes mellitus (DM) has become a growing health problem, across all globe. Many factors have contributed into this issue, among them inappropriate lifestyle, unhealthy eating habits and growing spiritual/mental concerns are to be rated higher. Likewise much research needed to be diverted in progress for treatment of DM. Herein, we report synthesis and antidiabetic activity evaluation of ten novel phenolic derivatives of triaryl-1,2,4-oxadiazole 7 a–j. The compounds have synthesized using multistep reactions in acceptable purity and yields. Final step was done using 1,3-dipolar cycloaddition reaction between various Schiff bases and arylnitrile oxides. 7 a–j were characterized by spectroscopic methods (1H NMR, 13C NMR, MS and IR) and their purities were confirmed using elemental analysis. All 7 a–j were evaluated for their α-Glucosidase inhibitory activity. All compounds showed higher activity in inhibiting the enzyme, in comparison to standard, acarbose. Compounds 7 e and 7 g exerted the best activity with the IC50 value of 193.6 and 222.0 μM respectively. Furthermore, enzyme kinetic study approach was adopted to judge the effect of 7 e on enzyme inhibition. Finally, docking simulations revealed the possible mode of interactions between 7 e and 7 g and enzyme active sites. Final conclusion of results showed that oxadiazole scaffold/s are a potential antidiabetic target. © 2024 Wiley-VCH GmbH.

Style	Citing Format
MLA	Roustaei S, et al.. "Preparation of Novel 3,4,5-Triaryl-1,2,4-Oxadiazole Derivatives: Molecular Docking and Α-Glucosidase Assessment." ChemistrySelect, vol. 9, no. 6, 2024, pp. -.
APA	Roustaei S, Saeedian Moghadam E, Faramarzi MA, Amini M (2024). Preparation of Novel 3,4,5-Triaryl-1,2,4-Oxadiazole Derivatives: Molecular Docking and Α-Glucosidase Assessment. ChemistrySelect, 9(6), -.
Chicago	Roustaei S, Saeedian Moghadam E, Faramarzi MA, Amini M. "Preparation of Novel 3,4,5-Triaryl-1,2,4-Oxadiazole Derivatives: Molecular Docking and Α-Glucosidase Assessment." ChemistrySelect 9, no. 6 (2024): -.
Harvard	Roustaei S et al. (2024) 'Preparation of Novel 3,4,5-Triaryl-1,2,4-Oxadiazole Derivatives: Molecular Docking and Α-Glucosidase Assessment', ChemistrySelect, 9(6), pp. -.
Vancouver	Roustaei S, Saeedian Moghadam E, Faramarzi MA, Amini M. Preparation of Novel 3,4,5-Triaryl-1,2,4-Oxadiazole Derivatives: Molecular Docking and Α-Glucosidase Assessment. ChemistrySelect. 2024;9(6):-.
BibTex	@article{ author = {Roustaei S and Saeedian Moghadam E and Faramarzi MA and Amini M}, title = {Preparation of Novel 3,4,5-Triaryl-1,2,4-Oxadiazole Derivatives: Molecular Docking and Α-Glucosidase Assessment}, journal = {ChemistrySelect}, volume = {9}, number = {6}, pages = {-}, year = {2024} }
RIS	TY - JOUR AU - Roustaei S AU - Saeedian Moghadam E AU - Faramarzi MA AU - Amini M TI - Preparation of Novel 3,4,5-Triaryl-1,2,4-Oxadiazole Derivatives: Molecular Docking and Α-Glucosidase Assessment JO - ChemistrySelect VL - 9 IS - 6 SP - EP - PY - 2024 ER -

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