Synthesis and Bioactivities Evaluation of Quinazolin-4(3H)-One Derivatives As Α-Glucosidase Inhibitors

Synthesis and Bioactivities Evaluation of Quinazolin-4(3H)-One Derivatives As Α-Glucosidase Inhibitors Publisher

Moheb M¹ ; Iraji A^{2, 3} ; Dastyafteh N⁴ ; Khalili Ghomi M⁴ ; Noori M⁴ ; Mojtabavi S⁵ ; Faramarzi MA⁵ ; Rasekh F⁶ ; Larijani B¹ ; Zomorodian K⁷ ; Sadatebrahimi SE¹ ; Mahdavi M⁴

Show Affiliations

1. Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran
2. Stem Cells Technology Research Center, Shiraz University of Medical Sciences, Shiraz, Iran
3. Central Research Laboratory, Shiraz University of Medical Sciences, Shiraz, Iran
4. Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran
5. Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
6. Department of Biology, Payame Noor University (PNU), Tehran, Iran
7. Department of Medical Mycology and Parasitology, School of Medicine, Shiraz University of Medical Sciences, Shiraz, Iran

Source: BMC Chemistry Published:2022

Abstract

The development of new antidiabetes agents is necessary to obtain optimal glycemic control and overcome its complications. Different quinazolin-4(3H)-one bearing phenoxy-acetamide derivatives (7a–r) were designed and synthesized to develop α-glucosidase inhibitors. All the synthesized derivatives were evaluated against α-glucosidase in vitro and among them, compound 7b showed the highest α-glucosidase inhibition with an IC50 of 14.4 µM, which was ∼53 times stronger than that of acarbose. The inhibition kinetic studies showed that the inhibitory mechanism of compound 7b was a competitive type towards α-glucosidase. Also, molecular docking studies analyzed the interaction between the most potent derivative and α-glucosidase. Current findings indicate the new potential of quinazolin-4(3H)-ones that could be used for the development of novel agents against diabetes mellitus. © 2022, The Author(s).

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Somayeh Mojtabavi (15)

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Style	Citing Format
MLA	Moheb M, et al.. "Synthesis and Bioactivities Evaluation of Quinazolin-4(3H)-One Derivatives As Α-Glucosidase Inhibitors." BMC Chemistry, vol. 16, no. 1, 2022, pp. -.
APA	Moheb M, Iraji A, Dastyafteh N, Khalili Ghomi M, Noori M, Mojtabavi S, Faramarzi MA, Rasekh F, Larijani B, Zomorodian K, Sadatebrahimi SE, Mahdavi M (2022). Synthesis and Bioactivities Evaluation of Quinazolin-4(3H)-One Derivatives As Α-Glucosidase Inhibitors. BMC Chemistry, 16(1), -.
Chicago	Moheb M, Iraji A, Dastyafteh N, Khalili Ghomi M, Noori M, Mojtabavi S, Faramarzi MA, et al.. "Synthesis and Bioactivities Evaluation of Quinazolin-4(3H)-One Derivatives As Α-Glucosidase Inhibitors." BMC Chemistry 16, no. 1 (2022): -.
Harvard	Moheb M et al. (2022) 'Synthesis and Bioactivities Evaluation of Quinazolin-4(3H)-One Derivatives As Α-Glucosidase Inhibitors', BMC Chemistry, 16(1), pp. -.
Vancouver	Moheb M, Iraji A, Dastyafteh N, Khalili Ghomi M, Noori M, Mojtabavi S, et al.. Synthesis and Bioactivities Evaluation of Quinazolin-4(3H)-One Derivatives As Α-Glucosidase Inhibitors. BMC Chemistry. 2022;16(1):-.
BibTex	@article{ author = {Moheb M and Iraji A and Dastyafteh N and Khalili Ghomi M and Noori M and Mojtabavi S and Faramarzi MA and Rasekh F and Larijani B and Zomorodian K and Sadatebrahimi SE and Mahdavi M}, title = {Synthesis and Bioactivities Evaluation of Quinazolin-4(3H)-One Derivatives As Α-Glucosidase Inhibitors}, journal = {BMC Chemistry}, volume = {16}, number = {1}, pages = {-}, year = {2022} }
RIS	TY - JOUR AU - Moheb M AU - Iraji A AU - Dastyafteh N AU - Khalili Ghomi M AU - Noori M AU - Mojtabavi S AU - Faramarzi MA AU - Rasekh F AU - Larijani B AU - Zomorodian K AU - Sadatebrahimi SE AU - Mahdavi M TI - Synthesis and Bioactivities Evaluation of Quinazolin-4(3H)-One Derivatives As Α-Glucosidase Inhibitors JO - BMC Chemistry VL - 16 IS - 1 SP - EP - PY - 2022 ER -

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