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



Moheb M1 ; Iraji A2, 3 ; Dastyafteh N4 ; Khalili Ghomi M4 ; Noori M4 ; Mojtabavi S5 ; Faramarzi MA5 ; Rasekh F6 ; Larijani B1 ; Zomorodian K7 ; Sadatebrahimi SE1 ; Mahdavi M4
Authors

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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