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Synthesis and bioactivities evaluation of quinazolin-4(3H)-one derivatives as α-glucosidase inhibitors.

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.

SUBMITTER: Moheb M

PROVIDER: S-EPMC9667588 | biostudies-literature | 2022 Nov

REPOSITORIES: biostudies-literature

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Synthesis and bioactivities evaluation of quinazolin-4(3H)-one derivatives as α-glucosidase inhibitors.

Moheb Mahshid M Iraji Aida A Dastyafteh Navid N Khalili Ghomi Minoo M Noori Milad M Mojtabavi Somayeh S Faramarzi Mohammad Ali MA Rasekh Fatemeh F Larijani Bagher B Zomorodian Kamiar K Sadat-Ebrahimi Seyed Esmaeil SE Mahdavi Mohammad M

BMC chemistry 20221115 1

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 IC<sub>50</sub> of 14.4 µM, which was ∼53 times stronger than that of acarbo ...[more]

PMID: 36380337

Dataset Information

Synthesis and bioactivities evaluation of quinazolin-4(3H)-one derivatives as α-glucosidase inhibitors.

Publications

Synthesis and bioactivities evaluation of quinazolin-4(3H)-one derivatives as α-glucosidase inhibitors.

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