| Autor: |
Mahshid Moheb, Aida Iraji, Navid Dastyafteh, Minoo Khalili Ghomi, Milad Noori, Somayeh Mojtabavi, Mohammad Ali Faramarzi, Fatemeh Rasekh, Bagher Larijani, Kamiar Zomorodian, Seyed Esmaeil Sadat-Ebrahimi, Mohammad Mahdavi |
| Jazyk: |
angličtina |
| Rok vydání: |
2022 |
| Předmět: |
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| Zdroj: |
BMC Chemistry, Vol 16, Iss 1, Pp 1-12 (2022) |
| Druh dokumentu: |
article |
| ISSN: |
2661-801X |
| DOI: |
10.1186/s13065-022-00885-z |
| Popis: |
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. |
| Databáze: |
Directory of Open Access Journals |
| Externí odkaz: |
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