| Autor: |
Davood Rezapour Niri, Mohammad Hosein Sayahi, Somayeh Behrouz, Ali Moazzam, Somayeh Mojtabavi, Mohammad Ali Faramarzi, Bagher Larijani, Hossein Rastegar, Maryam Mohammadi-Khanaposhtani, Mohammad Mahdavi |
| Jazyk: |
angličtina |
| Rok vydání: |
2022 |
| Předmět: |
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| Zdroj: |
BMC Chemistry, Vol 16, Iss 1, Pp 1-10 (2022) |
| Druh dokumentu: |
article |
| ISSN: |
2661-801X |
| DOI: |
10.1186/s13065-022-00882-2 |
| Popis: |
Abstract Background A series of coumarin-indole hybrids was synthesized as the new α-glucosidase inhibitors. The title hybrids were considered as α-glucosidase inhibitors because had two active pharmacophores against α-glucosidase: coumarin and indole. Methods The thirteen various derivatives 4a–m were synthesized, purified, and fully characterized. These compounds were evaluated against α-glucosidase in vitro and in silico. In silico pharmacokinetic studies of the most potent compounds were also performed. Results Most of the title compounds exhibited high anti-α-glucosidase activity in comparison to standard drug acarbose. In particular, the phenoxy derivative 4d namely 3-((1H-indol-3-yl)(3-phenoxyphenyl)methyl)-4-hydroxy-2H-chromen-2-one showed promising activity. This compound is a competitive inhibitor against α-glucosidase and showed the lowest binding energy at the α-glucosidase active site in comparison to other potent synthesized compounds and acarbose. Conclusion Compound 4d can be a lead compound for further structural development to obtain effective and potent α-glucosidase inhibitors. |
| Databáze: |
Directory of Open Access Journals |
| Externí odkaz: |
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