Synthesis, α-Glucosidase and β-Galactosidase Inhibitory Potentials and Molecular Docking of Some Novel Benzofuran-Pyridazine Derivatives

A novel series of benzofuran-pyridazine derivatives have been synthesized and characterized by different spectroscopic techniques including FT-IR, 1 H-NMR, 13 C-NMR, and ESI-MS spectrometry. All synthesized compounds were evaluated in vitro for their antidiabetic activity against α-glucosidase and β...

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Published inPolycyclic aromatic compounds Vol. 43; no. 9; pp. 8482 - 8493
Main Authors Boukharsa, Youness, Karrouchi, Khalid, Anouar, El Hassane, Albalwi, Hanan, Jarbi, Ibtissam, Ramli, Youssef, Faouzi, My El Abbes, Ansar, M'hammed
Format Journal Article
LanguageEnglish
Published Philadelphia Taylor & Francis 21.10.2023
Taylor & Francis Ltd
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ISSN1040-6638
1563-5333
DOI10.1080/10406638.2022.2149561

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Abstract A novel series of benzofuran-pyridazine derivatives have been synthesized and characterized by different spectroscopic techniques including FT-IR, 1 H-NMR, 13 C-NMR, and ESI-MS spectrometry. All synthesized compounds were evaluated in vitro for their antidiabetic activity against α-glucosidase and β-galactosidase enzymes. All derivatives (3a-3h) and (4a-4b) showed a remarkable inhibitory potential greater than 89% against α-glucosidase enzyme compared to standard acarbose (42.50%), and compounds 3 b and 4a exhibited significant inhibitory potential against β-galactosidase enzyme with 50.33% and 57.67% respectively, compared to standard Queretin (52.00%). A molecular docking study was conducted to understand the binding interactions of the compounds with the active site of the α-glucosidase enzyme.
AbstractList A novel series of benzofuran-pyridazine derivatives have been synthesized and characterized by different spectroscopic techniques including FT-IR, 1H-NMR, 13C-NMR, and ESI-MS spectrometry. All synthesized compounds were evaluated in vitro for their antidiabetic activity against α-glucosidase and β-galactosidase enzymes. All derivatives (3a-3h) and (4a-4b) showed a remarkable inhibitory potential greater than 89% against α-glucosidase enzyme compared to standard acarbose (42.50%), and compounds 3 b and 4a exhibited significant inhibitory potential against β-galactosidase enzyme with 50.33% and 57.67% respectively, compared to standard Queretin (52.00%). A molecular docking study was conducted to understand the binding interactions of the compounds with the active site of the α-glucosidase enzyme.
A novel series of benzofuran-pyridazine derivatives have been synthesized and characterized by different spectroscopic techniques including FT-IR, 1 H-NMR, 13 C-NMR, and ESI-MS spectrometry. All synthesized compounds were evaluated in vitro for their antidiabetic activity against α-glucosidase and β-galactosidase enzymes. All derivatives (3a-3h) and (4a-4b) showed a remarkable inhibitory potential greater than 89% against α-glucosidase enzyme compared to standard acarbose (42.50%), and compounds 3 b and 4a exhibited significant inhibitory potential against β-galactosidase enzyme with 50.33% and 57.67% respectively, compared to standard Queretin (52.00%). A molecular docking study was conducted to understand the binding interactions of the compounds with the active site of the α-glucosidase enzyme.
Author Albalwi, Hanan
Jarbi, Ibtissam
Ramli, Youssef
Karrouchi, Khalid
Faouzi, My El Abbes
Boukharsa, Youness
Anouar, El Hassane
Ansar, M'hammed
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Snippet A novel series of benzofuran-pyridazine derivatives have been synthesized and characterized by different spectroscopic techniques including FT-IR, 1 H-NMR, 13...
A novel series of benzofuran-pyridazine derivatives have been synthesized and characterized by different spectroscopic techniques including FT-IR, 1H-NMR,...
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SubjectTerms Acarbose
Benzofuran
Diabetes mellitus
Galactosidase
Glucosidase
Molecular docking
NMR
Nuclear magnetic resonance
pyridazin-3(2H)-one
pyridazin-3(2H)-thione
Pyridazines
Spectrometry
Synthesis
α-Glucosidase
β-Galactosidase
Title Synthesis, α-Glucosidase and β-Galactosidase Inhibitory Potentials and Molecular Docking of Some Novel Benzofuran-Pyridazine Derivatives
URI https://www.tandfonline.com/doi/abs/10.1080/10406638.2022.2149561
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