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 in | Polycyclic aromatic compounds Vol. 43; no. 9; pp. 8482 - 8493 |
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Main Authors | , , , , , , , |
Format | Journal Article |
Language | English |
Published |
Philadelphia
Taylor & Francis
21.10.2023
Taylor & Francis Ltd |
Subjects | |
Online Access | Get full text |
ISSN | 1040-6638 1563-5333 |
DOI | 10.1080/10406638.2022.2149561 |
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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. |
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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 |
Author_xml | – sequence: 1 givenname: Youness surname: Boukharsa fullname: Boukharsa, Youness organization: Laboratory of Medicinal Chemistry, Faculty of Medicine and Pharmacy, Mohammed V University of Rabat – sequence: 2 givenname: Khalid orcidid: 0000-0002-8075-8051 surname: Karrouchi fullname: Karrouchi, Khalid organization: Laboratory of Analytical Chemistry and Bromatology, Team of Formulation and Quality Control of Health Products, Faculty of Medicine and Pharmacy, Mohammed V University – sequence: 3 givenname: El Hassane orcidid: 0000-0001-9240-7163 surname: Anouar fullname: Anouar, El Hassane organization: Department of Chemistry, College of Science and Humanities in Al-Kharj, Prince Sattam Bin Abdulaziz University – sequence: 4 givenname: Hanan surname: Albalwi fullname: Albalwi, Hanan organization: Department of Chemistry, College of Science and Humanities in Al-Kharj, Prince Sattam Bin Abdulaziz University – sequence: 5 givenname: Ibtissam surname: Jarbi fullname: Jarbi, Ibtissam organization: Laboratory of Pharmacology and Toxicology, Biopharmaceutical and Toxicological Analysis Research Team, Faculty of Medicine and Pharmacy, Mohammed V University of Rabat – sequence: 6 givenname: Youssef surname: Ramli fullname: Ramli, Youssef organization: Laboratory of Medicinal Chemistry, Faculty of Medicine and Pharmacy, Mohammed V University of Rabat – sequence: 7 givenname: My El Abbes orcidid: 0000-0003-3863-4677 surname: Faouzi fullname: Faouzi, My El Abbes organization: Laboratory of Pharmacology and Toxicology, Biopharmaceutical and Toxicological Analysis Research Team, Faculty of Medicine and Pharmacy, Mohammed V University of Rabat – sequence: 8 givenname: M'hammed surname: Ansar fullname: Ansar, M'hammed organization: Laboratory of Medicinal Chemistry, Faculty of Medicine and Pharmacy, Mohammed V University of Rabat |
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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 |
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