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

• Published in: Polycyclic 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
• Language: English
• Published: Philadelphia Taylor & Francis 21.10.2023; Taylor & Francis Ltd
• Subjects: 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
• ISSN: 1040-6638; 1563-5333
• DOI: 10.1080/10406638.2022.2149561

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.