Synthesis of Novel Azabenzimidazole Bridged bis-Coumarin Compounds, Investigation of Pancreatic Lipase Inhibitory Properties, and Docking Studies

Russian Journal of Bioorganic Chemistry(2023)

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摘要
In this study, new azabenzimidazole-bridged bis-coumarin compounds have been synthesized and screened for their pancreatic lipase inhibitory properties. All compounds showed a considerable lipase inhibitory potential with IC 50 values ranging from 0.67 ± 0.047 to 3.15 ±0.081 µM. Compound N ʹ ,N ʹʹ-[(6-bromo-2-oxo-1 H imidazo[4,5- b ]pyridine-1,3-diyl)bis(1-oxoethane-2,1-diyl)]bis(8-methyl-2-oxo-2 H -chromene-3-carbohydrazide) ( IIIe ) having methoxy group on coumarin ring and compound N',N'' -[(6-bromo-2-oxo-1 H -imidazo[4,5- b ]pyridine-1,3-diyl)bis(1-oxoethane-2,1-diyl)]bis(6-chloro-2-oxo-2 H -chromene-3-carbohydrazide) ( IIIb ) having –Cl atom on coumarin ring have the highest inhibitory effects. A molecular docking study was performed on the binding pose and affinity of synthesized compounds at the binding sites of lipase.
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关键词
azabenzimidazole,bis-coumarin,lipase inhibition,docking study
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