Ionic liquid-enabled synthesis,cholinesterase inhibitory activity,and molecular docking study of highly functionalized tetrasubstituted pyrrolidines |
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| Affiliation: | 1. CIQUP, Departamento de Química e Bioquímica, Faculdade de Ciências, Universidade do Porto, Rua do Campo Alegre, 687, P-4169-007 Porto, Portugal;2. QOPNA Unit, Departamento de Química, Universidade de Aveiro, 3810-193 Aveiro, Portugal;3. Institut de Chimie de Clermont-Ferrand, CNRS & Univ Clermont Auvergne, 63000 Clermont-Ferrand, France;4. Laboratoire de Chimie de l''ENS Lyon, CNRS & Univ Lyon, 46 allée Italie, 69634 Lyon, France |
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| Abstract: | A small library of novel spiropyrrolidine heterocyclic hybrids has been prepared regioselectively in 1-butyl-3-methylimidazoliumbromide ([bmim]Br) with good to excellent yields using a [3+2] cycloaddition reaction. These synthesized compounds were evaluated as potential agents for treating Alzheimer’s disease. Compound 4b showed the most potent activity, with an IC50 of 7.9 ± 0.25 µM against acetylcholinesterase (AChE). The inhibition mechanisms for the most active compounds on AChE and butyrylcholinesterase (BChE) receptors were elucidated using molecular docking simulations. |
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| Keywords: | Alzheimer’s disease AChE BChE 1,3-dipolar cycloaddition Spiropyrrolidines Molecular docking study |
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