Submitted by kej2006 on June 6, 2018 - 4:13pm
Title | Ionic liquid-enabled synthesis, cholinesterase inhibitory activity, and molecular docking study of highly functionalized tetrasubstituted pyrrolidines. |
Publication Type | Journal Article |
Year of Publication | 2018 |
Authors | Kumar RSuresh, Almansour AI, Arumugam N, Althomili DMohammed Q, Altaf M, Basiri A, D K, Manohar TSai, S V |
Journal | Bioorg Chem |
Volume | 77 |
Pagination | 263-268 |
Date Published | 2018 Apr |
ISSN | 1090-2120 |
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 IC 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. |
DOI | 10.1016/j.bioorg.2018.01.019 |
Alternate Journal | Bioorg. Chem. |
PubMed ID | 29421701 |