The synthesis and activity of 1,3-indandione derivatives as acetylcholinesterase (AChE) inhibitors are reported. The synthetic keystep consists of the Knovenagel olefination between 1,3-indandione and a substituted (1-benzylpiperidin-4-yl)methanal followed by selective double bond reduction. AChE inhibitory activity was measured by a quick fluorimetric method. One of the new compounds showed a significant interaction with the enzyme. Molecular modelling studies were performed in order to propose the binding modes within the AChE gorge compared to the known inhibitor Donepezil.
Caruso, A., Garofalo, A., Grande, F., Aiello, F., Anzini, M., Ortuso, F., et al. (2009). Synthesis and Biological Evaluation of 1,3-Indandione Derivatives as Acetylcholineterase Inhibitors. PHARMACOLOGYONLINE, 1, 264-277.
Synthesis and Biological Evaluation of 1,3-Indandione Derivatives as Acetylcholineterase Inhibitors
Anzini, Maurizio;
2009-01-01
Abstract
The synthesis and activity of 1,3-indandione derivatives as acetylcholinesterase (AChE) inhibitors are reported. The synthetic keystep consists of the Knovenagel olefination between 1,3-indandione and a substituted (1-benzylpiperidin-4-yl)methanal followed by selective double bond reduction. AChE inhibitory activity was measured by a quick fluorimetric method. One of the new compounds showed a significant interaction with the enzyme. Molecular modelling studies were performed in order to propose the binding modes within the AChE gorge compared to the known inhibitor Donepezil.
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https://hdl.handle.net/11365/9269
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