Synthesis of New Indole Derivatives Structurally Related to Donepezil and Their Biological Evaluation as Acetylcholinesterase Inhibitors

New series of indole derivatives analogous to donepezil, a well known anti-Alzheimer and acetylcholinesterase inhibitor drug, was synthesized. A full chemical characterization of the new compounds is provided. Biological evaluation of the new compounds as acetylcholinesterase inhibitors was performe...

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Autores principales: Ismail, Mohamed M., Kamel, Mona M., Mohamed, Lamia W., Faggal, Samar I.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2012
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6268345/
https://www.ncbi.nlm.nih.gov/pubmed/22534665
http://dx.doi.org/10.3390/molecules17054811
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author Ismail, Mohamed M.
Kamel, Mona M.
Mohamed, Lamia W.
Faggal, Samar I.
author_facet Ismail, Mohamed M.
Kamel, Mona M.
Mohamed, Lamia W.
Faggal, Samar I.
author_sort Ismail, Mohamed M.
collection PubMed
description New series of indole derivatives analogous to donepezil, a well known anti-Alzheimer and acetylcholinesterase inhibitor drug, was synthesized. A full chemical characterization of the new compounds is provided. Biological evaluation of the new compounds as acetylcholinesterase inhibitors was performed. Most of the compounds were found to have potent acetylcholinesterase inhibitor activity compared to donepezil as standard. The compound 1-(2-(4-(2-fluorobenzyl) piperazin-1-yl)acetyl)indoline-2,3-dione (IIId) was found to be the most potent.
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spelling pubmed-62683452018-12-20 Synthesis of New Indole Derivatives Structurally Related to Donepezil and Their Biological Evaluation as Acetylcholinesterase Inhibitors Ismail, Mohamed M. Kamel, Mona M. Mohamed, Lamia W. Faggal, Samar I. Molecules Article New series of indole derivatives analogous to donepezil, a well known anti-Alzheimer and acetylcholinesterase inhibitor drug, was synthesized. A full chemical characterization of the new compounds is provided. Biological evaluation of the new compounds as acetylcholinesterase inhibitors was performed. Most of the compounds were found to have potent acetylcholinesterase inhibitor activity compared to donepezil as standard. The compound 1-(2-(4-(2-fluorobenzyl) piperazin-1-yl)acetyl)indoline-2,3-dione (IIId) was found to be the most potent. MDPI 2012-04-25 /pmc/articles/PMC6268345/ /pubmed/22534665 http://dx.doi.org/10.3390/molecules17054811 Text en © 2012 by the authors; licensee MDPI, Basel, Switzerland. http://creativecommons.org/licenses/by/3.0/ This article is an open-access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Ismail, Mohamed M.
Kamel, Mona M.
Mohamed, Lamia W.
Faggal, Samar I.
Synthesis of New Indole Derivatives Structurally Related to Donepezil and Their Biological Evaluation as Acetylcholinesterase Inhibitors
title Synthesis of New Indole Derivatives Structurally Related to Donepezil and Their Biological Evaluation as Acetylcholinesterase Inhibitors
title_full Synthesis of New Indole Derivatives Structurally Related to Donepezil and Their Biological Evaluation as Acetylcholinesterase Inhibitors
title_fullStr Synthesis of New Indole Derivatives Structurally Related to Donepezil and Their Biological Evaluation as Acetylcholinesterase Inhibitors
title_full_unstemmed Synthesis of New Indole Derivatives Structurally Related to Donepezil and Their Biological Evaluation as Acetylcholinesterase Inhibitors
title_short Synthesis of New Indole Derivatives Structurally Related to Donepezil and Their Biological Evaluation as Acetylcholinesterase Inhibitors
title_sort synthesis of new indole derivatives structurally related to donepezil and their biological evaluation as acetylcholinesterase inhibitors
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6268345/
https://www.ncbi.nlm.nih.gov/pubmed/22534665
http://dx.doi.org/10.3390/molecules17054811
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