Synthesis and Biological Evaluation of Thiophene Derivatives as Acetylcholinesterase Inhibitors

A series of new thiophene derivatives has been synthesized using the Gewald protocol. The acetylcholinesterase inhibition activity was assayed according to Ellman’s method using donepezil as reference. Some of the compounds were found to be more potent inhibitors than the reference. 2-(2-(4-(4-Metho...

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Autores principales: Ismail, Mohamed M., Kamel, Mona M., Mohamed, Lamia W., Faggal, Samar I., Galal, Mai A.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2012
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6268334/
https://www.ncbi.nlm.nih.gov/pubmed/22692245
http://dx.doi.org/10.3390/molecules17067217
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author Ismail, Mohamed M.
Kamel, Mona M.
Mohamed, Lamia W.
Faggal, Samar I.
Galal, Mai A.
author_facet Ismail, Mohamed M.
Kamel, Mona M.
Mohamed, Lamia W.
Faggal, Samar I.
Galal, Mai A.
author_sort Ismail, Mohamed M.
collection PubMed
description A series of new thiophene derivatives has been synthesized using the Gewald protocol. The acetylcholinesterase inhibition activity was assayed according to Ellman’s method using donepezil as reference. Some of the compounds were found to be more potent inhibitors than the reference. 2-(2-(4-(4-Methoxyphenyl)piperazin-1-yl)acetamido)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamide (IIId) showed 60% inhibition, compared to only 40% inhibition by donepezil.
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spelling pubmed-62683342018-12-12 Synthesis and Biological Evaluation of Thiophene Derivatives as Acetylcholinesterase Inhibitors Ismail, Mohamed M. Kamel, Mona M. Mohamed, Lamia W. Faggal, Samar I. Galal, Mai A. Molecules Article A series of new thiophene derivatives has been synthesized using the Gewald protocol. The acetylcholinesterase inhibition activity was assayed according to Ellman’s method using donepezil as reference. Some of the compounds were found to be more potent inhibitors than the reference. 2-(2-(4-(4-Methoxyphenyl)piperazin-1-yl)acetamido)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamide (IIId) showed 60% inhibition, compared to only 40% inhibition by donepezil. MDPI 2012-06-12 /pmc/articles/PMC6268334/ /pubmed/22692245 http://dx.doi.org/10.3390/molecules17067217 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.
Galal, Mai A.
Synthesis and Biological Evaluation of Thiophene Derivatives as Acetylcholinesterase Inhibitors
title Synthesis and Biological Evaluation of Thiophene Derivatives as Acetylcholinesterase Inhibitors
title_full Synthesis and Biological Evaluation of Thiophene Derivatives as Acetylcholinesterase Inhibitors
title_fullStr Synthesis and Biological Evaluation of Thiophene Derivatives as Acetylcholinesterase Inhibitors
title_full_unstemmed Synthesis and Biological Evaluation of Thiophene Derivatives as Acetylcholinesterase Inhibitors
title_short Synthesis and Biological Evaluation of Thiophene Derivatives as Acetylcholinesterase Inhibitors
title_sort synthesis and biological evaluation of thiophene derivatives as acetylcholinesterase inhibitors
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6268334/
https://www.ncbi.nlm.nih.gov/pubmed/22692245
http://dx.doi.org/10.3390/molecules17067217
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