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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Detalles Bibliográficos
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
Descripción
Sumario: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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