Synthesis and Biological Evaluation of Thiophene Derivatives as Acetylcholinesterase Inhibitors
| Autor: | Lamia W. Mohamed, Samar I. Faggal, Mai A. Galal, Mohamed M. Ismail, Mona M. Kamel |
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| Rok vydání: | 2012 |
| Předmět: |
Models
Molecular thiophene Ellman Pharmaceutical Science Thiophenes Gewald acetylcholinesterase Alzheimer’s disease Article Analytical Chemistry lcsh:QD241-441 chemistry.chemical_compound lcsh:Organic chemistry Drug Discovery Thiophene medicine Organic chemistry Physical and Theoretical Chemistry Donepezil Biological evaluation Organic Chemistry Acetylcholinesterase Thiophene derivatives chemistry Chemistry (miscellaneous) Molecular Medicine Cholinesterase Inhibitors Protein Binding medicine.drug |
| Zdroj: | Molecules; Volume 17; Issue 6; Pages: 7217-7231 Molecules Molecules, Vol 17, Iss 6, Pp 7217-7231 (2012) |
| ISSN: | 1420-3049 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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