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...
| Main Authors: | , , , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2012-04-01
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| Series: | Molecules |
| Subjects: | |
| Online Access: | http://www.mdpi.com/1420-3049/17/5/4811 |
| _version_ | 1819037269917433856 |
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| author | Samar I. Faggal Lamia W. Mohamed Mona M. Kamel Mohamed M. Ismail |
| author_facet | Samar I. Faggal Lamia W. Mohamed Mona M. Kamel Mohamed M. Ismail |
| author_sort | Samar I. Faggal |
| collection | DOAJ |
| 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<strong> (IIId)</strong> was found to be the most potent. |
| first_indexed | 2024-12-21T08:18:44Z |
| format | Article |
| id | doaj.art-1dcfc4bf73854fb8ad02388f5a88ed00 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-12-21T08:18:44Z |
| publishDate | 2012-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-1dcfc4bf73854fb8ad02388f5a88ed002022-12-21T19:10:29ZengMDPI AGMolecules1420-30492012-04-011754811482310.3390/molecules17054811Synthesis of New Indole Derivatives Structurally Related to Donepezil and Their Biological Evaluation as Acetylcholinesterase InhibitorsSamar I. FaggalLamia W. MohamedMona M. KamelMohamed M. IsmailNew 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<strong> (IIId)</strong> was found to be the most potent.http://www.mdpi.com/1420-3049/17/5/4811indoleisatinoxindoleacetylcholinesterase inhibitorsAlzheimerdonepezil |
| spellingShingle | Samar I. Faggal Lamia W. Mohamed Mona M. Kamel Mohamed M. Ismail Synthesis of New Indole Derivatives Structurally Related to Donepezil and Their Biological Evaluation as Acetylcholinesterase Inhibitors Molecules indole isatin oxindole acetylcholinesterase inhibitors Alzheimer donepezil |
| 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 | indole isatin oxindole acetylcholinesterase inhibitors Alzheimer donepezil |
| url | http://www.mdpi.com/1420-3049/17/5/4811 |
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