Design and synthesis of thienopyridines as novel templates for acetylcholinesterase inhibitors
New dual binding site acetylcholinesterase (AChE) inhibitors have been designed and synthesized as a new drug candidate for the treatment of Alzheimer’s disease (AD) through the binding to both catalytic and peripheral sites of the enzyme. Therefore, a series of thienopyridine analogs of tacrine wer...
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Veröffentlicht in: | Medicinal chemistry research 2013-09, Vol.22 (9), p.4087-4095 |
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Hauptverfasser: | , , , , |
Format: | Artikel |
Sprache: | eng |
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Online-Zugang: | Volltext |
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Zusammenfassung: | New dual binding site acetylcholinesterase (AChE) inhibitors have been designed and synthesized as a new drug candidate for the treatment of Alzheimer’s disease (AD) through the binding to both catalytic and peripheral sites of the enzyme. Therefore, a series of thienopyridine analogs of tacrine were synthesized and investigated for their ability to inhibit the activity of AChE in comparison with tacrine. All the compounds were found to inhibit AChE activity, especially compounds
7b
and
11a
, which were found to be more potent than tacrine. |
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ISSN: | 1054-2523 1554-8120 |
DOI: | 10.1007/s00044-012-0403-5 |