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Molecules 2015, 20(12), 22084-22101; doi:10.3390/molecules201219836

7-Methoxytacrine-p-Anisidine Hybrids as Novel Dual Binding Site Acetylcholinesterase Inhibitors for Alzheimer’s Disease Treatment

1
Biomedical Research Centre, University Hospital Hradec Kralove, Sokolska 581, 500 05 Hradec Kralove, Czech Republic
2
Department of Toxicology and Military Pharmacy, Faculty of Military Health Sciences, Trebesska 1575, 500 01 Hradec Kralove, Czech Republic
3
National Institute of Mental Health, Topolova 748, 250 67 Klecany, Czech Republic
*
Author to whom correspondence should be addressed.
Academic Editor: Maria Emília de Sousa
Received: 2 November 2015 / Revised: 2 December 2015 / Accepted: 4 December 2015 / Published: 10 December 2015
(This article belongs to the Section Medicinal Chemistry)
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Abstract

Alzheimer’s disease (AD) is a debilitating progressive neurodegenerative disorder that ultimately leads to the patient’s death. Despite the fact that novel pharmacological approaches endeavoring to block the neurodegenerative process are still emerging, none of them have reached use in clinical practice yet. Thus, palliative treatment represented by acetylcholinesterase inhibitors (AChEIs) and memantine are still the only therapeutics used. Following the multi-target directed ligands (MTDLs) strategy, herein we describe the synthesis, biological evaluation and docking studies for novel 7-methoxytacrine-p-anisidine hybrids designed to purposely target both cholinesterases and the amyloid cascade. Indeed, the novel derivatives proved to be effective non-specific cholinesterase inhibitors showing non-competitive AChE inhibition patterns. This compounds’ behavior was confirmed in the subsequent molecular modeling studies. View Full-Text
Keywords: Alzheimer’s disease; acetylcholinesterase; butyrylcholinesterase; tacrine; 7-methoxy-tacrine; MTDLs Alzheimer’s disease; acetylcholinesterase; butyrylcholinesterase; tacrine; 7-methoxy-tacrine; MTDLs
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Korabecny, J.; Andrs, M.; Nepovimova, E.; Dolezal, R.; Babkova, K.; Horova, A.; Malinak, D.; Mezeiova, E.; Gorecki, L.; Sepsova, V.; Hrabinova, M.; Soukup, O.; Jun, D.; Kuca, K. 7-Methoxytacrine-p-Anisidine Hybrids as Novel Dual Binding Site Acetylcholinesterase Inhibitors for Alzheimer’s Disease Treatment. Molecules 2015, 20, 22084-22101.

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