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Synthesis and In Vitro Evaluation of N-(Bromobut-3-en-2-yl)-7-methoxy-1,2,3,4-tetrahydroacridin-9-amine as a Cholinesterase Inhibitor with Regard to Alzheimer's Disease Treatment

1
Department of Pharmaceutical Chemistry and Drug Control, Faculty of Pharmacy in Hradec Kralove, Charles University in Prague, Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic
2
Department of Toxicology, Faculty of Military Health Sciences, Trebesska 1575, 500 01 Hradec Kralove, Czech Republic
3
Center of Advanced Studies, Faculty of Military Health Sciences, Trebesska 1575, 500 01 Hradec Kralove, Czech Republic
4
Department of Radiology and Toxicology, Faculty of Health and Social Studies, University of South Bohemia, Ceske Budejovice, Czech Republic
5
Department of Chemistry, Faculty of Sciences, J.E. Purkinje University, Usti nad Labem, Czech Republic
6
Department of Toxicology, Research Center of Military Health Service (CRSSA), 38702 La Tronche Cedex, France
7
Department of Psychiatry, First faculty of Medicine, Charles University in Prague and General University Hospital in Prague, Prague, Czech Republic
*
Author to whom correspondence should be addressed.
Molecules 2010, 15(12), 8804-8812; https://doi.org/10.3390/molecules15128804
Received: 4 November 2010 / Revised: 30 November 2010 / Accepted: 1 December 2010 / Published: 2 December 2010
(This article belongs to the Section Medicinal Chemistry)
A new tacrine based cholinesterase inhibitor, N-(bromobut-3-en-2-yl)-7-methoxy-1,2,3,4-tetrahydroacridin-9-amine (1), was designed and synthesized to interact with specific regions of human acetylcholinesterase and human butyrylcholinesterase. Its inhibitory ability towards cholinesterases was determined and compared to tacrine (THA) and 9-amino-7-methoxy-1,2,3,4-tetrahydroacridine (7-MEOTA). The assessment of IC50 values revealed 1 as a weak inhibitor of both tested enzymes. View Full-Text
Keywords: tacrine; acetylcholinesterase; butyrylcholinesterase; 7-MEOTA; inhibition; Alzheimer disease tacrine; acetylcholinesterase; butyrylcholinesterase; 7-MEOTA; inhibition; Alzheimer disease
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Korabecny, J.; Musilek, K.; Holas, O.; Nepovimova, E.; Jun, D.; Zemek, F.; Opletalova, V.; Patocka, J.; Dohnal, V.; Nachon, F.; Hroudova, J.; Fisar, Z.; Kuca, K. Synthesis and In Vitro Evaluation of N-(Bromobut-3-en-2-yl)-7-methoxy-1,2,3,4-tetrahydroacridin-9-amine as a Cholinesterase Inhibitor with Regard to Alzheimer's Disease Treatment. Molecules 2010, 15, 8804-8812.

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