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Molecules 2010, 15(12), 8804-8812; doi:10.3390/molecules15128804
Communication

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

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Received: 4 November 2010 / Revised: 30 November 2010 / Accepted: 1 December 2010 / Published: 2 December 2010
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Abstract

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.
Keywords: tacrine; acetylcholinesterase; butyrylcholinesterase; 7-MEOTA; inhibition; Alzheimer disease tacrine; acetylcholinesterase; butyrylcholinesterase; 7-MEOTA; inhibition; Alzheimer disease
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.

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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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