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

Jan Korabecny 1 email, Kamil Musilek 2,* email, Ondrej Holas 1 , Eugenie Nepovimova 1 , Daniel Jun 3 , Filip Zemek 2 , Veronika Opletalova 1 , Jiri Patocka 4 email, Vlastimil Dohnal 5 , Florian Nachon 6 email, Jana Hroudova 7 , Zdenek Fisar 7  and Kamil Kuca 3 email
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.
Received: 4 November 2010; in revised form: 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

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MDPI and ACS Style

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.

AMA Style

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(12):8804-8812.

Chicago/Turabian Style

Korabecny, Jan; Musilek, Kamil; Holas, Ondrej; Nepovimova, Eugenie; Jun, Daniel; Zemek, Filip; Opletalova, Veronika; Patocka, Jiri; Dohnal, Vlastimil; Nachon, Florian; Hroudova, Jana; Fisar, Zdenek; Kuca, Kamil. 2010. "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 15, no. 12: 8804-8812.

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