Synthesis and In Vitro Evaluation of New Tacrine Derivates-Bis-Alkylene Linked 7-MEOTA

Author(s): Jan Korabecny, Ondrej Holas, Kamil Musilek, Miroslav Pohanka, Veronika Opletalova, Vlastimil Dohnal, Kamil Kuca

Journal Name: Letters in Organic Chemistry

Volume 7 , Issue 4 , 2010

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Formerly, 9-amino-7-methoxy-1,2,3,4-tetrahydroacridine (7-MEOTA) was investigated as promising tacrine analogue beneficial for its low toxicity compared to tacrine. In this study, novel 7-MEOTA derivatives were synthesized — namely - 9,9-di-(alkane-1,ω-diyldiimino)-di-(7-methoxy-1,2,3,4-tetrahydroacridine) was prepared from the corresponding diiodoalkanes. The novel compounds exhibit anticholinesterase (acetylcholinesterase and butyrylcholinesterase) activity in vitro. The synthesis and in vitro data are summarized in this article.

Keywords: Acetylcholinesterase, butyrylcholinesterase, Alzheimer's disease, tacrine, inhibition selectivity

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Article Details

Year: 2010
Page: [327 - 331]
Pages: 5
DOI: 10.2174/157017810791130540
Price: $65

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