Abstract
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
Letters in Organic Chemistry
Title: Synthesis and In Vitro Evaluation of New Tacrine Derivates-Bis-Alkylene Linked 7-MEOTA
Volume: 7 Issue: 4
Author(s): Jan Korabecny, Ondrej Holas, Kamil Musilek, Miroslav Pohanka, Veronika Opletalova, Vlastimil Dohnal and Kamil Kuca
Affiliation:
Keywords: Acetylcholinesterase, butyrylcholinesterase, Alzheimer's disease, tacrine, inhibition selectivity
Abstract: 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.
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Korabecny Jan, Holas Ondrej, Musilek Kamil, Pohanka Miroslav, Opletalova Veronika, Dohnal Vlastimil and Kuca Kamil, Synthesis and In Vitro Evaluation of New Tacrine Derivates-Bis-Alkylene Linked 7-MEOTA, Letters in Organic Chemistry 2010; 7 (4) . https://dx.doi.org/10.2174/157017810791130540
DOI https://dx.doi.org/10.2174/157017810791130540 |
Print ISSN 1570-1786 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6255 |
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