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.