Synthesis and biological activity of putative mono-hydroxylated metabolites of velnacrine

Ten 9-amino-1,2,3,4-tetrahydroacridinediols were prepared as potential mono-hydroxy metabolites of velnacrine. They were tested for acute toxicity as well as for their ability to inhibit acetylcholinesterase in vitro and to reverse scopolamine-induced memory impairment in mice. Synthesis and prelimi...

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Published inBioorganic & medicinal chemistry letters Vol. 2; no. 8; pp. 865 - 870
Main Authors Shutske, Gregory M., Bores, Gina M., Bradshaw, Katherine C., Huger, Francis P., Kapples, Kevin J., Larsen, Raymond D., Rush, Douglas K., Tomer, John D.
Format Journal Article
LanguageEnglish
Published Elsevier Ltd 1992
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Summary:Ten 9-amino-1,2,3,4-tetrahydroacridinediols were prepared as potential mono-hydroxy metabolites of velnacrine. They were tested for acute toxicity as well as for their ability to inhibit acetylcholinesterase in vitro and to reverse scopolamine-induced memory impairment in mice. Synthesis and preliminary biological testing is reported for ten potential mono-hydroxylated metabolites ( 2a–d and 3a–5b) of velnacrine ( 1a).
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(00)80546-6