Synthesis and in vitro evaluation of 7-methoxy-N-(pent-4-enyl)-1,2,3,4-tetrahydroacridin-9-amine-new tacrine derivate with cholinergic properties
Language English Country Great Britain, England Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
21920739
DOI
10.1016/j.bmcl.2011.08.042
PII: S0960-894X(11)01127-9
Knihovny.cz E-resources
- MeSH
- Acridines chemical synthesis pharmacology MeSH
- Cholinergic Agents chemical synthesis pharmacology MeSH
- Cholinesterase Inhibitors chemical synthesis pharmacology MeSH
- Models, Molecular MeSH
- Half-Life MeSH
- Drug Evaluation, Preclinical MeSH
- Tacrine chemical synthesis pharmacology MeSH
- In Vitro Techniques MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Acridines MeSH
- Cholinergic Agents MeSH
- Cholinesterase Inhibitors MeSH
- Tacrine MeSH
Cholinesterase inhibitors are, so far, the only successful strategy for the symptomatic treatment of Alzheimer's disease. Tacrine (THA) is a potent acetylcholinesterase inhibitor that was used in the treatment of Alzheimer's disease for a long time. However, the clinical use of THA was hampered by its low therapeutic index, short half-life and liver toxicity. 7-Methoxytacrine (7-MEOTA) is equally pharmacological active compound with lower toxicity compared to THA. In this Letter, the synthesis, biological activity and molecular modelling of elimination by-product isolated during synthesis of 7-MEOTA based bis-alkylene linked compound is described.
References provided by Crossref.org
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