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
Jazyk angličtina Země Anglie, Velká Británie Médium print-electronic
Typ dokumentu časopisecké články, práce podpořená grantem
PubMed
21920739
DOI
10.1016/j.bmcl.2011.08.042
PII: S0960-894X(11)01127-9
Knihovny.cz E-zdroje
- MeSH
- akridiny chemická syntéza farmakologie MeSH
- cholinergní látky chemická syntéza farmakologie MeSH
- cholinesterasové inhibitory chemická syntéza farmakologie MeSH
- molekulární modely MeSH
- poločas MeSH
- preklinické hodnocení léčiv MeSH
- takrin chemická syntéza farmakologie MeSH
- techniky in vitro MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- akridiny MeSH
- cholinergní látky MeSH
- cholinesterasové inhibitory MeSH
- takrin 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.
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