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Title: 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. Author: Korabecny J, Musilek K, Zemek F, Horova A, Holas O, Nepovimova E, Opletalova V, Hroudova J, Fisar Z, Jung YS, Kuca K. Journal: Bioorg Med Chem Lett; 2011 Nov 01; 21(21):6563-6. PubMed ID: 21920739. Abstract: 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.[Abstract] [Full Text] [Related] [New Search]