| 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 - Korabecny_2011_Bioorg.Med.Chem.Lett_21_6563 |
| Author(s) : Korabecny J , Musilek K , Zemek F , Horova A , Holas O , Nepovimova E , Opletalova V , Hroudova J , Fisar Z , Jung YS , Kuca K |
| Ref : Bioorganic & Medicinal Chemistry Lett , 21 :6563 , 2011 |
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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. |
| PubMedSearch : Korabecny_2011_Bioorg.Med.Chem.Lett_21_6563 |
| PubMedID: 21920739 |
Korabecny J, Musilek K, Zemek F, Horova A, Holas O, Nepovimova E, Opletalova V, Hroudova J, Fisar Z, Jung YS, Kuca K (2011)
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
Bioorganic & Medicinal Chemistry Lett
21 :6563
Korabecny J, Musilek K, Zemek F, Horova A, Holas O, Nepovimova E, Opletalova V, Hroudova J, Fisar Z, Jung YS, Kuca K (2011)
Bioorganic & Medicinal Chemistry Lett
21 :6563