About: 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     Goto   Sponge   NotDistinct   Permalink

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Description
  • 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 paper, the synthesis, biological activity and molecular modelling of elimination by-product isolated during synthesis of 7-MEOTA based bis-alkylene linked compound is described.
  • 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 paper, the synthesis, biological activity and molecular modelling of elimination by-product isolated during synthesis of 7-MEOTA based bis-alkylene linked compound is described. (en)
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
  • 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 (en)
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  • 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
  • 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 (en)
skos:notation
  • RIV/60162694:G44__/11:00002428!RIV13-GA0-G44_____
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • P(GAP303/11/1907), S, Z(MSM0021620849)
http://linked.open...iv/cisloPeriodika
  • 21
http://linked.open...vai/riv/dodaniDat
http://linked.open...aciTvurceVysledku
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  • 233871
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  • RIV/60162694:G44__/11:00002428
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http://linked.open.../riv/klicovaSlova
  • inhibition selectivity; molecular modelling; butyrylcholinesterase; Alzheimer disease; acetylcholinesterase; 7-methoxytacrine (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...odStatuVydavatele
  • GB - Spojené království Velké Británie a Severního Irska
http://linked.open...ontrolniKodProRIV
  • [06A420AD599A]
http://linked.open...i/riv/nazevZdroje
  • Bioorganic & Medicinal Chemistry Letters
http://linked.open...in/vavai/riv/obor
http://linked.open...ichTvurcuVysledku
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http://linked.open...vavai/riv/projekt
http://linked.open...UplatneniVysledku
http://linked.open...v/svazekPeriodika
  • 21
http://linked.open...iv/tvurceVysledku
  • Fišar, Zdeněk
  • Hroudová, Jana
  • Jung, Young-Sik
  • Kuča, Kamil
  • Musílek, Kamil
  • Zemek, Filip
  • Korábečný, Jan
  • Opletalová, Veronika
  • Holas, Ondřej
  • Horová, Anna
  • Nepovimova, Eugenie
http://linked.open...ain/vavai/riv/wos
  • 000296025900071
http://linked.open...n/vavai/riv/zamer
issn
  • 0960-894X
number of pages
http://bibframe.org/vocab/doi
  • 10.1016/j.bmcl.2011.08.042
http://localhost/t...ganizacniJednotka
  • G44
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