Molecules (Dec 2010)

Synthesis and In Vitro Evaluation of N-(Bromobut-3-en-2-yl)-7-methoxy-1,2,3,4-tetrahydroacridin-9-amine as a Cholinesterase Inhibitor with Regard to Alzheimer's Disease Treatment

  • Jiri Patocka,
  • Jan Korabecny,
  • Kamil Kuca,
  • Zdenek Fisar,
  • Jana Hroudova,
  • Florian Nachon,
  • Vlastimil Dohnal,
  • Filip Zemek,
  • Veronika Opletalova,
  • Daniel Jun,
  • Eugenie Nepovimova,
  • Ondrej Holas,
  • Kamil Musilek

DOI
https://doi.org/10.3390/molecules15128804
Journal volume & issue
Vol. 15, no. 12
pp. 8804 – 8812

Abstract

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A new tacrine based cholinesterase inhibitor, N-(bromobut-3-en-2-yl)-7-methoxy-1,2,3,4-tetrahydroacridin-9-amine (1), was designed and synthesized to interact with specific regions of human acetylcholinesterase and human butyrylcholinesterase. Its inhibitory ability towards cholinesterases was determined and compared to tacrine (THA) and 9-amino-7-methoxy-1,2,3,4-tetrahydroacridine (7-MEOTA). The assessment of IC50 values revealed 1 as a weak inhibitor of both tested enzymes.

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