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.

نویسندگان

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

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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عنوان ژورنال:
  • Molecules

دوره 15 12  شماره 

صفحات  -

تاریخ انتشار 2010