• Title of article

    Tacrine based human cholinesterase inhibitors: Synthesis of peptidic-tethered derivatives and their effect on potency and selectivity

  • Author/Authors

    Stefania Butini، نويسنده , , Egeria Guarino، نويسنده , , Giuseppe Campiani، نويسنده , , Margherita Brindisi، نويسنده , , Salvatore Sanna Coccone، نويسنده , , Isabella Fiorini، نويسنده , , Ettore Novellino، نويسنده , , Tatyana Belinskaya، نويسنده , , Ashima Saxena، نويسنده , , Sandra Gemma، نويسنده ,

  • Issue Information
    روزنامه با شماره پیاپی سال 2008
  • Pages
    4
  • From page
    5213
  • To page
    5216
  • Abstract
    Tacrine based reversible inhibitors of cholinesterases (ChEIs) containing peptidic tethers were synthesized to interact with specific regions at the gorge level, and their potency was determined with human (h) acetylcholinesterase and butyrylcholinesterase. Analogues 3i,j and 3l,m were identified as promising hits and may pave the way for the development of a new series of tacrine based enzyme selective hChEIs.
  • Keywords
    inhibitors , Tacrine , Cholinesterases , Alzeheimer’s disease
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Serial Year
    2008
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Record number

    799983