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
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