| Title : Tacrine based human cholinesterase inhibitors: synthesis of peptidic-tethered derivatives and their effect on potency and selectivity - Butini_2008_Bioorg.Med.Chem.Lett_18_5213 |
| Author(s) : Butini S , Guarino E , Campiani G , Brindisi M , Coccone SS , Fiorini I , Novellino E , Belinskaya T , Saxena A , Gemma S |
| Ref : Bioorganic & Medicinal Chemistry Lett , 18 :5213 , 2008 |
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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. |
| PubMedSearch : Butini_2008_Bioorg.Med.Chem.Lett_18_5213 |
| PubMedID: 18786825 |
Butini S, Guarino E, Campiani G, Brindisi M, Coccone SS, Fiorini I, Novellino E, Belinskaya T, Saxena A, Gemma S (2008)
Tacrine based human cholinesterase inhibitors: synthesis of peptidic-tethered derivatives and their effect on potency and selectivity
Bioorganic & Medicinal Chemistry Lett
18 :5213
Butini S, Guarino E, Campiani G, Brindisi M, Coccone SS, Fiorini I, Novellino E, Belinskaya T, Saxena A, Gemma S (2008)
Bioorganic & Medicinal Chemistry Lett
18 :5213