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. © 2008 Elsevier Ltd. All rights reserved.
Butini, S., Guarino, E., Campiani, G., Brindisi, M., Coccone, S.S., Fiorini, I., et al. (2008). Tacrine based human cholinesterase inhibitors: synthesis of peptidic-tethered derivatives and their effects on potency and selectivity. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 18(19), 5213-5216 [10.1016/j.bmcl.2008.08.076].
Tacrine based human cholinesterase inhibitors: synthesis of peptidic-tethered derivatives and their effects on potency and selectivity
Butini, Stefania;Guarino, Egeria;Campiani, Giuseppe;Brindisi, Margherita;Coccone, Salvatore Sanna;Fiorini, Isabella;Gemma, Sandra
2008-01-01
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. © 2008 Elsevier Ltd. All rights reserved.
| File | Dimensione | Formato | |
|---|---|---|---|
|
23_2008_BMCL_AChE.pdf
non disponibili
Tipologia:
Abstract
Licenza:
NON PUBBLICO - Accesso privato/ristretto
Dimensione
180.62 kB
Formato
Adobe PDF
|
180.62 kB | Adobe PDF | Visualizza/Apri Richiedi una copia |
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
https://hdl.handle.net/11365/3725
Attenzione
Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo