854716-73-7Relevant articles and documents
Cholinesterase inhibitors: Xanthostigmine derivatives blocking the acetylcholinesterase-induced β-amyloid aggregation
Belluti, Federica,Rampa, Angela,Piazzi, Lorna,Bisi, Alessandra,Gobbi, Silvia,Bartolini, Manuela,Andrisano, Vincenza,Cavalli, Andrea,Recanatini, Maurizio,Valenti, Piero
, p. 4444 - 4456 (2007/10/03)
In continuing research that led us to identify a new class of carbamate derivatives acting as potent (Rampa et al. J. Med. Chem. 1998, 41, 3976) and long-lasting (Rampa et al. J. Med. Chem. 2001, 44, 3810) acetylcholinesterase (AChE) inhibitors, we obtained some analogues able to simultaneously block both the catalytic and the β-amyloid (Aβ) proaggregatory activities of AChE. The key feature of these derivatives is a 2-arylidenebenzocycloalkanone moiety that provides the ability to bind at the AChE peripheral site responsible for promoting the Aβ aggregation. The new carbamates were tested in vitro for the inhibition of both cholinesterases and also for the ability to prevent the AChE-induced Aβ aggregation. All of the compounds had AChE IC 50 values in the nanomolar range and showed the ability to block the AChE-induced Aβ aggregation, thus supporting the feasibility of this new strategy in the search of compounds for the treatment of Alzheimer's disease.
