1008798-50-2Relevant articles and documents
Multi-target-directed coumarin derivatives: hAChE and BACE1 inhibitors as potential anti-Alzheimer compounds
Piazzi, Lorna,Cavalli, Andrea,Colizzi, Francesco,Belluti, Federica,Bartolini, Manuela,Mancini, Francesca,Recanatini, Maurizio,Andrisano, Vincenza,Rampa, Angela
, p. 423 - 426 (2008/12/21)
The complex etiology of Alzheimer's disease (AD) prompts scientists to develop multifunctional compounds to combat causes and symptoms of such neurodegeneration. To this aim we designed, synthesized, and tested a series of compounds by introducing halophenylalkylamidic functions on the scaffold of AP2238, which is a dual binding site acetylcholinesterase inhibitor. The inhibitory activity was successfully extended to the beta-site amyloid precursor protein cleavage enzyme, leading to the discovery of a potent inhibitor of this enzyme (3) and affording multifunctional compounds (2, 6, 8) for the treatment of AD.