1区 · 医学
Article
作者: Castaldo, Cristiana ; Valacchi, Michela ; Genesio, Eva ; Ghiron, Chiara ; Haydar, Simon N. ; Scali, Carla ; Dunlop, John ; Maccari, Laura ; Micco, Iolanda ; Nencini, Arianna ; Cocconcelli, Giuseppe ; Bettinetti, Laura ; Pratelli, Carmela ; Comery, Thomas A. ; Zanaletti, Riccardo ; Ceccarelli, Ilaria ; Jow, Flora ; Turlizzi, Elisa
α7 Nicotinic acetylcholine receptors (α7 nAChR) represent promising therapeutic candidates for the treatment of cognitive impairment associated with Alzheimer's disease (AD) and schizophrenia. A medicinal chemistry effort around previously reported compound 1 (SEN15924, WAY-361789) led to the identification of 12 (SEN78702, WYE-308775) a potent and selective full agonist of the α7 nAChR that demonstrated improved plasma stability, brain levels, and efficacy in behavioral cognition models.