1区 · 医学
Article
作者: Comery, Thomas A. ; Castaldo, Cristiana ; Cocconcelli, Giuseppe ; Pratelli, Carmela ; Dunlop, John ; Scali, Carla ; Zanaletti, Riccardo ; Haydar, Simon N. ; Ghiron, Chiara ; Bettinetti, Laura ; Maccari, Laura ; Genesio, Eva ; Valacchi, Michela ; Jow, Flora ; Nencini, Arianna ; Ceccarelli, Ilaria ; Turlizzi, Elisa ; Micco, Iolanda
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.