N-[5-(5-Fluoropyridin-3-yl)-1 H-pyrazol-3-yl]-4-piperidin-1-ylbutyramide (SEN78702, WYE-308775): A Medicinal Chemistry Effort toward an α7 Nicotinic Acetylcholine …

…, C Castaldo, I Ceccarelli, G Cocconcelli…

文献索引：Zanaletti, Riccardo; Bettinetti, Laura; Castaldo, Cristiana; Ceccarelli, Ilaria; Cocconcelli, Giuseppe; Comery, Thomas A.; Dunlop, John; Genesio, Eva; Ghiron, Chiara; Haydar, Simon N.; Jow, Flora; Maccari, Laura; Micco, Iolanda; Nencini, Arianna; Pratelli, Carmela; Scali, Carla; Turlizzi, Elisa; Valacchi, Michela Journal of Medicinal Chemistry, 2012 , vol. 55, # 22 p. 10277 - 10281

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被引用次数: 7

摘要

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, ...