N-[5-(5-Fluoropyridin-3-yl)-1H-pyrazol-3-yl]-4-piperidin-1-ylbutyramide (SEN78702, WYE-308775): A Medicinal Chemistry Effort toward an α7 Nicotinic Acetylcholine Receptor Agonist Preclinical Candidate
Journal of Medicinal Chemistry2012Vol. 55(22), pp. 10277–10281
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Riccardo Zanaletti, Laura Bettinetti, Cristiana Castaldo, Ilaria Ceccarelli, Giuseppe Cocconcelli, Thomas A. Comery, John Dunlop, Eva Genesio, Chiara Ghiron, Simon N. Haydar, Flora Jow, Laura Maccari, Iolanda Micco, Arianna Nencini, Carmela Pratelli, Carla Scali, Elisa Turlizzi, Michela Valacchi
Abstract
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.
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