N-[5-(5-Fluoropyridin-3-yl)-1H-pyrazol-3-yl]-4-piperidin-1-ylbutyramide (SEN78702, WYE-308775): A Medicinal Chemistry Effort toward an 伪7 Nicotinic Acetylcholine Receptor Agonist Preclin
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- 作者：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
- 刊名：Journal of Medicinal Chemistry
- 出版年：2012
- 出版时间：November 26, 2012
- 年：2012
- 卷：55
- 期：22
- 页码：10277-10281
- 全文大小：236K
- 年卷期：v.55,no.22(November 26, 2012)
- ISSN：1520-4804
文摘
伪7 nicotinic acetylcholine receptors (伪7 nAChR) represent promising therapeutic candidates for the treatment of cognitive impairment associated with Alzheimer鈥檚 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 伪7 nAChR that demonstrated improved plasma stability, brain levels, and efficacy in behavioral cognition models.