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

被引：15

作者：

Zanaletti, Riccardo ^{[1
]}

Bettinetti, Laura ^{[1
]}

Castaldo, Cristiana ^{[1
]}

Ceccarelli, Ilaria ^{[1
]}

Cocconcelli, Giuseppe ^{[1
]}

Comery, Thomas A. ^{[2
]}

Dunlop, John ^{[2
]}

Genesio, Eva ^{[1
]}

Ghiron, Chiara ^{[1
]}

Haydar, Simon N. ^{[2
]}

Jow, Flora ^{[2
]}

Maccari, Laura ^{[1
]}

Micco, Iolanda ^{[1
]}

Nencini, Arianna ^{[1
]}

Fratelli, Carmela ^{[1
]}

Scali, Carla ^{[1
]}

Turlizzi, Elisa ^{[1
]}

Valacchi, Michela ^{[1
]}

机构：

[1] Siena Biotech SpA, I-53100 Siena, Italy

[2] Pfizer Inc, Neurosci Res Unit, Groton, CT 06340 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2012年 / 55卷 / 22期

关键词：

DISCOVERY; SCHIZOPHRENIA; RAT;

D O I：

10.1021/jm3013568

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

alpha 7 nicotinic acetylcholine receptors (alpha 7 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 alpha 7 nAChR that demonstrated improved plasma stability, brain levels, and efficacy in behavioral cognition models.

引用

页码：10277 / 10281

页数：5

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