2. Academic Validation
  3. 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

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

  • J Med Chem. 2012 Nov 26;55(22):10277-81. doi: 10.1021/jm3013568.
Riccardo Zanaletti 1,  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
Affiliations

Affiliation

  • 1 Siena Biotech SpA, Strada del Petriccio e Belriguardo 35, 53100 Siena, Italy. riccardozanaletti@hotmail.com
PMID: 23083093 DOI: 10.1021/jm3013568
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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