| Title : N-[5-(5-fluoropyridin-3-yl)-1H-pyrazol-3-yl]-4-piperidin-1-ylbutyramide (SEN78702, WYE-308775): a medicinal chemistry effort toward an alpha7 nicotinic acetylcholine receptor agonist preclinical candidate - Zanaletti_2012_J.Med.Chem_55_10277 |
| Author(s) : Zanaletti R , Bettinetti L , Castaldo C , Ceccarelli I , Cocconcelli G , Comery TA , Dunlop J , Genesio E , Ghiron C , Haydar SN , Jow F , Maccari L , Micco I , Nencini A , Pratelli C , Scali C , Turlizzi E , Valacchi M |
| Ref : Journal of Medicinal Chemistry , 55 :10277 , 2012 |
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Abstract :
alpha7 Nicotinic acetylcholine receptors (alpha7 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 alpha7 nAChR that demonstrated improved plasma stability, brain levels, and efficacy in behavioral cognition models. |
| PubMedSearch : Zanaletti_2012_J.Med.Chem_55_10277 |
| PubMedID: 23083093 |
Zanaletti R, Bettinetti L, Castaldo C, Ceccarelli I, Cocconcelli G, Comery TA, Dunlop J, Genesio E, Ghiron C, Haydar SN, Jow F, Maccari L, Micco I, Nencini A, Pratelli C, Scali C, Turlizzi E, Valacchi M (2012)
N-[5-(5-fluoropyridin-3-yl)-1H-pyrazol-3-yl]-4-piperidin-1-ylbutyramide (SEN78702, WYE-308775): a medicinal chemistry effort toward an alpha7 nicotinic acetylcholine receptor agonist preclinical candidate
Journal of Medicinal Chemistry
55 :10277
Zanaletti R, Bettinetti L, Castaldo C, Ceccarelli I, Cocconcelli G, Comery TA, Dunlop J, Genesio E, Ghiron C, Haydar SN, Jow F, Maccari L, Micco I, Nencini A, Pratelli C, Scali C, Turlizzi E, Valacchi M (2012)
Journal of Medicinal Chemistry
55 :10277