<i>N</i>-[5-(5-Fluoropyridin-3-yl)-1<i>H</i>-pyrazol-3-yl]-4-piperidin-1-ylbutyramide (SEN78702, WYE-308775): A Medicinal Chemistry Effort toward an α7 Nicotinic Acetylcholine Receptor Agonist Preclinical Candidate - Concepedia

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<i>N</i>-[5-(5-Fluoropyridin-3-yl)-1<i>H</i>-pyrazol-3-yl]-4-piperidin-1-ylbutyramide (SEN78702, WYE-308775): A Medicinal Chemistry Effort toward an α7 Nicotinic Acetylcholine Receptor Agonist Preclinical Candidate

DOI Full Paper Access

14

Citations

8

References

2012

Year

Riccardo Zanaletti, Laura Bettinetti, Cristiana Castaldo, Ilaria Ceccarelli, Giuseppe Cocconcelli, Thomas A. Comery, John Dunlop, Eva Genesio, Chiara Ghiron, Simon N. Haydar,

Journal of Medicinal Chemistry

Drug TargetPharmacotherapyPharmaceutical ChemistryMolecular PharmacologyMedicinal ChemistryAlzheimer's DiseaseNicotineα7 NachrNeurologyNeurochemistryCompound 1BiochemistryBehavioral PharmacologyMechanism Of ActionPharmacological AgentNeuropharmacologyPharmacologySelective Full AgonistNatural SciencesMedicinal Chemistry EffortNeuroscienceMedicineSmall MoleculesDrug Discovery

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.

References

	Year	Citations

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