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N-[5-(5-氟吡啶-3-基)-1H-吡唑-3-基]-4-哌啶-1-丁酰胺（SEN78702，WYE-308775）：一种针对α7 烟碱型乙酰胆碱受体激动剂的临床前候选药物的药物化学研究。

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.

机构信息

Siena Biotech SpA, Strada del Petriccio e Belriguardo 35, 53100 Siena, Italy.

出版信息

J Med Chem. 2012 Nov 26;55(22):10277-81. doi: 10.1021/jm3013568. Epub 2012 Nov 2.

DOI:10.1021/jm3013568
PMID:23083093
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.

摘要

α7 烟碱型乙酰胆碱受体 (α7 nAChR) 是治疗与阿尔茨海默病 (AD) 和精神分裂症相关认知障碍的有前途的治疗候选药物。此前报道的化合物 1（SEN15924，WAY-361789）的药物化学研究工作导致了 12（SEN78702，WYE-308775）的发现，它是一种有效的 α7 nAChR 全激动剂，具有改善的血浆稳定性、脑水平和行为认知模型中的疗效。

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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-氟吡啶-3-基)-1H-吡唑-3-基]-4-哌啶-1-丁酰胺（SEN78702，WYE-308775）：一种针对α7 烟碱型乙酰胆碱受体激动剂的临床前候选药物的药物化学研究。
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