Discovery of 2-(2-oxo-1-phenyl-5-pyridin-2-yl-1, 2-dihydropyridin-3-yl) benzonitrile (perampanel): a novel, noncompetitive α-amino-3-hydroxy-5-methyl-4- …

…, K Kawano, K Ito, Y Norimine, O Takenaka…

文献索引：Hibi, Shigeki; Ueno, Koshi; Nagato, Satoshi; Kawano, Koki; Ito, Koichi; Norimine, Yoshihiko; Takenaka, Osamu; Hanada, Takahisa; Yonaga, Masahiro Journal of Medicinal Chemistry, 2012 , vol. 55, # 23 p. 10584 - 10600

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被引用次数: 52

摘要

Dysfunction of glutamatergic neurotransmission has been implicated in the pathogenesis of epilepsy and numerous other neurological diseases. Here we describe the discovery of a series of 1, 3, 5-triaryl-1 H-pyridin-2-one derivatives as noncompetitive antagonists of AMPA- type ionotropic glutamate receptors. The structure–activity relationships for this series of compounds were investigated by manipulating individual aromatic rings located at ...