2-{3-[4-(Alkylsulfinyl) phenyl]-1-benzofuran-5-yl}-5-methyl-1, 3, 4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3β with good brain …

…, J Kunitomo, E Kimura, H Iwashita, Y Uno…

文献索引：Saitoh, Morihisa; Kunitomo, Jun; Kimura, Eiji; Iwashita, Hiroki; Uno, Yumiko; Onishi, Tomohiro; Uchiyama, Noriko; Kawamoto, Tomohiro; Tanaka, Toshimasa; Mol, Clifford D.; Dougan, Douglas R.; Textor, Garret P.; Snell, Gyorgy P.; Takizawa, Masayuki; Itoh, Fumio; Kori, Masakuni Journal of Medicinal Chemistry, 2009 , vol. 52, # 20 p. 6270 - 6286

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被引用次数: 66

摘要

Glycogen synthase kinase 3β (GSK-3β) inhibition is expected to be a promising therapeutic approach for treating Alzheimer's disease. Previously we reported a series of 1, 3, 4- oxadiazole derivatives as potent and highly selective GSK-3β inhibitors, however, the representative compounds 1a, b showed poor pharmacokinetic profiles. Efforts were made to address this issue by reducing molecular weight and lipophilicity, leading to the ...