6-(4-Pyridyl)pyrimidin-4(3H)-ones as CNS penetrant glycogen synthase kinase-3尾 inhibitors

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• 作者：Fumiaki Uehara ; Aya Shoda ; Keiichi Aritomo ; Kenji Fukunaga ; Kazutoshi Watanabe ; Ryoichi Ando ; Masaki Shinoda ; Hiroaki Ueno ; Hideo Kubodera ; Shinji Sunada ; Ken-Ichi Saito ; Takahide Kaji ; Shoichi Asano ; Jun-ichi Eguchi ; Satoshi Yuki ; Shinji Tanaka ; Yukimi Yoneyama ; Takuro Niwa
• 关键词：Glycogen synthase kinase 3尾 ; Alzheimer&rsquo ; s disease ; Tau protein ; Hyperphoshorylation ; Pyrimidin-4(3H)-one
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：15 December, 2013
• 年：2013
• 卷：23
• 期：24
• 页码：6928-6932
• 全文大小：2920 K

文摘

The discovery of a series of 6-(4-pyridyl)pyrimidin-4(3H)-ones derived from a hit compound with low molecular weight and sufficient chemical space is reported. Transformation of substituents led to subnanomolar potent inhibitors with in vivo tau phoshorylation lowering activity.