99985-89-4Relevant articles and documents
2-(2-Phenylmorpholin-4-yl)pyrimidin-4(3H)-ones; A new class of potent, selective and orally active glycogen synthase kinase-3β inhibitors
Fukunaga, Kenji,Uehara, Fumiaki,Aritomo, Keiichi,Shoda, Aya,Hiki, Shinsuke,Okuyama, Masahiro,Usui, Yoshihiro,Watanabe, Kazutoshi,Yamakoshi, Koichi,Kohara, Toshiyuki,Hanano, Tokushi,Tanaka, Hiroshi,Tsuchiya, Susumu,Sunada, Shinji,Saito, Ken-Ichi,Eguchi, Jun-Ichi,Yuki, Satoshi,Asano, Shoichi,Tanaka, Shinji,Mori, Akiko,Yamagami, Keiji,Baba, Hiroshi,Horikawa, Takashi,Fujimura, Masatake
, p. 6933 - 6937 (2013)
A series of 2-(2-phenylmorpholin-4-yl)pyrimidin-4(3H)-ones was synthesized and examined for their inhibitory activity against glycogen synthase kinase-3β (GSK-3β). We found 21, 29 and 30 to possess potent in vitro GSK-3β inhibitory activity with good in vitro PK profiles. 21 demonstrated significant decrease of tau phosphorylation after oral administration in mice and excellent PK profiles.
