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2-(2-Phenylmorpholin-4-yl)pyrimidin-4(3H)-ones; a new class of potent, selective and orally active glycogen synthase kinase-3β inhibitors. 2013
Kenji Fukunaga, and
Fumiaki Uehara, and
Keiichi Aritomo, and
Aya Shoda, and
Shinsuke Hiki, and
Masahiro Okuyama, and
Yoshihiro Usui, and
Kazutoshi Watanabe, and
Koichi Yamakoshi, and
Toshiyuki Kohara, and
Tokushi Hanano, and
Hiroshi Tanaka, and
Susumu Tsuchiya, and
Shinji Sunada, and
Ken-Ichi Saito, and
Jun-ichi Eguchi, and
Satoshi Yuki, and
Shoichi Asano, and
Shinji Tanaka, and
Akiko Mori, and
Keiji Yamagami, and
Hiroshi Baba, and
Takashi Horikawa, and
Masatake Fujimura
Mitsubishi Tanabe Pharma Corporation, Kamoshida-cho, Aoba-ku, Yokohama 227-0033, Japan.
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.
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