| Literature DB >> 24176395 |
Kenji Fukunaga1, Fumiaki Uehara, Keiichi Aritomo, Aya Shoda, Shinsuke Hiki, Masahiro Okuyama, Yoshihiro Usui, Kazutoshi Watanabe, Koichi Yamakoshi, Toshiyuki Kohara, Tokushi Hanano, Hiroshi Tanaka, Susumu Tsuchiya, Shinji Sunada, Ken-Ichi Saito, Jun-ichi Eguchi, Satoshi Yuki, Shoichi Asano, Shinji Tanaka, Akiko Mori, Keiji Yamagami, Hiroshi Baba, Takashi Horikawa, Masatake Fujimura.
Abstract
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.Entities:
Keywords: Alzheimer’s disease; Glycogen synthase kinase-3β; Hyperphosphorylation; Tau protein
Mesh：
Substances：
Year: 2013 PMID： 24176395 DOI： 10.1016/j.bmcl.2013.09.020
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823