2-(2-Phenylmorpholin-4-yl)pyrimidin-4(3H)-ones; A new class of potent, selective and orally active glycogen synthase kinase-3β inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 23, Issue 24, 2013, Pages 6933-6937

  Fukunaga, Kenji ^a   Uehara, Fumiaki ^a   Aritomo, Keiichi ^a   Shoda, Aya ^a   Hiki, Shinsuke ^a   Okuyama, Masahiro ^a   Usui, Yoshihiro ^a,b   Watanabe, Kazutoshi ^a   Yamakoshi, Koichi ^a,b   Kohara, Toshiyuki ^a   Hanano, Tokushi ^a   Tanaka, Hiroshi ^a   Tsuchiya, Susumu ^a,c   Sunada, Shinji ^a   Saito, Ken Ichi ^a,d   Eguchi, Jun Ichi ^a,e   Yuki, Satoshi ^a   Asano, Shoichi ^a   Tanaka, Shinji ^a   Mori, Akiko ^a   Yamagami, Keiji ^a,f   Baba, Hiroshi ^a   Horikawa, Takashi ^a   Fujimura, Masatake ^a,g   more..

^a MITSUBISHI TANABE PHARMA CORPORATION   (Japan)

^b Tanabe RandD Service Corporation   (Japan)

^c Mitsubishi Tanabe Pharma Factory Ltd   (Japan)

^d MITSUBISHI KAGAKU INSTITUTE OF LIFE SCIENCES   (Japan)

^e KAITEKI Institute Inc   (Japan)

^f UNIVERSITY OF TOKYO HOSPITAL   (Japan)

^g NATIONAL INSTITUTE FOR MINAMATA DISEASE   (Japan)

Author keywords

Alzheimer's disease; Glycogen synthase kinase 3 ; Hyperphosphorylation; Tau protein

Indexed keywords

GLYCOGEN SYNTHASE KINASE 3BETA; LITHIUM CHLORIDE; PROPRANOLOL; PYRIMIDINE DERIVATIVE; TAU PROTEIN;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; BLOOD BRAIN BARRIER; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG HALF LIFE; DRUG INHIBITION; DRUG POTENCY; DRUG SELECTIVITY; DRUG SYNTHESIS; DRUG TRANSFORMATION; ENZYME INHIBITION; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; MALE; MAXIMUM PLASMA CONCENTRATION; MOLECULAR DOCKING; MOUSE; NONHUMAN; PROTEIN PHOSPHORYLATION; RAT;

MUS;

ALZHEIMER'S DISEASE; GLYCOGEN SYNTHASE KINASE-3Β; HYPERPHOSPHORYLATION; TAU PROTEIN;

ADMINISTRATION, ORAL; ANIMALS; BINDING SITES; CYTOCHROME P-450 ENZYME SYSTEM; ENZYME ACTIVATION; FEMALE; GLYCOGEN SYNTHASE KINASE 3; HALF-LIFE; HUMANS; MALE; MICE; MICROSOMES, LIVER; MOLECULAR DOCKING SIMULATION; MORPHOLINES; PHOSPHORYLATION; PROTEIN KINASE INHIBITORS; PROTEIN STRUCTURE, TERTIARY; PYRIMIDINONES; RATS; RATS, SPRAGUE-DAWLEY; STEREOISOMERISM; TAU PROTEINS;

EID: 84888881229     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2013.09.020     Document Type: Article

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