Discovery of novel 2-(alkylmorpholin-4-yl)-6-(3-fluoropyridin-4-yl)-pyrimidin-4(3H)-ones as orally-active GSK-3β inhibitors for Alzheimer's disease

Bioorganic and Medicinal Chemistry Letters

Volumn 25, Issue 5, 2015, Pages 1086-1091

  Fukunaga, Kenji ^a   Sakai, Daiki ^a   Watanabe, Kazutoshi ^a   Nakayama, Kazuki ^a   Kohara, Toshiyuki ^a   Tanaka, Hiroshi ^a   Sunada, Shinji ^a   Nabeno, Mika ^a   Okamoto, Masako ^a   Saito, Ken Ichi ^a,b   Eguchi, Jun Ichi ^a,c   Mori, Akiko ^a   Tanaka, Shinji ^a   Inazawa, Keiko ^a   Horikawa, Takashi ^a  

^a MITSUBISHI TANABE PHARMA CORPORATION   (Japan)

^b Life Science Institute   (Japan)

^c KAITEKI Institute Inc   (Japan)

Author keywords

Alkylmorpholine; Alzheimer's disease; Glycogen synthase kinase 3

Indexed keywords

4 PYRIMIDINONE DERIVATIVE; ALKYL GROUP; CYTOCHROME P450 1A2; CYTOCHROME P450 2D6; CYTOCHROME P450 3A4; GLYCOGEN SYNTHASE KINASE 3 INHIBITOR; GLYCOGEN SYNTHASE KINASE 3BETA; GLYCOGEN SYNTHASE KINASE 3BETA INHIBITOR; METHYL GROUP; MORPHOLINE; NOOTROPIC AGENT; PHENYL GROUP; TAU PROTEIN; UDA 680; UNCLASSIFIED DRUG; GLYCOGEN SYNTHASE KINASE 3; GLYCOGEN SYNTHASE KINASE 3 BETA; MORPHOLINE DERIVATIVE; PYRIMIDINE DERIVATIVE;

ALZHEIMER DISEASE; ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG POTENCY; DRUG SYNTHESIS; ENZYME INHIBITION; HUMAN; IC50; IN VITRO STUDY; IN VIVO STUDY; LIPOPHILICITY; LIVER MICROSOME METABOLISM; MALE; MOLECULAR DOCKING; MOLECULAR WEIGHT; MOUSE; NONHUMAN; PROTEIN PHOSPHORYLATION; PROTON NUCLEAR MAGNETIC RESONANCE; STEREOCHEMISTRY; STEREOISOMERISM; STRUCTURE ACTIVITY RELATION; X RAY CRYSTALLOGRAPHY; ANIMAL; ANTAGONISTS AND INHIBITORS; CHEMISTRY; DRUG DEVELOPMENT; DRUG EFFECTS; ENZYMOLOGY; METABOLISM; ORAL DRUG ADMINISTRATION; PHOSPHORYLATION;

ADMINISTRATION, ORAL; ALZHEIMER DISEASE; ANIMALS; DRUG DISCOVERY; GLYCOGEN SYNTHASE KINASE 3; HUMANS; MICE; MOLECULAR DOCKING SIMULATION; MORPHOLINES; PHOSPHORYLATION; PYRIMIDINES; TAU PROTEINS;

EID: 84922689114     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2015.01.005     Document Type: Article

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