3,4-Dihydro-1,3,5-triazin-2(1H)-ones as the First Dual BACE-1/GSK-3β Fragment Hits against Alzheimer's Disease

ACS Chemical Neuroscience

Volumn 6, Issue 10, 2015, Pages 1665-1682

  Prati, Federica ^a,b   De Simone, Angela ^a,b   Armirotti, Andrea ^a   Summa, Maria ^a   Pizzirani, Daniela ^a   Scarpelli, Rita ^a   Bertozzi, Sine Mandrup ^a   Perez, Daniel I ^c   Andrisano, Vincenza ^b   Perez Castillo, Ana ^d,e   Monti, Barbara ^b   Massenzio, Francesca ^b   Polito, Letizia ^f   Racchi, Marco ^g   Sabatino, Piera ^b   Bottegoni, Giovanni ^a   Martinez, Ana ^c   Cavalli, Andrea ^a,b   Bolognesi, Maria L ^b  

^a ISTITUTO ITALIANO DI TECNOLOGIA   (Italy)

^b UNIVERSITY OF BOLOGNA   (Italy)

^c CENTRO DE INVESTIGACIONES BIOLÓGICAS   (Spain)

^d INSTITUTO DE INVESTIGACIONES BIOMÉDICAS ALBERTO SOLS   (Spain)

^e CENTRO DE INVESTIGACIÓN BIOMÉDICA EN RED SOBRE ENFERMEDADES NEURODEGENERATIVAS CIBERNED   (Spain)

^f Golgi Cenci Foundation   (Italy)

^g UNIVERSITY OF PAVIA   (Italy)

Author keywords

6 amino 3,4 dihydro 1,3,5 triazin 2(1H) one; Alzheimer's disease; drug design; glycogen synthase kinase 3 ; multitarget drug discovery; multitarget directed ligands; secretase

Indexed keywords

2 (3 CHLORO 4 HYDROXYANILINO) 3 (2 NITROPHENYL)MALEIMIDE; 3,4 DIHYDRO 1,3,5 TRIAZIN 2(1H) ONE; 6 AMINO 4 (2 BROMOPHENYL) 3,4 DIHYDRO 1,3,5 TRIAZIN 2(1H) ONE; 6 AMINO 4 (2 FLUOROPHENYL) 3,4 DIHYDRO 1,3,5 TRIAZIN 2(1H) ONE; 6 AMINO 4 (2 FLUOROPHENYL) 3,4 DIHYDRO 1,3,5 TRIAZIN 2(1H) THIONE; 6 AMINO 4 (2 NITROPHENYL) 3,4 DIHYDRO 1,3,5 TRIAZIN 2(1H) ONE; 6 AMINO 4 (2 TOLYL) 3,4 DIHYDRO 1,3,5 TRIAZIN 2(1H) ONE; 6 AMINO 4 (3 BROMOPHENYL) 3,4 DIHYDRO 1,3,5 TRIAZIN 2(1H) ONE; 6 AMINO 4 (3 CHLOROPHENYL) 3,4 DIHYDRO 1,3,5 TRIAZIN 2(1H) ONE; 6 AMINO 4 (3 FLUOROPHENYL) 3,4 DIHYDRO 1,3,5 TRIAZIN 2(1H) ONE; 6 AMINO 4 (3 NITROPHENYL) 3,4 DIHYDRO 1,3,5 TRIAZIN 2(1H) ONE; 6 AMINO 4 (3 TOLYL) 3,4 DIHYDRO 1,3,5 TRIAZIN 2(1H) ONE; 6 AMINO 4 (3,4 DICHLOROPHENYL) 3,4 DIHYDRO 1,3,5 TRIAZIN 2(1H) ONE; 6 AMINO 4 (3,5 DIFLUOROPHENYL) 3,4 DIHYDRO 1,3,5 TRIAZIN 2(1H) ONE; 6 AMINO 4 (4 CHLOROPHENYL) 3,4 DIHYDRO 1,3,5 TRIAZIN 2(1H) ONE; 6 AMINO 4 (4 NITROPHENYL) 3,4 DIHYDRO 1,3,5 TRIAZIN 2(1H) ONE; 6 AMINO 4 (PYRIDIN 3 YL) 3,4 DIHYDRO 1,3,5 TRIAZIN 2(1H) ONE; 6 AMINO 4 PHENYL 3,4 DIHYDRO 1,3,5 TRIAZIN 2(1H) THIONE; 6 AMINO 4 [2 (TRIFLUOROMETHYL)PHENYL] 3,4 DIHYDRO 1,3,5 TRIAZIN 2(1H) ONE; 6 AMINO 4 [3 (DIMETHYLAMINOL)PHENYL] 3,4 DIHYDRO 1,3,5 TRIAZIN 2(1H) ONE; 6 AMINO 4 [3 (TRIFLUOROMETHYL)PHENYL] 3,4 DIHYDRO 1,3,5 TRIAZIN 2(1H) ONE; 6 AMINO 4 [3 [(DIMETHYLAMINOL)METHYL]PHENYL] 3,4 DIHYDRO 1,3,5 TRIAZIN 2(1H) ONE; 6 AMINO 4 [4 (PIPERIDIN 1 YLMETHYL)PHENYL] 3,4 DIHYDRO 1,3,5 TRIAZIN 2(1H) ONE; AMYLOID BETA PROTEIN[1-40]; BETA SECRETASE 1; BETA SECRETASE INHIBITOR; GLYCOGEN SYNTHASE KINASE 3 INHIBITOR; GLYCOGEN SYNTHASE KINASE 3BETA; TRIAZINE DERIVATIVE; UNCLASSIFIED DRUG; UNINDEXED DRUG; AMYLOID PRECURSOR PROTEIN; ASPARTIC PROTEINASE; BACE PROTEIN, RAT; GLYCOGEN SYNTHASE KINASE 3; GLYCOGEN SYNTHASE KINASE 3 BETA; LIPOPOLYSACCHARIDE; NEUROLEPTIC AGENT; SECRETASE; TUBULIN;

ALZHEIMER DISEASE; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; AREA UNDER THE CURVE; ARTICLE; BLOOD BRAIN BARRIER; CONTROLLED STUDY; DRUG HALF LIFE; DRUG PENETRATION; DRUG SYNTHESIS; ENZYME INHIBITION; HUMAN; HUMAN CELL; IC50; MAXIMUM PLASMA CONCENTRATION; NERVOUS SYSTEM DEVELOPMENT; NEUROPROTECTION; NONHUMAN; PRIORITY JOURNAL; RAT; STRUCTURE ACTIVITY RELATION; ANIMAL; BRAIN CORTEX; CELL CULTURE; CHEMISTRY; CYTOLOGY; DRUG EFFECTS; GENETICS; GLIA; GLIOMA; METABOLISM; MOUSE; NEWBORN; PATHOLOGY; TIME FACTOR; WISTAR RAT;

AMYLOID BETA-PROTEIN PRECURSOR; AMYLOID PRECURSOR PROTEIN SECRETASES; ANIMALS; ANIMALS, NEWBORN; ANTIPSYCHOTIC AGENTS; ASPARTIC ACID ENDOPEPTIDASES; CELLS, CULTURED; CEREBRAL CORTEX; GLIOMA; GLYCOGEN SYNTHASE KINASE 3; HUMANS; INHIBITORY CONCENTRATION 50; LIPOPOLYSACCHARIDES; MICE; NEUROGLIA; RATS; RATS, WISTAR; TIME FACTORS; TRIAZINES; TUBULIN;

EID: 84945541753     PISSN: None     EISSN: 19487193     Source Type: Journal    
DOI: 10.1021/acschemneuro.5b00121     Document Type: Article

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