Design, synthesis and biological evaluation of benzo[e][1,2,4]triazin-7(1H) -one and [1,2,4]-triazino[5,6,1-jk]carbazol-6-one derivatives as dual inhibitors of beta-amyloid aggregation and acetyl/butyryl cholinesterase

European Journal of Medicinal Chemistry

Volumn 58, Issue , 2012, Pages 84-97

  Catto, Marco ^a   Berezin, Andrey A ^b   Lo Re, Daniele ^b   Loizou, Georgia ^b   Demetriades, Marina ^b   De Stradis, Angelo ^a   Campagna, Francesco ^a   Koutentis, Panayiotis A ^b   Carotti, Angelo ^a  

^a UNIVERSITY OF BARI   (Italy)

^b UNIVERSITY OF CYPRUS   (Cyprus)

Author keywords

Amyloid aggregation inhibitors; Alzheimer's disease; Benzotriazinones; Cholinesterase inhibitors; Multitarget directed ligands; Triazafluoranthenones

Indexed keywords

2 PHENYL 5 (4 PHENYLPIPERIDIN 1 YL) 6H (1,2,4)TRIAZINO (5,6,1 JK)CARBAZOL 6 ONE; 5 (N BENZYL N METHYLAMINO) 2 PHENYL 6H (1,2,4)TRIAZINO(5,6,1 JK)CARBAZOL 6 ONE; 5 [[8 [BENZYL(METHYL)AMINO]OCTYL]AMINO] 2 PHENYL 6H (1,2,4)TRIAZINO(5,6,1 JK) CARBAZOL 6 ONE; 5 [N [3 (DIMETHYLAMINO)PROPYL] N METHYLAMINO] 2 PHENYL 6H (1,2,4)TRIAZINO(5,6,1 JK) CARBAZOL 6 ONE; 6 (2 METHYLPIPERIDIN 1 YL) 1,3 DIPHENYLBENZO(E)(1,2,4)TRIAZIN 7 (1H) ONE; 6 (3 METHYLPIPERIDIN 1 YL) 1,3 DIPHENYLBENZO(E)(1,2,4)TRIAZIN 7 (1H) ONE; 6 (3,5 DIMETHYLPIPERIDIN 1 YL) 1,3 DIPHENYLBENZO(E)(1,2,4)TRIAZIN 7 (1H) ONE; 6 (4 BENZYLPIPERAZIN 1 YL) 1,3 DIPHENYLBENZO(E)(1,2,4)TRIAZIN 7 (1H) ONE; 6 (4 METHYLPIPERIDIN 1 YL) 1,3 DIPHENYLBENZO(E)(1,2,4)TRIAZIN 7 (1H) ONE; 6 (4 PHENYLPIPERIDIN 1 YL) 1,3 DIPHENYLBENZO(E)(1,2,4)TRIAZIN 7 (1H) ONE; 6 (AZEPAN 1 YL) 1,3 DIPHENYLBENZO(E)(1,2,4)TRIAZIN 7(1H)ONE; 6 (N BENZYL N ETHYLAMINO) 1,3 DIPHENYLBENZO(E)(1,2,4)TRIAZIN 7(1H)ONE; 6 (N BENZYL N METHYLAMINO) 1,3 DIPHENYLBENZO(E)(1,2,4)TRIAZIN 7(1H)ONE; 6 [3,4 DIHYDROQUINOLIN 1 (2H)YL] 1,3 DIPHENYLBENZO(E)(1,2,4)TRIAZIN 7(1H)ONE; 6 [8 (N BENZYL N METHYLAMINO)OCTYLAMINO] 1,3 DIPHENYLBENZO(E)(1,2,4)TRIAZIN 7(1H)ONE; 6 [N [3 (DIMETHYLAMINO)PROPYL] N METHYLAMINO] 1,3 DIPHENYLBENZO(E)(1,2,4) TRIAZIN 7(1H) ONE; 6 MORPHOLINO 1,3 DIPHENYLBENZO(E)(1,2,4)TRIAZIN 7 (1H)ONE; 6 THIOMORPHOLINO 1,3 DIPHENYLBENZO(E)(1,2,4)TRIAZIN 7 (1H)ONE; ACETYLCHOLINESTERASE; AMYLOID BETA PROTEIN; CHOLINESTERASE; CHOLINESTERASE INHIBITOR; COLLAGEN FIBRIL; THIOFLAVINE; UNCLASSIFIED DRUG;

AQUEOUS SOLUTION; ARTICLE; BETA SHEET; BINDING SITE; BIOLOGICAL ACTIVITY; CIRCULAR DICHROISM; COMPETITIVE INHIBITION; CONCENTRATION RESPONSE; CONFORMATION; DRUG DESIGN; DRUG SYNTHESIS; IC 50; PROTEIN AGGREGATION; PROTEIN STABILITY; PROTEIN TARGETING; SPECTROFLUOROMETRY; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION; THIN LAYER CHROMATOGRAPHY; TRANSMISSION ELECTRON MICROSCOPY;

ACETYLCHOLINESTERASE; AMYLOID BETA-PEPTIDES; ANIMALS; BUTYRYLCHOLINESTERASE; CHOLINESTERASE INHIBITORS; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DESIGN; ELECTROPHORUS; HORSES; MOLECULAR STRUCTURE; PEPTIDE FRAGMENTS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84867830552     PISSN: 02235234     EISSN: 17683254     Source Type: Journal    
DOI: 10.1016/j.ejmech.2012.10.003     Document Type: Article

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