1,2,3,4-Tetrahydrobenzo[h][1,6]naphthyridines as a new family of potent peripheral-to-midgorge-site inhibitors of acetylcholinesterase: Synthesis, pharmacological evaluation and mechanistic studies

European Journal of Medicinal Chemistry

Volumn 73, Issue , 2014, Pages 141-152

  Di Pietro, Ornella ^a   Viayna, Elisabet ^a   Vicente García, Esther ^b   Bartolini, Manuela ^c   Ramón, Rosario ^b   Juárez Jiménez, Jordi ^a   Clos, M Victòria ^d   Pérez, Belén ^d   Andrisano, Vincenza ^c   Luque, F Javier ^a   Lavilla, Rodolfo ^a,b   Muñoz Torrero, Diego ^a  

^a UNIVERSITY OF BARCELONA   (Spain)

^b Barcelona Science Park   (Spain)

^c UNIVERSITY OF BOLOGNA   (Italy)

^d INSTITUT DE NEUROCIÈNCIES   (Spain)

Author keywords

AChE midgorge binding; AChE PAS binding; Benzo h 1,6 naphthyridines; Dual inhibitors; Povarov reaction

Indexed keywords

1 (TERT BUTOXYCARBONYL) 5 (4 CHLOROPHENYL) N ETHYL 1,2,3,4 TETRAHYDROBENZO[H][1,6]NAPHTHYRIDINE 9 CARBOXAMIDE; 5 (4 CHLOROPHENYL) N ETHYL 1,2,3,4 TETRAHYDROBENZO[H][1,6]NAPHTHYRIDINE 9 CARBOXAMIDE; ACETYLCHOLINESTERASE; ALDEHYDE; ALKENE; ANILINE; CHOLINESTERASE; CHOLINESTERASE INHIBITOR; ENAMINE; ETHYL 1 (TERT BUTOXYCARBONYL) 5 (4 CHLOROPHENYL) 1,2,3,4 TETRAHYDROBENZO[H][1,6]NAPHTHYRIDINE 9 CARBOXYLATE; N [[5 (4 CHLOROPHENYL) 1,2,3,4 TETRAHYDROBENZO[H][1,6]NAPHTHYRIDIN 9 YL]METHYL]ETHANAMINE; NAPHTHYRIDINE DERIVATIVE; PROPIDIUM IODIDE; RECOMBINANT ENZYME; TACRINE; UNCLASSIFIED DRUG;

ARTICLE; BLOOD BRAIN BARRIER; CATALYSIS; CHEMICAL REACTION; CHEMICAL STRUCTURE; CHOLINESTERASE INHIBITION; CONTROLLED STUDY; DRUG BINDING SITE; DRUG MECHANISM; DRUG PENETRATION; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SCREENING; DRUG SYNTHESIS; ELECTROPHORUS; ENZYME ACTIVE SITE; IC 50; INHIBITION KINETICS; MEMBRANE PERMEABILITY; MOLECULAR MODEL;

ACHE MIDGORGE BINDING; ACHE PAS BINDING; BENZO[H][1,6]NAPHTHYRIDINES; DUAL INHIBITORS; POVAROV REACTION;

ACETYLCHOLINESTERASE; ANIMALS; BINDING SITES; BLOOD-BRAIN BARRIER; BUTYRYLCHOLINESTERASE; CHOLINESTERASE INHIBITORS; DRUG DESIGN; ELECTROPHORUS; HUMANS; MEMBRANES, ARTIFICIAL; MODELS, BIOLOGICAL; MOLECULAR DOCKING SIMULATION; MOLECULAR DYNAMICS SIMULATION; MOLECULAR STRUCTURE; NAPHTHYRIDINES; PERMEABILITY; PROTEIN BINDING;

EID: 84891708382     PISSN: 02235234     EISSN: 17683254     Source Type: Journal    
DOI: 10.1016/j.ejmech.2013.12.008     Document Type: Article

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