Synthesis, biological evaluation, and receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as κ-opioid receptor agonists endowed with antinociceptive and antiamnesic activity

Journal of Medicinal Chemistry

Volumn 46, Issue 18, 2003, Pages 3853-3864

  Anzini, Maurizio ^a   Canullo, Laura ^a   Braile, Carlo ^a   Cappelli, Andrea ^a   Gallelli, Andrea ^a   Vomero, Salvatore ^a   Menziani, M Cristina ^b   De Benedetti, Pier G ^b   Rizzo, Milena ^c   Collina, Simona ^d   Azzolina, Ornella ^d   Sbacchi, Massimo ^e,f   Ghelardini, Carla ^g   Galeotti, Nicoletta ^g  

^a UNIVERSITY OF SIENA   (Italy)

^b UNIVERSITY OF MODENA AND REGGIO EMILIA   (Italy)

^c UNIVERSITY MAGNA GRAECIA OF CATANZARO   (Italy)

^d UNIVERSITY OF PAVIA   (Italy)

^e GSK   (Italy)

^f Università degli Studi di Firenze ^*  (Italy)

^g UNIVERSITY OF FLORENCE   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

2,3 DIHYDRO 2 [[(2 FLUOROBENZOYL)AMINO]ETHYL] 5 PHENYL 1H 1,4 BENZODIAZEPINE; 2,3 DIHYDRO 2 [[(2 THIENYLCARBONYL)AMINO]ETHYL] 5 PHENYL 1H 1,4 BENZODIAZEPINE; 2,3 DIHYDRO 2 [[(4 FLUOROBENZOYL)AMINO]ETHYL] 5 PHENYL 1H 1,4 BENZODIAZEPINE; 2,3 DIHYDRO 2 [[(BENZOYL)AMINO]ETHYL] 5 PHENYL 1H 1,4 BENZODIAZEPINE; BENZODIAZEPINE DERIVATIVE; ENKEPHALIN[2 DEXTRO ALANINE 4 METHYLPHENYLALANINE 5 GLYCINE]; ENKEPHALIN[2 DEXTRO ALANINE 5 DEXTRO LEUCINE]; KAPPA OPIATE RECEPTOR; KAPPA OPIATE RECEPTOR AGONIST; KAPPA OPIATE RECEPTOR ANTAGONIST; MORPHINE; N METHYL N [7 (1 PYRROLIDINYL) 1 OXASPIRO[4.5]DEC 8 YL]BENZENEACETAMIDE; NALOXONE; NALTRINDOLE; NORBINALTORPHIMINE; RADIOLIGAND; RHODOPSIN; TIFLUADOM; UNCLASSIFIED DRUG;

AMNESIA; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ANTINOCICEPTION; ARTICLE; CHEMICAL ANALYSIS; CHIRAL CHROMATOGRAPHY; CIRCULAR DICHROISM; CONTROLLED STUDY; CORRELATION ANALYSIS; CRYSTAL STRUCTURE; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SCREENING; DRUG SPECIFICITY; DRUG SYNTHESIS; ENANTIOMER; GUINEA PIG; HOT PLATE TEST; HUMAN; HUMAN CELL; LIQUID CHROMATOGRAPHY; MALE; MOLECULAR CLONING; MOLECULAR DYNAMICS; MOUSE; NONHUMAN; PASSIVE AVOIDANCE; PROTON NUCLEAR MAGNETIC RESONANCE; RACEMIC MIXTURE; RECEPTOR AFFINITY; SIMULATION; STEREOCHEMISTRY; STRUCTURE ACTIVITY RELATION; VALIDATION PROCESS;

AMINO ACID SEQUENCE; ANALGESICS; ANIMALS; AVOIDANCE LEARNING; BENZODIAZEPINES; CELL LINE; CRICETINAE; GUINEA PIGS; HUMANS; LIGANDS; MALE; MICE; MODELS, MOLECULAR; MOLECULAR CONFORMATION; MOLECULAR SEQUENCE DATA; NOOTROPIC AGENTS; PAIN THRESHOLD; RADIOLIGAND ASSAY; RECEPTORS, OPIOID, KAPPA; REGRESSION ANALYSIS; SEQUENCE HOMOLOGY, AMINO ACID; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0041927964     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm0307640     Document Type: Article

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