Optimization of 5-pyridazin-3-one phenoxypropylamines as potent, selective histamine H 3 receptor antagonists with potent cognition enhancing activity

Journal of Medicinal Chemistry

Volumn 55, Issue 1, 2012, Pages 414-423

  Tao, Ming ^a   Aimone, Lisa D ^a   Huang, Zeqi ^a   Mathiasen, Joanne ^a   Raddatz, Rita ^a   Lyons, Jacquelyn ^a   Hudkins, Robert L ^a  

^a CEPHALON INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 [4 (3 CHLOROPROPOXYL)PHENYL]PROPAN 2 ONE; 2 [4 (3 CHLOROPROPOXY)PHENYL]ETHANOL; 2 METHYL 5 [4 (3 AZEPAN 1 YLPROPOXY)PHENYL] 2 METHYL 2H PYRIDAZIN 3 ONE; 2 METHYL 5 [4 (3 PIPERIDIN 1 YLPROPOXY)PHENYL] 2H PYRIDAZIN 3 ONE; 2 METHYL 5 [4 [3 (2 METHYLPYRROLIDIN 1 YL)PROPOXY]PHENYL] 2H PYRIDAZIN 3 ONE; 4 [4 (3 CHLOROPROPOXY)PHENYL] 5 HYDROXY 5H FURAN 2 ONE; 4 METHOXYPHENYLACETALDEHYDE; 5 (4 HYDROXYPHENYL) 2 (3 METHYLPYRIDIN 2 YL) 2H PYRIDAZIN 3 ONE; 5 (4 HYDROXYPHENYL) 2 (6 METHYLPYRIDIN 2 YL) 2H PYRIDAZIN 3 ONE; 5 (4 HYDROXYPHENYL) 2 METHYL 2H PYRIDAZIN 3 ONE; 5 (4 METHOXYPHENYL) 2 (3 METHYLPYRIDIN 2 YL) 2H PYRIDAZIN 3 ONE; 5 (4 METHOXYPHENYL) 2 (6 METHYLPYRIDIN 2 YL) 2H PYRIDAZIN 3 ONE; 5 (4 METHOXYPHENYL) 2 METHYL 2H PYRIDAZIN 3 ONE; 5 (4 METHOXYPHENYL) 2,6 DIMETHYL 2H PYRIDAZIN 3 ONE; 5 (4 METHOXYPHENYL) 2H PYRIDAZIN 3 ONE; 5 (4 METHOXYPHENYL) 6 METHYL 2 (3 METHYLPYRIDIN 2 YL) 2H PYRIDAZIN 3 ONE; 5 (4 METHOXYPHENYL) 6 METHYL 2H PYRIDAZIN 3 ONE; 5 [4 (3 AZEPAN 1 YLPROPOXY)PHENYL] 6 METHYL 2H PYRIDAZIN 3 ONE; 5 [4 (3 CHLOROPROPOXY)PHENYL] 2 ISOPROPYL 2H PYRIDAZIN 3 ONE; 5 [4 (3 CHLOROPROPOXY)PHENYL] 6 METHYL 2 PYRIDIN 2 YL 2H PYRIDAZIN 3 ONE; 5 [4 (3 CHLOROPROPOXY)PHENYL] 6 METHYL 2H PYRIDAZIN 3 ONE; 5 [4 (3 PIPERIDIN 1 YLPROPOXY)PHENYL] 2H PYRIDAZIN 3 ONE; 5 HYDROXY 4 (4 METHOXYPHENYL) 5H FURAN 2 ONE; 5 PYRIDAZIN 3 ONE; 6 METHYL 5 [4 (3 PIPERIDIN 1 YLPROPOXY)PHENYL] 2H PYRIDAZIN 3 ONE; 6 METHYL 5 [4 [3 (2 METHYLPYRROLIDIN 1 YL)PROPOXY]PHENYL] 2 (1 PYRIDAZIN 3 ONE); [4 (3 CHLOROPROPOXY)PHENYL]ACETALDEHYDE; HISTAMINE H3 RECEPTOR ANTAGONIST; PYRIDAZINE DERIVATIVE; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ALKYLATION; ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; COGNITION; DEMETHYLATION; DRUG BINDING; DRUG CLEARANCE; DRUG EFFICACY; DRUG HALF LIFE; DRUG SYNTHESIS; EXPERIMENTAL DOG; EXPERIMENTAL MONKEY; GENOTOXICITY; HUMAN; IN VITRO STUDY; MALE; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; RAT;

ANIMALS; CHO CELLS; CRICETINAE; CRICETULUS; DOGS; DRUG INVERSE AGONISM; HISTAMINE AGONISTS; HISTAMINE H3 ANTAGONISTS; HUMANS; MACACA FASCICULARIS; MALE; MEMORY, SHORT-TERM; MUTAGENICITY TESTS; NOOTROPIC AGENTS; PROPYLAMINES; PYRIDAZINES; RADIOLIGAND ASSAY; RATS; RATS, LONG-EVANS; RATS, SPRAGUE-DAWLEY; RECEPTORS, HISTAMINE H3; RECOGNITION (PSYCHOLOGY); STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; THIRST; TISSUE DISTRIBUTION;

EID: 84855845974     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm201295j     Document Type: Article

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