The synthesis and biological evaluation of quinolyl-piperazinyl piperidines as potent serotonin 5-HT1A antagonists

Journal of Medicinal Chemistry

Volumn 53, Issue 10, 2010, Pages 4066-4084

  Childers, Wayne E ^a   Havran, Lisa M ^a   Asselin, Magda ^a   Bicksler, James J ^a   Chong, Dan C ^a   Grosu, George T ^a   Shen, Zhongqi ^a   Abou Gharbia, Magid A ^a   Bach, Alvin C ^a   Harrison, Boyd L ^a   Kagan, Natasha ^a   Kleintop, Teresa ^a   Magolda, Ronald ^a   Marathias, Vasilios ^a   Robichaud, Albert J ^a   Sabb, Annmarie L ^a   Zhang, Mei Yi ^a   Andree, Terrance H ^a   Aschmies, Susan H ^a   Beyer, Chad ^a   Comery, Thomas A ^a   Day, Mark ^a   Grauer, Steven M ^a   Hughes, Zoe A ^a   Rosenzweig Lipson, Sharon ^a   Platt, Brian ^a   Pulicicchio, Claudine ^a   Smith, Deborah E ^a   Sukoff Rizzo, Stacy J ^a   Sullivan, Kelly M ^a   Adedoyin, Adedayo ^a   Huselton, Christine ^a   Hirst, Warren D ^a   more..

^a PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 FLUORO 8 [4 [4 (6 METHOXYQUINOLIN 8 YL)PIPERAZIN 1 YL]PIPERIDIN 1 YL] QUINOLINE TRIHYDROCHLORIDE; 3,5 DIFLUORO 8 [4 [4 (6 METHOXYQUINOLIN 8 YL)PIPERAZIN 1 YL]PIPERIDIN 1 YL] QUINOLINE TRIHYDROCHLORIDE; 4 METHOXY 8 [4 [4 (6 METHOXYQUINOLIN 8 YL)PIPERAZIN 1 YL]PIPERIDIN 1 YL] 2 (TRIFLUOROMETHYL) QUINOLINE TRIHYDROCHLORIDE; 5 FLUORO 4 METHOXY 8 [4 [4 (6 METHOXYQUINOLIN 8 YL)PIPERAZIN 1 YL]PIPERIDIN 1 YL] 2 (TRIFLUOROMETHYL)QUINOLINE TRIHYDROCHLORIDE; 5 FLUORO 8 [4 [4 (6 METHOXYQUINOLIN 8 YL)PIPERAZIN 1 YL]PIPERIDIN 1 YL] 2 (TRIFLUOROMETHYL) QUINOLINE TRIHYDROCHLORIDE; 5 FLUORO 8 [4 [4 (6 METHOXYQUINOLIN 8 YL)PIPERAZIN 1 YL]PIPERIDIN 1 YL] 2,4 DIMETHYLQUINOLINE TRIHYDROCHLORIDE; 5 FLUORO 8 [4 [4 (6 METHOXYQUINOLIN 8 YL)PIPERAZIN 1 YL]PIPERIDIN 1 YL] 3 (TRIFLUOROMETHYL) QUINOLINE TRIHYDROCHLORIDE; 5 FLUORO 8 [4 [4 (6 METHOXYQUINOLIN 8 YL)PIPERAZIN 1 YL]PIPERIDIN 1 YL] QUINOLINE TRIHYDROCHLORIDE; 6 BROMO 8 [4 [4 (6 METHOXYQUINOLIN 8 YL)PIPERAZIN 1 YL]PIPERIDIN 1 YL] QUINOLINE TRIHYDROCHLORIDE; 6 FLUORO 8 [4 [4 (6 METHOXYQUINOLIN 8 YL)PIPERAZIN 1 YL]PIPERIDIN 1 YL]QUINOLINE TRIHYDROCHLORIDE; 6 METHOXY 8 [1 (TERT BUTOXYCARBONYL) 4 PIPERAZINO]QUINOLINE; 6 METHOXY 8 [4 [1 (8 QUINOLINYL) 4 PIPERIDINYL] 1 PIPERAZINYL] QUINOLINE TRIHYDROCHLORIDE; 6 METHOXY 8 PIPERAZINOQUINOLINE; 7 FLUORO 8 [4 [4 (6 METHOXYQUINOLIN 8 YL)PIPERAZIN 1 YL]PIPERIDIN 1 YL] QUINOLINE TRIHYDROCHLORIDE; 7,8 DIFLUOROQINOLINE; 8 [4 [4 (6 METHOXYQUINOLIN 8 YL)PIPERAZIN 1 YL]PIPERIDIN 1 YL] 2 (TRIFLUOROMETHYL) QUINOLINE TRIHYDROCHLORIDE; 8 [4 [4 (6 METHOXYQUINOLIN 8 YL)PIPERAZIN 1 YL]PIPERIDIN 1 YL] 2 METHYLQUINOLINE TRIHYDROCHLORIDE; 8 [4 [4 (6 METHOXYQUINOLIN 8 YL)PIPERAZIN 1 YL]PIPERIDIN 1 YL] 3 (TRIFLUOROMETHYL) QUINOLINE TRIHYDROCHLORIDE; 8 [4 [4 (6 METHOXYQUINOLIN 8 YL)PIPERAZIN 1 YL]PIPERIDIN 1 YL] 3 METHYLQUINOLINE TRIHYDROCHLORIDE; 8 [4 [4 (6 METHOXYQUINOLIN 8 YL)PIPERAZIN 1 YL]PIPERIDIN 1 YL} 2,4 DIMETHYLQUINOLINE TRIHYDROCHLORIDE; 8 [4 [4 (6 METHOXYQUINOLIN 8 YL)PIPERAZIN 1 YL]PIPERIDIN 1 YL} 4 METHYLQUINOLINE TRIHYDROCHLORIDE; 8 BROMO 6 FLUOROQUINOLINE; 8 CHLORO 5 FLUOROQUINOLINE; 8 CHLORO 6 HYDROXYQUINOLINE; 8 CHLORO 6 METHOXYQUINOLINE; 8 FLUORO 6 BROMOQUINOLINE; FLUOXETINE; PIPERIDINE DERIVATIVE; SEROTONIN 1A ANTAGONIST; UNCLASSIFIED DRUG; UNINDEXED DRUG;

AEROBIC METABOLISM; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; COGNITION; DENATURING HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; DEPRESSION; DRUG ANTAGONISM; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG POTENCY; DRUG SCREENING; DRUG STRUCTURE; DRUG SYNTHESIS; IC 50; IN VITRO STUDY; LEARNING; LIQUID CHROMATOGRAPHY; LIVER MICROSOME METABOLISM; MASS SPECTROMETRY; MEMORY; MICRODIALYSIS; MOUSE; NONHUMAN; PROTON NUCLEAR MAGNETIC RESONANCE; SEXUAL DYSFUNCTION; STRUCTURE ACTIVITY RELATION;

ACETYLCHOLINE; ADMINISTRATION, ORAL; AMYLOID BETA-PROTEIN PRECURSOR; ANIMALS; ANTIDEPRESSIVE AGENTS; BIOLOGICAL AVAILABILITY; CEREBRAL CORTEX; CHO CELLS; COGNITION; CRICETINAE; CRICETULUS; FLUOXETINE; HIPPOCAMPUS; MAZE LEARNING; MEMORY; MICE; MICE, TRANSGENIC; MICROSOMES, LIVER; NOOTROPIC AGENTS; PENILE ERECTION; PIPERAZINES; PIPERIDINES; QUINOLINES; RATS; RECEPTOR, SEROTONIN, 5-HT1A; SEROTONIN; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 77952736758     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm1000908     Document Type: Article

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