Discovery of tetrasubstituted imidazolines as potent and selective neuropeptide Y Y5 receptor antagonists: Reduced human ether-a-go-go related gene potassium channel binding affinity and potent antiobesity effect

Journal of Medicinal Chemistry

Volumn 52, Issue 10, 2009, Pages 3385-3396

  Sato, Nagaaki ^a   Ando, Makoto ^a   Ishikawa, Shiho ^a   Jitsuoka, Makoto ^a   Nagai, Keita ^a   Takahashi, Hirobumi ^a   Sakuraba, Aya ^a   Tsuge, Hiroyasu ^a   Kitazawa, Hidefumi ^a   Iwaasa, Hisashi ^a   Mashiko, Satoshi ^a   Gomori, Akira ^a   Moriya, Ryuichi ^a   Fujino, Naoko ^a   Ohe, Tomoyuki ^a   Ishihara, Akane ^a   Kanatani, Akio ^a   Fukami, Takehiro ^a  

^a BANYU PHARMACEUTICAL CO LTD   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

2 [(4 (4 FLUOROPHENYL) 4 (6 FLUORO 3 PYRIDYL) 5 METHYL 4,5 DIHYDRO 1H IMIDAZOL 2 YL] 4 METHYLOXYPYRIDINE; 2 [(4 (4 FLUOROPHENYL) 4 (6 FLUORO 3 PYRIDYL) 5 METHYL 4,5 DIHYDRO 1H IMIDAZOL 2 YL] 4 PYRIMIDINECARBONITRILE; 2 [4 (4 FLUOROPHENYL) 4 (6 FLUORO 3 PYRIDYL) 5 METHYL 4,5 DIHYDRO 1H IMIDAZOL 2 YL] 4 PYRIDINECARBONITRILE; 2 [4 (4 FLUOROPHENYL) 4 (6 FLUORO 3 PYRIDYL) 5 METHYL 4,5 DIHYDRO 1H IMIDAZOL 2 YL] 4 PYRIDINECARBOXAMIDE; 2 [4 (4 FLUOROPHENYL) 4 (6 FLUORO 3 PYRIDYL) 5 METHYL 4,5 DIHYDRO 1H IMIDAZOL 2 YL]PYRAZINE; 2 [4,4 BIS(4 FLUOROPHENYL) 5 HYDROXYMETHYL 4,5 DIHYDRO 1H IMIDAZOL 2 YL] 4 PYRIDINECARBONITRILE; 2 [4,4 BIS(4 FLUOROPHENYL) 5 METHYL 4,5 DIHYDRO 1H IMIDAZOL 2 YL] 4 PYRIDINECARBONITRILE; 2 [4,4 BIS(4 FLUOROPHENYL) 5 METHYL 4,5 DIHYDRO 1H IMIDAZOL 2 YL]PYRAZINE; 2 [4,4 BIS(4 FLUOROPHENYL) 5 PROPYL 4,5 DIHYDRO 1H IMIDAZOL 2 YL] 4 PYRIDINECARBONITRILE; 2 [4,4 BIS(6 FLUORO 3 PYRIDYL) 5 METHYL 4,5 DIHYDRO 1H IMIDAZOL 2 YL] 4 PYRIDINECARBONITRILE; 2 [5 ETHYL 4,4 BIS(4 FLUOROPHENYL) 4,5 DIHYDRO 1H IMIDAZOL 2 YL] 4 PYRIDINECARBONITRILE; 2 FLUORO 5 [4 (4 FLUOROPHENYL) 5 METHYL 2 (1,2,5 THIADIAZOL 3 YL) 4,5 DIHYDRO 1H IMIDAZOL 4 YL]PYRIDINE; 2 FLUORO 5 [4 (4 FLUOROPHENYL) 5 METHYL 2 (1,3 THIAZOL 2 YL) 4,5 DIHYDRO 1H IMIDAZOL 4 YL]PYRIDINE; 2 FLUORO 5 [4 (4 FLUOROPHENYL) 5 METHYL 2 (3 METHYLSULFONYLPHENYL) 4,5 DIHYDRO 1H IMIDAZOL 4 YL]PYRIDINE; 3 [4 (4 FLUOROPHENYL) 4 (6 FLUORO 3 PYRIDYL) 5 METHYL 4,5 DIHYDRO 1H IMIDAZOL 2 YL]BENZONITRILE; 4 [4 (4 FLUOROPHENYL) 4 (6 FLUORO 3 PYRIDYL) 5 METHYL 4,5 DIHYDRO 1H IMIDAZOL 2 YL] 2 PYRIDINECARBONITRILE; 4 [4 (4 FLUOROPHENYL) 4 (6 FLUORO 3 PYRIDYL) 5 METHYL 4,5 DIHYDRO 1H IMIDAZOL 2 YL]PYRIDINE 1 OXIDE; 4 CHLORO 2 [(4 (4 FLUOROPHENYL) 4 (6 FLUORO 3 PYRIDYL) 5 METHYL 4,5 DIHYDRO 1H IMIDAZOL 2 YL]PYRIDINE; 5 [4 (4 FLUOROPHENYL) 4 (6 FLUORO 3 PYRIDYL) 5 METHYL 4,5 DIHYDRO 1H IMIDAZOL 2 YL] 3 PYRIDINECARBONITRILE; 6 [4 (4 FLUOROPHENYL) 4 (6 FLUORO 3 PYRIDYL) 5 METHYL 4,5 DIHYDRO 1H IMIDAZOL 2 YL] 2 PYRIDINECARBONITRILE; 6 [4 (4 FLUOROPHENYL) 4 (6 FLUORO 3 PYRIDYL) 5 METHYL 4,5 DIHYDRO 1H IMIDAZOL 2 YL] 2(1H) PYRIDINONE; ETHYL 2 [4 (4 FLUOROPHENYL) 4 (6 FLUORO 3 PYRIDYL) 5 METHYL 4,5 DIHYDRO 1H IMIDAZOL 2 YL] 4 PYRIMIDINECARBOXYLATE; IMIDAZOLINE DERIVATIVE; METHYL 2 [4 (4 FLUOROPHENYL) 4 (6 FLUORO 3 PYRIDYL) 5 METHYL 4,5 DIHYDRO 1H IMIDAZOL 2 YL] 4 PYRIDINECARBOXYLATE; NEUROPEPTIDE Y RECEPTOR ANTAGONIST; POTASSIUM CHANNEL HERG; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BINDING AFFINITY; CONTROLLED STUDY; DRUG BRAIN LEVEL; DRUG EFFECT; DRUG PENETRATION; DRUG SCREENING; DRUG STRUCTURE; DRUG SYNTHESIS; FOOD INTAKE; MALE; MAXIMUM PLASMA CONCENTRATION; MOUSE; NONHUMAN; OBESITY; RAT; STRUCTURE ACTIVITY RELATION; WEIGHT REDUCTION;

ANIMALS; ANTI-OBESITY AGENTS; BRAIN; CEREBROSPINAL FLUID; DISEASE MODELS, ANIMAL; DRUG DISCOVERY; ETHER-A-GO-GO POTASSIUM CHANNELS; HUMANS; IMIDAZOLINES; OBESITY; PHARMACOKINETICS; PROTEIN BINDING; RATS; RECEPTORS, NEUROPEPTIDE Y; STRUCTURE-ACTIVITY RELATIONSHIP; WEIGHT LOSS;

EID: 66249142634     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm900110t     Document Type: Article

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