Atropisomeric 4-phenyl-4 H -1,2,4-triazoles as selective glycine transporter 1 inhibitors

Journal of Medicinal Chemistry

Volumn 56, Issue 14, 2013, Pages 5744-5756

  Sugane, Takashi ^a   Tobe, Takahiko ^a   Hamaguchi, Wataru ^a   Shimada, Itsuro ^a   Maeno, Kyoichi ^a   Miyata, Junji ^a   Suzuki, Takeshi ^a   Kimizuka, Tetsuya ^a   Sakamoto, Shuichi ^a   Tsukamoto, Shin Ichi ^a  

^a ASTELLAS PHARMA INC   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

1 [3 [3 (BIPHENYL 4 YL) 5 ETHYL 4H 1,2,4 TRIAZOL 4 YL] 2 METHYLPHENYL] N,N DIMETHYLMETHANAMINE; 1,2,4 TRIAZOLE DERIVATIVE; 3 (BIPHENYL 4 YL) 4 [3 (CHLOROMETHYL) 2 METHYLPHENYL] 5 ETHYL 4H 1,2,4 TRIAZOLE; 3 (BIPHENYL 4 YL) 5 ETHYL 4 [3 (METHOXYMETHYL) 2 METHYLPHENYL] 5 ETHYL 4H 1,2,4 TRIAZOLE; 3 [3 (BIPHENYL 4 YL) 5 ETHYL 4H 1,2,4 TRIAZOL 4 YL] 2 METHYLANILINE; 3 [3 (BIPHENYL 4 YL) 5 ETHYL 4H 1,2,4 TRIAZOL 4 YL] 2 METHYLBENZAMIDE; 3 [3 (BIPHENYL 4 YL) 5 ETHYL 4H 1,2,4 TRIAZOL 4 YL] 2 METHYLBENZONITRILE; 3 [3 (BIPHENYL 4 YL) 5 ETHYL 4H 1,2,4 TRIAZOL 4 YL] 2 METHYLPHENOL; 3 [3 (BIPHENYL 4 YL) 5 ETHYL 4H 1,2,4 TRIAZOL 4 YL] N,N,2 TRIMETHYLANILINE; 3 [3 ETHYL 5 (6 PHENYLPYRIDIN 3 YL) 4H 1,2,4 TRIAZOL 4 YL] 2 METHYLBENZAMIDE; 3 [3 ETHYL 5 (6 PHENYLPYRIDIN 3 YL) 4H 1,2,4 TRIAZOL 4 YL] 2 METHYLMETHYLBENZONITRILE; 3 [3 ETHYL 5 (6 PHENYLPYRIDIN 3 YL) 4H 1,2,4 TRIAZOL 4 YL] 2METHYLBENZONITRILE; 3 BIPHENYL 4 YL 4 (3 BROMO 2 METHYLPHENYL) 5 ETHYL 4H 1,2,4 TRIAZOLE; 3 BIPHENYL 4 YL 5 ETHYL 4 (2 METHYL 3 NITROPHENYL) 4H 1,2,4 TRIAZOLE; 3 BIPHENYL 4 YL 5 ETHYL 4 (2 METHYLPHENYL) 4H [1,2,4]TRIAZOLE; 3 BIPHENYL 4 YL 5 ETHYL 4 (3 CHLORO 2 METHYLPHENYL) 4H [1,2,4]TRIAZOLE; 3 BIPHENYL 4 YL 5 ETHYL 4 (3 FLUORO 2 METHYLPHENYL) 4H [1,2,4]TRIAZOLE; 3 BIPHENYL 4 YL 5 ETHYL 4 [2 METHYL 3 (TRIFLUOROMETHYL)PHENYL] 4H 1,2,4 TRIAZOLE; 4 [3 [(BENZYLOXY)METHYL] 2 METHYLPHENYL] 3 (BIPHENYL 4 YL) 5 ETHYL 4H 1,2,4 TRIAZOLE; 4 BENZYLOXY 3,5 DIMETHOXY N [1 (DIMETHYLAMINOCYCLOPENTYL)METHYL]BENZAMIDE; [3 [3 (BIPHENYL 4 YL) 5 ETHYL 4H 1,2,4 TRIAZOL 4 YL] 2 METHYLPHENYL]ACETONITRILE; [3 [3 (BIPHENYL 4 YL) 5 ETHYL 4H 1,2,4 TRIAZOL 4 YL] 2 METHYLPHENYL]METHANOL; GLYCINE TRANSPORTER 1; GLYCINE TRANSPORTER 1 INHIBITOR; METHYL 3 [3 (BIPHENYL 4 YL) 5 ETHYL 4H 1,2,4 TRIAZOL 4 YL] 2 METHYLBENZOATE; ORG 25543; PROTEIN INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; ARTICLE; CELL MEMBRANE PERMEABILITY; CONTROLLED STUDY; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SELECTIVITY; DRUG SOLUBILITY; DRUG STABILITY; DRUG SYNTHESIS; EXPERIMENTAL MONKEY; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN CELL; HYPERACTIVITY; IC 50; IN VITRO STUDY; IN VIVO STUDY; ISOMER; LIPOPHILICITY; LIVER MICROSOME METABOLISM; LOCOMOTION; MALE; MAZE TEST; MEMORY DISORDER; MOUSE; NONHUMAN; PHYSICAL CHEMISTRY; PLASMA PROTEIN BINDING; RAT; REACTION OPTIMIZATION; STRUCTURE ACTIVITY RELATION; THERMOSTABILITY; WORKING MEMORY;

ANIMALS; DIZOCILPINE MALEATE; FEMALE; GLYCINE PLASMA MEMBRANE TRANSPORT PROTEINS; HUMANS; MALE; MAZE LEARNING; MICE; MICE, INBRED ICR; RATS; RATS, WISTAR; STRUCTURE-ACTIVITY RELATIONSHIP; TRIAZOLES;

EID: 84880892418     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm400383w     Document Type: Article

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