(Z)-2-(2-bromophenyl)-3-{[4-(1-methyl-piperazine)amino]phenyl}acrylonitrile (DG172): An orally bioavailable PPARβ/δ-selective ligand with inverse agonistic properties

Journal of Medicinal Chemistry

Volumn 55, Issue 6, 2012, Pages 2858-2868

  Lieber, Sonja ^a   Scheer, Frithjof ^a   Meissner, Wolfgang ^a   Naruhn, Simone ^a   Adhikary, Till ^a   Müller Brüsselbach, Sabine ^a   Diederich, Wibke E ^a   Müller, Rolf ^a  

^a PHILIPPS UNIVERSITY MARBURG   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

2 (2 BROMOPHENYL) 3 [4 (4 METHYLPIPERAZIN 1 YL)PHENYL] ACRYLONITRILE DIHYDROCHLORIDE; 2 (2 BROMOPHENYL) 3 [4 (DIMETHYLAMINO)PHENYL]ACRYLONITRILE; 2 (2 BROMOPHENYL) 3 [[4 (1 METHYL PIPERAZINE)AMINO]PHENYL] ACRYLONITRILE; 2 (2 CHLOROPHENYL) 3 [4 (DIMETHYLAMINO)PHENYL]ACRYLONITRILE; 2 (3 CHLOROPHENYL) 3 [4 (DIMETHYLAMINO)PHENYL]ACRYLONITRILE; 2 (4 CHLOROPHENYL) 3 [4 (DIMETHYLAMINO)PHENYL]ACRYLONITRILE; 2 [4 [2 [3 CYCLOHEXYL 1 (4 CYCLOHEXYLBUTYL)UREIDO]ETHYL]PHENYLTHIO] 2 METHYLPROPIONIC ACID; 2 PHENYL 3 [4 (PHENYLAMINO)PHENYL]ACRYLONITRILE; 2 PHENYL 3 [4 (PIPERAZIN 1 YL)PHENYL]ACRYLONITRILE; 2 PHENYL 3 [4 (PIPERIDIN 1 YL)PHENYL]ACRYLONITRILE; 3 [4 (4 METHYLPIPERAZIN 1 YL)PHENYL] 2 PHENYLACRYLONITRILE; 3 [4 (4 METHYLPIPERIDIN 1 YL)PHENYL] 2 PHENYLACRYLONITRILE; 3 [4 (CYCLOHEXYLAMINO)PHENYL] 2 PHENYLACRYLONITRILE; 3 [4 (DIMETHYLAMINO)PHENYL] 2 (2 (TRIFLUOROMETHYL)PHENYL) ACRYLONITRILE; 3 [4 (DIMETHYLAMINO)PHENYL] 2 (2 FLUOROPHENYL)ACRYLONITRILE; 3 [4 (DIMETHYLAMINO)PHENYL] 2 (2 IODOPHENYL)ACRYLONITRILE; 3 [4 (DIMETHYLAMINO)PHENYL] 2 (2 METHOXYPHENYL) ACRYLONITRILE; 3 [4 [(DIMETHYLAMINO)METHYL]PHENYL] 2 PHENYLACRYLONITRILE HYDROCHLORIDE; 4 [4 [3 (4 ACETYL 3 HYDROXY 2 PROPYLPHENOXY)PROPOXY]PHENOXY]ACETIC ACID; [2 METHYL 4 [4 METHYL 2 (4 TRIFLUOROMETHYLPHENYL) 5 THIAZOLYLMETHYLTHIO]PHENOXY]ACETIC ACID; DG 172; N (2 BENZOYLPHENYL) O [2 (METHYL 2 PYRIDINYLAMINO)ETHYL]TYROSINE; NSC 636948; NSC 667251; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR ANTAGONIST; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR DELTA; PTS 58; UNCLASSIFIED DRUG;

ANGPTL4 GENE; ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; CLINICAL DATA REPOSITORY; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG DESIGN; DRUG DETERMINATION; DRUG POTENCY; DRUG SCREENING; FLUORESCENCE RESONANCE ENERGY TRANSFER; GENE; GENETIC TRANSCRIPTION; HEALTH PROGRAM; HUMAN; HUMAN CELL; IC 50; INVERSE AGONISM; LIGAND BINDING; MAXIMUM PLASMA CONCENTRATION; MOLECULAR INTERACTION; MOUSE; MYOBLAST; NATIONAL COUNCIL LICENSURE EXAMINATION; NATIONAL HEALTH ORGANIZATION; NONHUMAN; PROGRAM DEVELOPMENT; RECEPTOR DOWN REGULATION; STRUCTURE ACTIVITY RELATION;

ACRYLONITRILE; ADMINISTRATION, ORAL; ANIMALS; BINDING, COMPETITIVE; BIOLOGICAL AVAILABILITY; CHROMATIN; CO-REPRESSOR PROTEINS; DRUG INVERSE AGONISM; FLUORESCENCE RESONANCE ENERGY TRANSFER; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; LIGANDS; MALE; MICE; MYOBLASTS; PIPERAZINES; PPAR GAMMA; PPAR-BETA; SMALL MOLECULE LIBRARIES; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; TRANSCRIPTION, GENETIC;

EID: 84858728715     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm2017122     Document Type: Article

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