Identification of trisubstituted-pyrazol carboxamide analogs as novel and potent antagonists of farnesoid X receptor

Bioorganic and Medicinal Chemistry

Volumn 22, Issue 11, 2014, Pages 2919-2938

  Yu, Donna D ^a   Lin, Wenwei ^b   Forman, Barry M ^a   Chen, Taosheng ^b  

^a CITY OF HOPE NATIONAL MEDICAL CENTER   (United States)

^b ST JUDE CHILDREN S RESEARCH HOSPITAL   (United States)

Author keywords

Abbreviations; BAs; bile acids; bile salt export pump; BSEP; Cyp7A1; cytochrome 7A1; farnesoid X receptor; FXR; high throughput screen; HTS; LBD; ligand binding domain; NRs; nuclear receptors; SAR; structure activity relationship

Indexed keywords

1 (2,3 DIHYDRO 1H INDEN 1 YL) 3 (PARA TOLYL) 1H PYRAZOLE 4 CARBALDEHYDE; 1 (2,4 DICHLOROPHENYL) 2 (1 PARA TOLYLETHYLIDENE)HYDRAZINE; 1 (2,4 DICHLOROPHENYL) 3 PARA TOLYL 1H PYRAZOLE 4 CARBALDEHYDE; 1 (2,4 DICHLOROPHENYL) 3 PARA TOLYL 1H PYRAZOLE 4 CARBOXYLIC ACID; 1 (2,4 DICHLOROPHENYL) N [4 METHYL 3 (MORPHOLINOSULFONYL)PHENYL] 3 (PARA TOLYL) 1H PYRAZOLE 4 CARBOXAMIDE; 1 (3 CHLOROPHENYL) 2 (1 PARA TOLYLETHYLIDENE)HYDRAZINE; 1 (3 CHLOROPHENYL) 3 PARA TOLYL 1H PYRAZOLE 4 CARBALDEHYDE; 1 (3 CHLOROPHENYL) 3 PARA TOLYL 1H PYRAZOLE 4 CARBOXYLIC ACID; 1 (3 CHLOROPHENYL) N [4 METHYL 3 (MORPHOLINOSULFONYL)PHENYL] 3 (PARA TOLYL) 1H PYRAZOLE 4 CARBOXAMIDE; 1 (3 METHOXYBENZYL) 3 (3 METHOXYPHENYL) N [4 METHYL 3 (MORPHOLINOSULFONYL)PHENYL] 1H PYRAZOLE 4 CARBOXAMIDE; 1 (3 TRIFLUROMETHYLPHENYL) 2 (1 PARA TOLYLETHYLIDENE)HYDRAZINE; 1 (4 FLUOROPHENYL) 2 (1 PARA TOLYLETHYLIDENE)HYDRAZINE; 1 (4 FLUOROPHENYL) 3 PARA TOLYL 1H PYRAZOLE 4 CARBALDEHYDE; 1 (4 FLUOROPHENYL) 3 PARA TOLYL 1H PYRAZOLE 4 CARBOXYLIC ACID; 1 (4 FLUOROPHENYL) N [4 METHYL 3 (MORPHOLINOSULFONYL)PHENYL] 3 PARA TOLYL 1H PYRAZOLE 4 CARBOXAMIDE; 1 (BENZO[D]THIAZOL 2 YL) N [4 METHYL 3 (MORPHOLINOSULFONYL)PHENYL] 3 (PARA TOLYL) 1H PYRAZOLE 4 CARBOXAMIDE; 1 BUTYL N [4 METHYL 3 (MORPHOLINOSULFONYL)PHENYL] 3 (PARA TOLYL) 1H PYRAZOLE 4 CARBOXAMIDE; 1 ISOPROPYL N [4 METHYL 3 (MORPHOLINOSULFONYL)PHENYL] 3 (PARA TOLYL) 1H PYRAZOLE 4 CARBOXAMIDE; 2 [2 [1 (PARA TOLYL)ETHYLIDENE]HYDRAZINYL]BENZO[D]THIAZOLE; 3 (PARA TOLYL) 1 (3 (TRIFLUOROMETHYL)PHENYL) 1H PYRAZOLE 4 CARBOXYLIC ACID; 3 PARA TOLYL 1 [3 (TRIFLUOROMETHYL)PHENYL] 1H PYRAZOLE 4 CARBALDEHYDE; AMIDE; CARBOXYLIC ACID; CHEMICAL COMPOUND; FARNESOID X RECEPTOR; HORMONE RECEPTOR BLOCKING AGENT; HYDRAZINE; N [4 METHYL 3 (MORPHOLINOSULFONYL)PHENYL] 3 (PARA TOLYL) 1 [3 (TRIFLUOROMETHYL) PHENYL] 1H PYRAZOLE 4 CARBOXAMIDE; THIAZOLE; UNCLASSIFIED DRUG; UNINDEXED DRUG; CELL RECEPTOR; FARNESOID X-ACTIVATED RECEPTOR; PYRAZOLE DERIVATIVE;

ARTICLE; BINDING AFFINITY; CONCENTRATION RESPONSE; CONTROLLED STUDY; CYTOTOXICITY ASSAY; DRUG IDENTIFICATION; DRUG RECEPTOR BINDING; DRUG SCREENING; DRUG SYNTHESIS; DRUG TOXICITY; FLUORESCENCE RESONANCE ENERGY TRANSFER; IC 50; PHYSICAL CHEMISTRY; PROTEIN BINDING; RECEPTOR BINDING ASSAY; STRUCTURE ACTIVITY RELATION; TRANSACTIVATION ASSAY; ANTAGONISTS AND INHIBITORS; CHEMICAL STRUCTURE; CHEMISTRY; DOSE RESPONSE; HEK293 CELL LINE; HUMAN; SYNTHESIS;

AMIDES; DOSE-RESPONSE RELATIONSHIP, DRUG; HEK293 CELLS; HUMANS; MOLECULAR STRUCTURE; PYRAZOLES; RECEPTORS, CYTOPLASMIC AND NUCLEAR; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84899938747     PISSN: 09680896     EISSN: 14643391     Source Type: Journal    
DOI: 10.1016/j.bmc.2014.04.014     Document Type: Article

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