Pyrazole[3,4-e][1,4]thiazepin-7-one derivatives as a novel class of Farnesoid X Receptor (FXR) agonists

Bioorganic and Medicinal Chemistry

Volumn 20, Issue 11, 2012, Pages 3429-3445

  Marinozzi, Maura ^a   Carotti, Andrea ^a   Sansone, Emanuele ^a   MacChiarulo, Antonio ^a   Rosatelli, Emiliano ^a   Sardella, Roccaldo ^a   Natalini, Benedetto ^a   Rizzo, Giovanni ^b   Adorini, Luciano ^b   Passeri, Daniela ^b   De Franco, Francesca ^b   Pruzanski, Mark ^b   Pellicciari, Roberto ^a  

^a UNIVERSITY OF PERUGIA   (Italy)

^b INTERCEPT PHARMACEUTICALS   (United States)

Author keywords

1H Pyrazole 3,4 e 1,4 thiazepin 7 one; Farnesoid X Receptor (FXR); Heterocyclic chemistry; Non steroidal FXR agonist; Virtual screening

Indexed keywords

4 (2' METHOXYBIPHENYL 4 YL) 3,6 DIMETHYL 1 (2 METHYLPHENYL) 4,8 DIHYDRO 1H PYRAZOLE[3,4 E][1,4]THIAZEPIN 7 ONE; 4 (3 METHOXY 4 PHENOXYPHENYL) 3,6 DIMETHYL 1 (2 METHYLPHENYL) 4,8 DIHYDRO 1H PYRAZOLE[3,4 E][1,4]THIAZEPIN 7 ONE; 4 (3' CARBOMETHOXYBIPHENYL 4 YL) 3,6 DIMETHYL 1 (2 METHYLPHENYL) 4,8 DIHYDRO 1H PYRAZOLE[3,4 E][1,4]THIAZEPIN 7 ONE; 4 (3' ETHOXYBIPHENYL 4 YL) 3,6 DIMETHYL 1 (2 METHYLPHENYL) 4,8 DIHYDRO 1H PYRAZOLE[3,4 E][1,4]THIAZEPIN 7 ONE; 4 (3' METHOXYBIPHENYL 4 YL) 3,6 DIMETHYL 1 (2 METHYLPHENYL) 4,8 DIHYDRO 1H PYRAZOLE[3,4 E][1,4]THIAZEPIN 7 ONE; 4 (4 PHENOXYPHENYL) 3,6 DIMETHYL 1 (2 ETHYLPHENYL) 4,8 DIHYDRO 1H PYRAZOLE[3,4 E][1,4]THIAZEPIN 7 ONE; 4 (4 PHENOXYPHENYL) 3,6 DIMETHYL 1 (2 METHYLPHENYL) 4,8 DIHYDRO 1H PYRAZOLE[3,4 E][1,4]THIAZEPIN 7 ONE; 4 (4 PHENOXYPHENYL) 3,6 DIMETHYL 1 (2 NPROPYLPHENYL) 4,8 DIHYDRO 1H PYRAZOLE[3,4 E][1,4]THIAZEPIN 7 ONE; 4 (4 PHENOXYPHENYL) 3,6 DIMETHYL 1 (3 METHYLPHENYL) 4,8 DIHYDRO 1H PYRAZOLE[3,4 E][1,4]THIAZEPIN 7 ONE; 4 (4 PHENOXYPHENYL) 3,6 DIMETHYL 1 (4 METHYLPHENYL) 4,8 DIHYDRO 1H PYRAZOLE[3,4 E][1,4]THIAZEPIN 7 ONE; 4 (4' CARBOMETHOXYBIPHENYL 4 YL) 3,6 DIMETHYL 1 (2 METHYLPHENYL) 4,8 DIHYDRO 1H PYRAZOLE[3,4 E][1,4]THIAZEPIN 7 ONE; 4 (4' METHOXYBIPHENYL 4 YL) 3,6 DIMETHYL 1 (2 METHYLPHENYL) 4,8 DIHYDRO 1H PYRAZOLE[3,4 E][1,4]THIAZEPIN 7 ONE; 4 [4 (2 BENZOFURAN)PHENYL] 3,6 DIMETHYL 1 (2 METHYLPHENYL) 4,8 DIHYDRO 1H PYRAZOLE[3,4 E][1,4]THIAZEPIN 7 ONE; 4 [4 (2 FURANYL)PHENYL] 3,6 DIMETHYL 1 (2 METHYLPHENYL) 4,8 DIHYDRO 1H PYRAZOLE[3,4 E][1,4]THIAZEPIN 7 ONE; 4 [4 (2 METHOXYPHENOXY)PHENYL] 3,6 DIMETHYL 1 (2 METHYLPHENYL) 4,8 DIHYDRO 1H PYRAZOLE[3,4 E][1,4]THIAZEPIN 7 ONE; 4 [4 (2 PHENYLVINYL)PHENYL] 3,6 DIMETHYL 1 (2 METHYLPHENYL) 4,8 DIHYDRO 1H PYRAZOLE[3,4 E][1,4]THIAZEPIN 7 ONE; 4 [4 (2 THIENYL)PHENYL] 3,6 DIMETHYL 1 (2 METHYLPHENYL) 4,8 DIHYDRO 1H PYRAZOLE[3,4 E][1,4]THIAZEPIN 7 ONE; 4 [4 (3 FURANYL)PHENYL] 3,6 DIMETHYL 1 (2 METHYLPHENYL) 4,8 DIHYDRO 1H PYRAZOLE[3,4 E][1,4]THIAZEPIN 7 ONE; 4 [4 (3 METHOXYPHENOXY)PHENYL] 3,6 DIMETHYL 1 (2 METHYLPHENYL) 4,8 DIHYDRO 1H PYRAZOLE[3,4 E][1,4]THIAZEPIN 7 ONE; 4 [4 (3 THIENYL)PHENYL] 3,6 DIMETHYL 1 (2 METHYLPHENYL) 4,8 DIHYDRO 1H PYRAZOLE[3,4 E][1,4]THIAZEPIN 7 ONE; 4 [4 (4 METHOXYPHENOXY)PHENYL] 3,6 DIMETHYL 1 (2 METHYLPHENYL) 4,8 DIHYDRO 1H PYRAZOLE[3,4 E][1,4]THIAZEPIN 7 ONE; 4 [4 (BENZYLOXY)PHENYL] 3,6 DIMETHYL 1 (2 METHYLPHENYL) 4,8 DIHYDRO 1H PYRAZOLE[3,4 E][1,4]THIAZEPIN 7 ONE; 4 BIPHENYL 4 YL 3,6 DIMETHYL 1 (2 METHYLPHENYL) 4,8 DIHYDRO 1H PYRAZOLE[3,4 E][1,4]THIAZEPIN 7 ONE; CHENODEOXYCHOLIC ACID; FARNESOID X RECEPTOR; LUCIFERASE; OBETICHOLIC ACID; PYRAZOLE[3,4 E][1,4]THIAZEPIN 7 ONE DERIVATIVE; THIAZEPINE DERIVATIVE; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ARTICLE; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG DESIGN; DRUG EFFICACY; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SCREENING; DRUG STRUCTURE; DRUG SYNTHESIS; STRUCTURE ACTIVITY RELATION; TRANSACTIVATION; VIRTUAL REALITY;

DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DESIGN; DRUG EVALUATION, PRECLINICAL; GENE EXPRESSION PROFILING; HEP G2 CELLS; HUMANS; LUCIFERASES; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PYRAZOLES; RECEPTORS, CYTOPLASMIC AND NUCLEAR; STRUCTURE-ACTIVITY RELATIONSHIP; THIAZEPINES; USER-COMPUTER INTERFACE;

HUMAN ECHOVIRUS 1;

EID: 84861192531     PISSN: 09680896     EISSN: 14643391     Source Type: Journal    
DOI: 10.1016/j.bmc.2012.04.021     Document Type: Article

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