Further studies with the 2-amino-1,3-thiazol-4(5H)-one class of 11β-hydroxysteroid dehydrogenase type 1 inhibitors: Reducing pregnane X receptor activity and exploring activity in a monkey pharmacodynamic model

Journal of Medicinal Chemistry

Volumn 51, Issue 24, 2008, Pages 7953-7967

  Fotsch, Christopher ^a   Bartberger, Michael D ^a   Bercot, Eric A ^a   Chen, Michelle ^a   Cupples, Rod ^a   Emery, Maury ^a   Fretland, Jenne ^a   Guram, Anil ^a   Hale, Clarence ^a   Han, Nianhe ^a   Hickman, Dean ^a   Hungate, Randall W ^a   Hayashi, Michael ^a   Komorowski, Renee ^a   Liu, Qingyian ^a   Matsumoto, Guy ^a   St Jean Jr , David J ^a   Ursu, Stefania ^a   Véniant, Murielle ^a   Xu, Guifen ^a   Ye, Qiuping ^a   Yuan, Chester ^a   Zhang, Jiandong ^a   Zhang, Xiping ^a   Tu, Hua ^a   Wang, Minghan ^a   more..

^a AMGEN INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

11BETA HYDROXYSTEROID DEHYDROGENASE 1; 2 [ 1 (4 FLUOROPHENYL)ETHYLAMINO] 5 (2 HYDROXYPROPAN 2 YL) 5 METHYLTHIAZOL 4(5H) ONE; 2 AMINO 1,3 THIAZOL 4(5H) ONE; ALCOHOL DERIVATIVE; AMIDE; PREGNANE X RECEPTOR; RIFAMPICIN; THIAZOLE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CHO CELL; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG CLEARANCE; DRUG EFFICACY; DRUG HALF LIFE; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG STRUCTURE; ENZYME ACTIVITY; ENZYME INHIBITION; HUMAN; HUMAN CELL; LIVER CELL; MONKEY; NONHUMAN; PHARMACODYNAMICS; PROTEIN EXPRESSION; SPECIES DIFFERENCE; STRUCTURE ACTIVITY RELATION; UPREGULATION;

11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1; ANIMALS; CHEMISTRY, PHARMACEUTICAL; CRYSTALLOGRAPHY, X-RAY; CYTOCHROME P-450 CYP3A; DRUG DESIGN; ENZYME INHIBITORS; HUMANS; KINETICS; MACACA FASCICULARIS; MALE; MODELS, MOLECULAR; MOLECULAR CONFORMATION; RECEPTORS, STEROID; TISSUE DISTRIBUTION;

EID: 58149087619     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm801073z     Document Type: Article

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