Discovery of novel, potent benzamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) exhibiting oral activity in an enzyme inhibition ex vivo model

Journal of Medicinal Chemistry

Volumn 51, Issue 13, 2008, Pages 3953-3960

  Julian, Lisa D ^a   Wang, Zhulun ^a   Bostick, Tracy ^b   Caille, Seb ^a   Choi, Rebekah ^a   DeGraffenreid, Michael ^a   Di, Yongmei ^a   He, Xiao ^a   Hungate, Randall W ^a   Jaen, Juan C ^c   Liu, Jinsong ^a   Monshouwer, Mario ^d   McMinn, Dustin ^a   Rew, Yosup ^a   Sudom, Athena ^a   Sun, Daqing ^a   Tu, Hua ^a   Ursu, Stefania ^a   Walker, Nigel ^a   Yan, Xuelei ^a   Ye, Qiuping ^a   Powers, Jay P ^c   more..

^a AMGEN INC   (United States)

^b GENENTECH INC   (United States)

^c ChemoCentryx Inc   (United States)

^d Roche   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

11BETA HYDROXYSTEROID DEHYDROGENASE; 11BETA HYDROXYSTEROID DEHYDROGENASE 1; 11BETA HYDROXYSTEROID DEHYDROGENASE 1 INHIBITOR; BENZAMIDE DERIVATIVE; ENZYME INHIBITOR; N [4 (2 CYANOETHYL)CYCLOHEXYL] 4 (1,1,1 TRIFLUORO 2 HYDROXYPROPAN 2 YL) N CYCLOPROPYLBENZAMIDE; N [4 (4 CYANOPHENYL)CYCLOHEXYL] 4 (1,1,1 TRIFLUORO 2 HYDROXYPROPAN 2 YL) N CYCLOPROPYLBENZAMIDE; N [4 (PYRIDIN 3 YL)]CYCLOHEXYL 4 (1,1,1 TRIFLUORO 2 HYDROXYPROPAN 2 YL) N CYCLOPROPYLBENZAMIDE;

ADIPOSE TISSUE; ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CELL STRAIN HEK293; CORRELATION ANALYSIS; DOG; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG EFFECT; DRUG HALF LIFE; DRUG POTENCY; DRUG TISSUE LEVEL; ENZYME ACTIVITY; ENZYME INHIBITION; HUMAN; HUMAN CELL; IC 50; MONKEY; NONHUMAN; PROCESS OPTIMIZATION; PROTON NUCLEAR MAGNETIC RESONANCE; RAT; X RAY CRYSTALLOGRAPHY;

11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1; ADMINISTRATION, ORAL; ANIMALS; BENZAMIDES; CELL LINE; CRYSTALLOGRAPHY, X-RAY; DOGS; ENZYME INHIBITORS; HUMANS; MACACA FASCICULARIS; MODELS, ANIMAL; MODELS, MOLECULAR; MOLECULAR STRUCTURE; RATS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 46849085801     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm800310g     Document Type: Article

References (32)

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