Synthesis and optimization of arylsulfonylpiperazines as a novel class of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1)

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 5, 2009, Pages 1522-1527

  Sun, Daqing ^a   Wang, Zhulun ^a   Cardozo, Mario ^a   Choi, Rebekah ^a   DeGraffenreid, Michael ^a   Di, Yongmei ^a   He, Xiao ^a   Jaen, Juan C ^a   Labelle, Marc ^a   Liu, Jinsong ^a   Ma, Ji ^a   Miao, Shichang ^a   Sudom, Athena ^a   Tang, Liang ^a   Tu, Hua ^a   Ursu, Stefania ^a   Walker, Nigel ^a   Yan, Xuelei ^a   Ye, Qiuping ^a   Powers, Jay P ^a  

^a AMGEN INC   (United States)

Author keywords

11 HSD1; 11 HSD2; Arylsulfonylpiperazines; Diabetes; Hydroxysteroid dehydrogenase; Metabolic syndrome

Indexed keywords

11BETA HYDROXYSTEROID DEHYDROGENASE 1; 11BETA HYDROXYSTEROID DEHYDROGENASE 1 INHIBITOR; ENZYME INHIBITOR; PIPERAZINE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG DOSE COMPARISON; DRUG DOSE INCREASE; DRUG POTENCY; DRUG SCREENING; DRUG SELECTIVITY; DRUG SYNTHESIS; DRUG TISSUE LEVEL; ENZYME INHIBITION; EX VIVO STUDY; HUMAN; HUMAN CELL; MONKEY; NONHUMAN; STRUCTURE ACTIVITY RELATION;

11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1; ADMINISTRATION, ORAL; ANIMALS; ARYLSULFONIC ACIDS; BIOLOGICAL AVAILABILITY; CELL LINE; CRYSTALLOGRAPHY, X-RAY; ENZYME STABILITY; HUMANS; MACACA FASCICULARIS; MICE; PIPERAZINES; RATS; STRUCTURE-ACTIVITY RELATIONSHIP;

MACACA FASCICULARIS;

EID: 60449092400     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.12.114     Document Type: Article

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