Discovery and optimization of piperidyl benzamide derivatives as a novel class of 11β-HSD1 inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 6, 2009, Pages 1797-1801

  Rew, Yosup ^a   McMinn, Dustin L ^a   Wang, Zhulun ^a   He, Xiao ^a   Hungate, Randall W ^a   Jaen, Juan C ^a   Sudom, Athena ^a   Sun, Daqing ^a   Tu, Hua ^a   Ursu, Stefania ^a   Villemure, Elisia ^a   Walker, Nigel P C ^a   Yan, Xuelei ^a   Ye, Qiuping ^a   Powers, Jay P ^a  

^a AMGEN INC   (United States)

Author keywords

11 HSD1; Cyclohexyl benzamide; Hepatocyte stability; Insulin sensitivity; Microsomal stability; Piperidyl benzamide; PXR; Type II diabetes

Indexed keywords

11BETA HYDROXYSTEROID DEHYDROGENASE; ANTIDIABETIC AGENT; BENZAMIDE DERIVATIVE; OXIDOREDUCTASE INHIBITOR; RIFAMPICIN;

ANIMAL CELL; ARTICLE; CONTROLLED STUDY; CRYSTAL STRUCTURE; CYTOTOXICITY; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG METABOLISM; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SOLUBILITY; DRUG STABILITY; HUMAN; HUMAN CELL; IC 50; LIVER MICROSOME METABOLISM; NONHUMAN; PLASMA CLEARANCE; RAT; STRUCTURE ACTIVITY RELATION;

11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1; BENZAMIDES; CRYSTALLOGRAPHY, X-RAY; DIABETES MELLITUS, TYPE 2; DRUG DESIGN; HEPATOCYTES; HUMANS; INHIBITORY CONCENTRATION 50; INSULIN; MICROSOMES; MODELS, CHEMICAL; MOLECULAR STRUCTURE; PIPERIDINES; SOLUBILITY; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 61349172663     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.01.058     Document Type: Article

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