期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 5, 页码 1446-1450出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.01.026
关键词
11 beta-HSD1; Diabetes; Metabolic syndrome; Hydroxysteroid dehydrogenase; Cardiovascular disease; Cyclohexylbenzamides
Novel 4,4-disubstituted cyclohexylbenzamide inhibitors of 11 beta-HSD1 were optimized to account for liabilities relating to in vitro pharmacokinetics, cytotoxicity and protein-related shifts in potency. A representative compound showing favorable in vivo pharmacokinetics was found to be an efficacious inhibitor of 11 beta-HSD1 in a rat pharmacodynamic model (ED(50) = 10 mg/kg). (C) 2009 Elsevier Ltd. All rights reserved.
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