Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1375576 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
Novel 4,4-disubstituted cyclohexylbenzamide inhibitors of 11β-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 11β-HSD1 in a rat pharmacodynamic model (ED50 = 10 mg/kg).
Graphical abstractNovel 4,4-disubstituted cyclohexylbenzamide inhibitors of 11β-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 11β-HSD1 in a rat pharmacodynamic model (ED50 = 10 mg/Kg).Figure optionsDownload full-size imageDownload as PowerPoint slide