1145688-40-9Relevant academic research and scientific papers
Optimization of novel di-substituted cyclohexylbenzamide derivatives as potent 11β-HSD1 inhibitors
McMinn, Dustin L.,Rew, Yosup,Sudom, Athena,Caille, Seb,DeGraffenreid, Michael,He, Xiao,Hungate, Randall,Jiang, Ben,Jaen, Juan,Julian, Lisa D.,Kaizerman, Jacob,Novak, Perry,Sun, Daqing,Tu, Hua,Ursu, Stefania,Walker, Nigel P.C.,Yan, Xuelei,Ye, Qiuping,Wang, Zhulun,Powers, Jay P.
scheme or table, p. 1446 - 1450 (2010/01/16)
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).
