National Center for
3PDJ: Crystal Structure Of Human 11-Beta-Hydroxysteroid Dehydrogenase 1 (11b-Hsd1) In Complex With 4,4-Disubstituted Cyclohexylbenzamide Inhibitor
Synthesis and optimization of novel 4,4-disubstituted cyclohexylbenzamide derivatives as potent 11beta-HSD1 inhibitors
Bioorg. Med. Chem. Lett. (2011) 21 p.405-410
The synthesis and SAR of a series of 4,4-disubstituted cyclohexylbenzamide inhibitors of 11beta-HSD1 are described. Optimization rapidly led to potent, highly selective, and orally bioavailable inhibitors demonstrating efficacy in both rat and non-human primate ex vivo pharmacodynamic models.