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Bioorg Med Chem Lett
; 20(3): 881-6, 2010 Feb 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-20064717
RESUMO
Structure-guided drug design led to the identification of a class of spirocyclic ureas which potently inhibit human 11beta-HSD1 in vitro. Lead compound 10j was shown to be orally bioavailable in three species, distributed into adipose tissue in the mouse, and its (R) isomer 10j2 was efficacious in a primate pharmacodynamic model.