1219012-03-9Relevant articles and documents
Spirocyclic ureas: Orally bioavailable 11β-HSD1 inhibitors identified by computer-aided drug design
Tice, Colin M.,Zhao, Wei,Xu, Zhenrong,Cacatian, Salvacion T.,Simpson, Robert D.,Ye, Yuan-Jie,Singh, Suresh B.,McKeever, Brian M.,Lindblom, Peter,Guo, Joan,Krosky, Paula M.,Kruk, Barbara A.,Berbaum, Jennifer,Harrison, Richard K.,Johnson, Judith J.,Bukhtiyarov, Yuri,Panemangalore, Reshma,Scott, Boyd B.,Zhao, Yi,Bruno, Joseph G.,Zhuang, Linghang,McGeehan, Gerard M.,He, Wei,Claremon, David A.
scheme or table, p. 881 - 886 (2010/09/11)
Structure-guided drug design led to the identification of a class of spirocyclic ureas which potently inhibit human 11β-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.
