Bioorg Med Chem Lett. 2010 Feb 1;20(3):881-6. Epub 2010 Jan 4.

Spirocyclic ureas: orally bioavailable 11 beta-HSD1 inhibitors identified by computer-aided drug design.

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Vitae Pharmaceuticals, 502 West Office Center Drive, Fort Washington, PA 19034, USA.

Abstract

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.

PMID:: 20064717; [PubMed - indexed for MEDLINE]

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