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

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

  • Bioorg Med Chem Lett. 2010 Feb 1;20(3):881-6. doi: 10.1016/j.bmcl.2009.12.082.
Colin M Tice 1,  Wei Zhao,  Zhenrong Xu,  Salvacion T Cacatian,  Robert D Simpson,  Yuan-Jie Ye,  Suresh B Singh,  Brian M McKeever,  Peter Lindblom,  Joan Guo,  Paula M Krosky,  Barbara A Kruk,  Jennifer Berbaum,  Richard K Harrison,  Judith J Johnson,  Yuri Bukhtiyarov,  Reshma Panemangalore,  Boyd B Scott,  Yi Zhao,  Joseph G Bruno,  Linghang Zhuang,  Gerard M McGeehan,  Wei He,  David A Claremon
Affiliations

Affiliation

  • 1 Vitae Pharmaceuticals, 502 West Office Center Drive, Fort Washington, PA 19034, USA.
PMID: 20064717 DOI: 10.1016/j.bmcl.2009.12.082
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.

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