| Literature DB >> 20064717 |
Colin M Tice1, 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.
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. Copyright (c) 2009 Elsevier Ltd. All rights reserved.Entities:
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Year: 2010 PMID： 20064717 DOI： 10.1016/j.bmcl.2009.12.082
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823