| Literature DB >> 21093258 |
Daqing Sun1, Zhulun Wang, Seb Caille, Michael DeGraffenreid, Felix Gonzalez-Lopez de Turiso, Randall Hungate, Juan C Jaen, Ben Jiang, Lisa D Julian, Ron Kelly, Dustin L McMinn, Jacob Kaizerman, Yosup Rew, Athena Sudom, Hua Tu, Stefania Ursu, Nigel Walker, Maren Willcockson, Xuelei Yan, Qiuping Ye, Jay P Powers.
Abstract
The synthesis and SAR of a series of 4,4-disubstituted cyclohexylbenzamide inhibitors of 11β-HSD1 are described. Optimization rapidly led to potent, highly selective, and orally bioavailable inhibitors demonstrating efficacy in both rat and non-human primate ex vivo pharmacodynamic models.Entities:
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Year: 2010 PMID： 21093258 DOI： 10.1016/j.bmcl.2010.10.129
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823