| Literature DB >> 16996734 |
Bryan Sorensen1, Jeff Rohde, Jiahong Wang, Steven Fung, Katina Monzon, William Chiou, Liping Pan, Xiaoqing Deng, DeAnne Stolarik, Ernst U Frevert, Peer Jacobson, J T Link.
Abstract
A series of potent and selective adamantane aminoamide 11-beta-HSD-1 inhibitors has been optimized. Chemically these studies were expedited by utilizing readily obtained amino acids as starting materials or an isocyanide multicomponent reaction. Structure-activity relationship studies resulted in the discovery of dual human and mouse 11-beta-HSD-1 potent and selective inhibitors like adamantane 11 and related compounds with high metabolic stability and robust pharmacokinetic profiles.Entities:
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Year: 2006 PMID： 16996734 DOI： 10.1016/j.bmcl.2006.08.129
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823