Adamantane 11-beta-HSD-1 inhibitors: Application of an isocyanide multicomponent reaction |
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| Authors: | Sorensen Bryan Rohde Jeff Wang Jiahong Fung Steven Monzon Katina Chiou William Pan Liping Deng Xiaoqing Stolarik DeAnne Frevert Ernst U Jacobson Peer Link J T |
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| Institution: | Metabolic Disease Research, Abbott, 100 Abbott Park Road, Abbott Park, IL 60064, USA. |
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| 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. |
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