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Discovery and biological evaluation of adamantyl amide 11beta-HSD1 inhibitors |
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| Authors: | Webster Scott P Ward Peter Binnie Margaret Craigie Eilidh McConnell Kirsty M M Sooy Karen Vinter Andy Seckl Jonathan R Walker Brian R |
| Institution: | Endocrinology Unit, Centre for Cardiovascular Science, The Queen's Medical Research Institute, University of Edinburgh, 47 Little France Crescent, Edinburgh EH16 4TJ, UK. scott.webster@ed.ac.uk |
| Abstract: | A series of adamantyl amide 11beta-HSD1 inhibitors has been discovered and chemically modified. Selected compounds are selective for 11beta-HSD1 over 11beta-HSD2 and possess excellent cellular potency in human and murine 11beta-HSD1 assays. Good pharmacodynamic characteristics are observed in ex vivo assays. |
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