Discovery and biological evaluation of adamantyl amide 11β-HSD1 inhibitors

…, P Ward, M Binnie, E Craigie, KMM McConnell…

文献索引：Webster, Scott P.; Ward, Peter; Binnie, Margaret; Craigie, Eilidh; McConnell, Kirsty M.M.; Sooy, Karen; Vinter, Andy; Seckl, Jonathan R.; Walker, Brian R. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 10 p. 2838 - 2843

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被引用次数: 49

摘要

A series of adamantyl amide 11β-HSD1 inhibitors has been discovered and chemically modified. Selected compounds are selective for 11β-HSD1 over 11β-HSD2 and possess excellent cellular potency in human and murine 11β-HSD1 assays. Good pharmacodynamic characteristics are observed in ex vivo assays.