Synthesis and Biological Evaluation of Cyclic Sulfamide Derivatives as 11尾-Hydroxysteroid Dehydrogenase 1 Inhibitors
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- 作者：Se Hoan Kim ; Ju Han Bok ; Jae Hong Lee ; Il Hyang Kim ; Sung Wook Kwon ; Gui Bin Lee ; Seung Kyu Kang ; Ji Seon Park ; Won Hoon Jung ; Hee Yeon Kim ; Sang Dal Rhee ; Sung Hoon Ahn ; Myung Ae Bae ; Deok Chan Ha ; Ki Young Kim ; Jin Hee Ahn
- 刊名：ACS Medicinal Chemistry Letters
- 出版年：2012
- 出版时间：February 9, 2012
- 年：2012
- 卷：3
- 期：2
- 页码：88-93
- 全文大小：352K
- 年卷期：v.3,no.2(February 9, 2012)
- ISSN：1948-5875
文摘
A new series of cyclic sulfamide derivatives were synthesized and evaluated for their ability to inhibit 11尾-HSD1. Among this series, 18e showed good in vitro activity toward human 11尾-HSD1, selectivity against 11尾-HSD2, microsomal stability, and pharmacokinetic and safety profiles (hERG, CYP, and acute toxicity). Additionally, 18e exhibited good in vivo efficacy in rat and monkey models.