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Synthesis and Biological Evaluation of Cyclic Sulfamide Derivatives as 11 beta-Hydroxysteroid Dehydrogenase 1 Inhibitors
- Authors
- Kim, Se Hoan; Bok, Ju Han; Lee, Jae Hong; Kim, Il Hyang; Kwon, Sung Wook; Lee, Gui Bin; Kang, Seung Kyu; Park, Ji Seon; Jung, Won Hoon; Kim, Hee Yeon; Rhee, Sang Dal; Ahn, Sung Hoon; Bae, Myung Ae; Ha, Deok Chan; Kim, Ki Young; Ahn, Jin Hee
- Issue Date
- Feb-2012
- Publisher
- AMER CHEMICAL SOC
- Keywords
- diabetes; antidiabetic agents; 11 beta-hydroxysteroid dehydrogenase type 1; cyclic sulfamide; adamantyl group
- Citation
- ACS MEDICINAL CHEMISTRY LETTERS, v.3, no.2, pp.88 - 93
- Indexed
- SCIE
SCOPUS
- Journal Title
- ACS MEDICINAL CHEMISTRY LETTERS
- Volume
- 3
- Number
- 2
- Start Page
- 88
- End Page
- 93
- ISSN
- 1948-5875
- Abstract
- A new series of cyclic sulfamide derivatives were synthesized and evaluated for their ability to inhibit 11 beta-HSD1. Among this series, 18e showed good in vitro activity toward human 11 beta-HSD1, selectivity against 11 beta-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.
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