Synthesis and Biological Evaluation of Cyclic Sulfamide Derivatives as 11 beta-Hydroxysteroid Dehydrogenase 1 Inhibitors

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

doi:10.1021/ml200226x

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Synthesis and Biological Evaluation of Cyclic Sulfamide Derivatives as 11 beta-Hydroxysteroid Dehydrogenase 1 Inhibitors

Kim, Se Hoan;
Bok, Ju Han;
Lee, Jae Hong;
Kim, Il Hyang;
Kwon, Sung Wook;
외 11명

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19

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23

초록

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.

키워드

diabetes; antidiabetic agents; 11 beta-hydroxysteroid dehydrogenase type 1; cyclic sulfamide; adamantyl group; 11-BETA-HSD1 INHIBITORS; METABOLIC SYNDROME; VISCERAL OBESITY; TYPE-1; MICE; HYPERGLYCEMIA

제목: Synthesis and Biological Evaluation of Cyclic Sulfamide Derivatives as 11 beta-Hydroxysteroid Dehydrogenase 1 Inhibitors

저자: 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

DOI: 10.1021/ml200226x

발행일: 2012-02

유형: Article

저널명: ACS Medicinal Chemistry Letters

권: 3

호: 2

페이지: 88 ~ 93