2. Academic Validation
  3. Synthesis and biological evaluation of cyclic sulfamide derivatives as 11β-hydroxysteroid dehydrogenase 1 inhibitors

Synthesis and biological evaluation of cyclic sulfamide derivatives as 11β-hydroxysteroid dehydrogenase 1 inhibitors

  • ACS Med Chem Lett. 2012 Jan 17;3(2):88-93. doi: 10.1021/ml200226x.
Se Hoan Kim 1,  Ju Han Bok 2,  Jae Hong Lee 1,  Il Hyang Kim 1,  Sung Wook Kwon 1,  Gui Bin Lee 2,  Seung Kyu Kang 2,  Ji Seon Park 2,  Won Hoon Jung 2,  Hee Yeon Kim 2,  Sang Dal Rhee 2,  Sung Hoon Ahn 2,  Myung Ae Bae 2,  Deok Chan Ha 3,  Ki Young Kim 2,  Jin Hee Ahn 2
Affiliations

Affiliations

  • 1 Bio-Organic Science Division, Korea Research Institute of Chemical Technology , Yuseong-Gu, Daejeon, 305-600, Korea ; Department of Chemistry, Korea University , Sungbuk-gu, Seoul 136-701, Korea.
  • 2 Bio-Organic Science Division, Korea Research Institute of Chemical Technology , Yuseong-Gu, Daejeon, 305-600, Korea.
  • 3 Department of Chemistry, Korea University , Sungbuk-gu, Seoul 136-701, Korea.
PMID: 24900439 DOI: 10.1021/ml200226x
Abstract

A new series of cyclic sulfamide derivatives were synthesized and evaluated for their ability to inhibit 11β-HSD1. Among this series, 18e showed good in vitro activity toward human 11β-HSD1, selectivity against 11β-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.

Keywords

11β-hydroxysteroid dehydrogenase type 1; adamantyl group; antidiabetic agents; cyclic sulfamide; diabetes.

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