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

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

Research output: Contribution to journalArticlepeer-review

15 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)88-93
Number of pages6
JournalACS Medicinal Chemistry Letters
Volume3
Issue number2
DOIs
Publication statusPublished - 2012 Feb 9

Keywords

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

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry

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