Discovery of cyclicsulfonamide derivatives as 11β-hydroxysteroid dehydrogenase 1 inhibitors

Se Hoan Kim, Ravirala Ramu, Sung Wook Kwon, Su Hee Lee, Chi Hyun Kim, Seung Kyu Kang, Sang Dal Rhee, Myung Ae Bae, Sung Hoon Ahn, Duck Chan Ha, Hyae Gyeong Cheon, Ki Young Kim, Jin Hee Ahn

Research output: Contribution to journalArticle

27 Citations (Scopus)

Abstract

A new series of cyclic sulfonamide derivatives was synthesized and evaluated for their ability to inhibit 11β-HSD1. Cyclic sulfonamides with phenylacetyl substituents at the 2-position showed nanomolar inhibitory activities. Among them, compound 4e exhibited a good in vitro inhibitory activity and selectivity toward human 11β-HSD2.

Original languageEnglish
Pages (from-to)1065-1069
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number3
DOIs
Publication statusPublished - 2010 Feb 1

Keywords

  • 11β-Hydroxysteroid dehydrogenase 1
  • Cyclic sulfonamide
  • Diabetes
  • Inhibitor

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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  • Cite this

    Kim, S. H., Ramu, R., Kwon, S. W., Lee, S. H., Kim, C. H., Kang, S. K., Rhee, S. D., Bae, M. A., Ahn, S. H., Ha, D. C., Cheon, H. G., Kim, K. Y., & Ahn, J. H. (2010). Discovery of cyclicsulfonamide derivatives as 11β-hydroxysteroid dehydrogenase 1 inhibitors. Bioorganic and Medicinal Chemistry Letters, 20(3), 1065-1069. https://doi.org/10.1016/j.bmcl.2009.12.035