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, Deok-Chan Ha, Hyae Gyeong Cheon, Ki Young Kim, Jin Hee Ahn

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26 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

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Keywords

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

ASJC Scopus subject areas

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

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