Identification of cyclicsulfonamide derivatives with an acetamide group as 11β-hydroxysteroid dehydrogenase 1 inhibitors

Se Hoan Kim, Sung Wook Kwon, So Young Chu, Jae Hong Lee, Banda Narsaiah, Chi Hyun Kim, Seung Kyu Kang, Nam Sook Kang, Sang Dal Rhee, Myung Ae Bae, Sung Hoon Ahn, Duck Chan Ha, Ki Young Kim, Jin Hee Ahn

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10 Citations (Scopus)

Abstract

In the continuation of our 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor research, cyclic sulfonamide derivatives with an acetamide group at the 2-position were synthesized and evaluated for their abilities to inhibit 11β-HSD1. Among this series, Compound 34 showed good in vitro activity toward human 11β-HSD1, selectivity against 11β-HSD2, microsomal stability, good pharmacokinetic and safety profiles human ether-a-go-go related gene (hERG and cytochrome P450 (CYP)). Also, a docking study explained the activity difference between human and mouse 11β-HSD1.

Original languageEnglish
Pages (from-to)46-52
Number of pages7
JournalChemical and Pharmaceutical Bulletin
Volume59
Issue number1
DOIs
Publication statusPublished - 2011 Jan

Keywords

  • 11β-hydroxysteroid dehydrogenase type 1
  • Anti-diabetic agent
  • Cyclic sulfonamide
  • Diabetes

ASJC Scopus subject areas

  • Chemistry(all)
  • Drug Discovery

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    Kim, S. H., Kwon, S. W., Chu, S. Y., Lee, J. H., Narsaiah, B., Kim, C. H., Kang, S. K., Kang, N. S., Rhee, S. D., Bae, M. A., Ahn, S. H., Ha, D. C., Kim, K. Y., & Ahn, J. H. (2011). Identification of cyclicsulfonamide derivatives with an acetamide group as 11β-hydroxysteroid dehydrogenase 1 inhibitors. Chemical and Pharmaceutical Bulletin, 59(1), 46-52. https://doi.org/10.1248/cpb.59.46