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, Deok-Chan Ha, Ki Young Kim, Jin Hee Ahn

Research output: Contribution to journalArticle

9 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 1

Fingerprint

11-beta-Hydroxysteroid Dehydrogenases
Derivatives
Pharmacokinetics
Sulfonamides
Human Activities
Ether
Cytochrome P-450 Enzyme System
Genes
Safety
acetamide
Research

Keywords

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

ASJC Scopus subject areas

  • Drug Discovery
  • Chemistry(all)

Cite this

Identification of cyclicsulfonamide derivatives with an acetamide group as 11β-hydroxysteroid dehydrogenase 1 inhibitors. / Kim, Se Hoan; Kwon, Sung Wook; Chu, So Young; Lee, Jae Hong; Narsaiah, Banda; Kim, Chi Hyun; Kang, Seung Kyu; Kang, Nam Sook; Rhee, Sang Dal; Bae, Myung Ae; Ahn, Sung Hoon; Ha, Deok-Chan; Kim, Ki Young; Ahn, Jin Hee.

In: Chemical and Pharmaceutical Bulletin, Vol. 59, No. 1, 01.01.2011, p. 46-52.

Research output: Contribution to journalArticle

Kim, SH, Kwon, SW, Chu, SY, Lee, JH, Narsaiah, B, Kim, CH, Kang, SK, Kang, NS, Rhee, SD, Bae, MA, Ahn, SH, Ha, D-C, Kim, KY & Ahn, JH 2011, 'Identification of cyclicsulfonamide derivatives with an acetamide group as 11β-hydroxysteroid dehydrogenase 1 inhibitors', Chemical and Pharmaceutical Bulletin, vol. 59, no. 1, pp. 46-52. https://doi.org/10.1248/cpb.59.46
Kim, Se Hoan ; Kwon, Sung Wook ; Chu, So Young ; Lee, Jae Hong ; Narsaiah, Banda ; Kim, Chi Hyun ; Kang, Seung Kyu ; Kang, Nam Sook ; Rhee, Sang Dal ; Bae, Myung Ae ; Ahn, Sung Hoon ; Ha, Deok-Chan ; Kim, Ki Young ; Ahn, Jin Hee. / Identification of cyclicsulfonamide derivatives with an acetamide group as 11β-hydroxysteroid dehydrogenase 1 inhibitors. In: Chemical and Pharmaceutical Bulletin. 2011 ; Vol. 59, No. 1. pp. 46-52.
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