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 journalArticlepeer-review

    37 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

    Bibliographical note

    Funding Information:
    This research was supported by the Center for Biological Modulators of the 21st Century Frontier R&D Program , Ministry of Education, Science and Technology, Korea .

    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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