Modulation of 11β-hydroxysteroid dehydrogenase type 1 activity by 1,5-substituted 1H-tetrazoles

Scott P. Webster, Margaret Binnie, Kirsty M M McConnell, Karen Sooy, Peter Ward, Michael F. Greaney, Andy Vinter, T. David Pallin, Hazel J. Dyke, Matthew I A Gill, Ines Warner, Jonathan R. Seckl, Brian R. Walker

    Research output: Contribution to journalArticlepeer-review

    Abstract

    Inhibitors of 11β-hydroxysteroid dehydrogenase (11β-HSD1) show promise as drugs to treat metabolic disease and CNS disorders such as cognitive impairment. A series of 1,5-substituted 1H-tetrazole 11β-HSD1 inhibitors has been discovered and chemically modified. Compounds are selective for 11β-HSD1 over 11β-HSD2 and possess good cellular potency in human and murine 11β-HSD1 assays. A range of in vitro stabilities are observed in human liver microsome assays. © 2010 Elsevier Ltd. All rights reserved.
    Original languageEnglish
    Pages (from-to)3265-3271
    Number of pages6
    JournalBioorganic and Medicinal Chemistry Letters
    Volume20
    Issue number11
    DOIs
    Publication statusPublished - 1 Jun 2010

    Keywords

    • 11β-HSD1
    • 11β-Hydroxysteroid dehydrogenase type 1
    • Drug discovery
    • Metabolic syndrome

    Fingerprint

    Dive into the research topics of 'Modulation of 11β-hydroxysteroid dehydrogenase type 1 activity by 1,5-substituted 1H-tetrazoles'. Together they form a unique fingerprint.

    Cite this