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Bioorg Med Chem Lett. 2010 Jun 1;20(11):3265-71. doi: 10.1016/j.bmcl.2010.04.055. Epub 2010 Apr 18.

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

Author information

1
Endocrinology Unit, Centre for Cardiovascular Science, The Queen's Medical Research Institute, University of Edinburgh, 47 Little France Crescent, Edinburgh EH16 4TJ, UK. scott.webster@ed.ac.uk

Abstract

Inhibitors of 11beta-hydroxysteroid dehydrogenase (11beta-HSD1) show promise as drugs to treat metabolic disease and CNS disorders such as cognitive impairment. A series of 1,5-substituted 1H-tetrazole 11beta-HSD1 inhibitors has been discovered and chemically modified. Compounds are selective for 11beta-HSD1 over 11beta-HSD2 and possess good cellular potency in human and murine 11beta-HSD1 assays. A range of in vitro stabilities are observed in human liver microsome assays.

PMID:
20452767
PMCID:
PMC3972730
DOI:
10.1016/j.bmcl.2010.04.055
[Indexed for MEDLINE]
Free PMC Article

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