Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 11, Pages 3265-3271Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.04.055
Keywords
11 beta-Hydroxysteroid dehydrogenase type 1; 11 beta-HSD1; Drug discovery; Metabolic syndrome
Categories
Funding
- Wellcome Trust
- Engineering and Physical Sciences Research Council [EP/G007519/1] Funding Source: researchfish
- Medical Research Council [G0700704B] Funding Source: researchfish
- EPSRC [EP/G007519/1] Funding Source: UKRI
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Inhibitors of 11 beta-hydroxysteroid dehydrogenase (11 beta-HSD1) show promise as drugs to treat metabolic disease and CNS disorders such as cognitive impairment. A series of 1,5-substituted 1H-tetrazole 11 beta-HSD1 inhibitors has been discovered and chemically modified. Compounds are selective for 11 beta-HSD1 over 11 beta-HSD2 and possess good cellular potency in human and murine 11 beta-HSD1 assays. A range of in vitro stabilities are observed in human liver microsome assays. (C) 2010 Elsevier Ltd. All rights reserved.
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