Literature DB >> 20452767

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

Scott P Webster1, 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.   

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. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20452767      PMCID： PMC3972730          DOI： 10.1016/j.bmcl.2010.04.055

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  20 in total

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Review 8.  Individual differences in hypothalamic-pituitary-adrenal activity in later life and hippocampal aging.

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Review 10.  Novel insights into glucocorticoid-mediated diabetogenic effects: towards expansion of therapeutic options?

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  4 in total

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3.  Core chemotype diversification in the HIV-1 entry inhibitor class using field-based bioisosteric replacement.

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4.  Synthesis, structure optimization and antifungal screening of novel tetrazole ring bearing acyl-hydrazones.

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  4 in total

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