Literature DB >> 18434143

Bis-aryl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.

Susan D Aster1, Donald W Graham, Divya Kharbanda, Gool Patel, Mitree Ponpipom, Gina M Santorelli, Michael J Szymonifka, Steven S Mundt, Kashmira Shah, Marty S Springer, Rolf Thieringer, Anne Hermanowski-Vosatka, Samuel D Wright, Jianying Xiao, Hratch Zokian, James M Balkovec.   

Abstract

3-Aryl-5-phenyl-(1,2,4)-triazoles were identified as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1). They are active in both in vitro and an in vivo mouse pharmacodynamic (PD) model. The synthesis and structure activity relationships are presented.

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Year:  2008        PMID: 18434143     DOI: 10.1016/j.bmcl.2008.04.010

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


  2 in total

Review 1.  11β-hydroxysteroid dehydrogenases and the brain: from zero to hero, a decade of progress.

Authors:  Caitlin S Wyrwoll; Megan C Holmes; Jonathan R Seckl
Journal:  Front Neuroendocrinol       Date:  2010-12-07       Impact factor: 8.606

2.  Discovery of adamantyl heterocyclic ketones as potent 11β-hydroxysteroid dehydrogenase type 1 inhibitors.

Authors:  Xiangdong Su; Nigel Vicker; Mark P Thomas; Fabienne Pradaux-Caggiano; Heather Halem; Michael D Culler; Barry V L Potter
Journal:  ChemMedChem       Date:  2011-05-23       Impact factor: 3.466

  2 in total

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