Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1370774 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
Abstract
3-(Phenylcyclobutyl)-1,2,4-triazoles were identified as inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 (HSD1). They were shown to be active in the mouse in vivo pharmacodynamic model (PD) for HSD1 but exhibited a potent off-target activation of the Pregnane X Receptor (PXR). SAR studies and synthesis of analogs that led to the discovery of a selective HSD1 inhibitor are described in detail.
Graphical abstractThe synthesis and biological activity of selective inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
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Authors
Wanying Sun, Milana Maletic, Steven S. Mundt, Kashmira Shah, Hratch Zokian, Kathy Lyons, Sherman T. Waddell, James Balkovec,