AI Article Synopsis
- 3-(Phenylcyclobutyl)-1,2,4-triazoles were discovered to inhibit 11β-Hydroxysteroid Dehydrogenase Type 1 (HSD1) effectively.
- These compounds demonstrated activity in a mouse model, but also activated the Pregnane X Receptor (PXR) significantly, which could lead to unintended effects.
- The study includes a detailed analysis of structure-activity relationship (SAR) and the synthesis of new analogs that resulted in the identification of a more selective HSD1 inhibitor.
Article 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.
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| http://dx.doi.org/10.1016/j.bmcl.2011.01.125 | DOI Listing |
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