Evaluation of selective inhibitors of 11β-HSD1 for the treatment of hypertension.

Bioorg Med Chem Lett 2013 Jun 22;23(12):3650-3. Epub 2013 Mar 22.

Department of Medicinal Chemistry, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065, USA.

In an effort to understand the origin of blood-pressure lowering effects observed in recent clinical trials with 11β-HSD1 inhibitors, we examined a set of 11β-HSD1 inhibitors in a series of relevant in vitro and in vivo assays. Select 11β-HSD1 inhibitors reduced blood pressure in our preclinical models but most or all of the blood pressure lowering may be mediated by a 11β-HSD1 independent pathway.

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http://dx.doi.org/10.1016/j.bmcl.2013.03.011DOI Listing
June 2013
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