N-(Pyridin-3-yl)benzamides as selective inhibitors of human aldosterone synthase (CYP11B2).
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Zimmer C, Hafner M, Zender M, Ammann D, Hartmann RW, Vock CA
N-(Pyridin-3-yl)benzamides as selective inhibitors of human aldosterone synthase (CYP11B2).
Bioorg Med Chem Lett. 2011 Jan 1;21(1):186-90. doi: 10.1016/j.bmcl.2010.11.040. Epub 2010 Nov 12.
- PubMed ID
- 21129965 [ View in PubMed]
- Abstract
A series of 23 N-(Pyridin-3-yl)benzamides was synthesized and evaluated for their potential to inhibit human steroid-11beta-hydroxylase (CYP11B1) and human aldosterone synthase (CYP11B2). The most potent and selective CYP11B2 inhibitors (IC(50) values 53-166 nM) were further evaluated for their potential to inhibit human CYP17 and CYP19, and no inhibition was observed. Clear evidence was shown for N-(Pyridin-3-yl)benzamides to be a highly selective class of CYP11B2 inhibitors in vitro.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Metyrapone Cytochrome P450 11B1, mitochondrial IC 50 (nM) 14.6 N/A N/A Details Metyrapone Cytochrome P450 11B2, mitochondrial IC 50 (nM) 72 N/A N/A Details