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

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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