2. Academic Validation
  3. N-(Pyridin-3-yl)benzamides as selective inhibitors of human aldosterone synthase (CYP11B2)

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.
Christina Zimmer 1,  Marieke Hafner,  Michael Zender,  Dominic Ammann,  Rolf W Hartmann,  Carsten A Vock
Affiliations

Affiliation

  • 1 Pharmaceutical and Medicinal Chemistry, Saarland University & Helmholtz Institute for Pharmaceutical Research Saarland, PO Box 15 11 50, D-66041 Saarbrücken, Germany.
PMID: 21129965 DOI: 10.1016/j.bmcl.2010.11.040
Abstract

A series of 23 N-(Pyridin-3-yl)benzamides was synthesized and evaluated for their potential to inhibit human steroid-11β-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.

Figures