4-Anilino-pyrimidine, novel aldosterone synthase (CYP11B2) inhibitors bearing pyrimidine structures

Bioorg Med Chem Lett. 2017 May 1;27(9):1902-1906. doi: 10.1016/j.bmcl.2017.03.034. Epub 2017 Mar 21.

Abstract

2,2,2-Trifluoro-1-{4-[(4-fluorophenyl)amino]pyrimidin-5-yl}-1-[1-(methylsulfonyl)piperidin-4-yl]ethanol 1 was identified as a novel potent aldosterone synthase inhibitor. Despite large species differences, compound 1 inhibits both human and rodent CYP11B2 in a nano-molar range.

Keywords: Aldosterone; Aldosterone synthase inhibitor; Amino-pyrimidine; CYP11B1; CYP11B2.

MeSH terms

  • Aniline Compounds / chemistry*
  • Aniline Compounds / pharmacology*
  • Cytochrome P-450 CYP11B2 / antagonists & inhibitors*
  • Cytochrome P-450 CYP11B2 / metabolism
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / pharmacology*
  • HEK293 Cells
  • Humans
  • Pyrimidines / chemistry*
  • Pyrimidines / pharmacology*

Substances

  • Aniline Compounds
  • Enzyme Inhibitors
  • Pyrimidines
  • Cytochrome P-450 CYP11B2