Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erbα

Bioorg Med Chem Lett. 2012 Jul 1;22(13):4413-7. doi: 10.1016/j.bmcl.2012.04.126. Epub 2012 May 8.

Abstract

The structure-activity relationship study of a small molecule Rev-erbα agonist is reported. The potency and efficacy of the agonists in a cell-based assay were optimized as compared to the initial lead. Modest mouse pharmacokinetics coupled with an improved in vitro profile make 12e a suitable in vivo probe to interrogate the functions of Rev-erbα in animal models of disease.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Amines / chemical synthesis
  • Amines / chemistry*
  • Amines / pharmacokinetics
  • Animals
  • Benzylamines / chemical synthesis
  • Benzylamines / chemistry*
  • Benzylamines / pharmacokinetics
  • Brain / metabolism
  • Mice
  • Nuclear Receptor Subfamily 1, Group D, Member 1 / agonists*
  • Nuclear Receptor Subfamily 1, Group D, Member 1 / metabolism
  • Structure-Activity Relationship
  • Thiophenes / chemical synthesis
  • Thiophenes / chemistry*
  • Thiophenes / pharmacokinetics

Substances

  • Amines
  • Benzylamines
  • Nuclear Receptor Subfamily 1, Group D, Member 1
  • Thiophenes