Synthesis and structure-activity relationships of 8-azabicyclo[3.2.1]octane benzylamine NK1 antagonists

Bioorg Med Chem Lett. 2006 Feb 15;16(4):811-4. doi: 10.1016/j.bmcl.2005.11.026. Epub 2005 Nov 22.

Abstract

A series of 8-azabicyclo[3.2.1]octane amine hNK1 antagonists has been investigated and structure-activity relationships of the benzylamine and 6-exo substituents described. Acidic substituents at C6 give a series of high affinity compounds for hNK1 with selectivity over the hERG channel.

MeSH terms

  • Aza Compounds / chemical synthesis*
  • Aza Compounds / chemistry
  • Bridged Bicyclo Compounds, Heterocyclic / chemical synthesis*
  • Bridged Bicyclo Compounds, Heterocyclic / chemistry
  • Humans
  • Molecular Conformation
  • Neurokinin-1 Receptor Antagonists*
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • 8-azabicyclo(3.2.1)octane benzylamine
  • Aza Compounds
  • Bridged Bicyclo Compounds, Heterocyclic
  • Neurokinin-1 Receptor Antagonists