Synthesis and activity of 1-(3-amino-1-phenylpropyl)indolin-2-ones: a new class of selective norepinephrine reuptake inhibitors

Bioorg Med Chem Lett. 2008 Sep 15;18(18):4929-31. doi: 10.1016/j.bmcl.2008.08.060. Epub 2008 Aug 22.

Abstract

Norepinephrine and serotonin play an important role in a wide variety of biological processes and are implicated in a number of neurological disorders. A novel class of 1-(3-amino-1-phenylpropyl)indolin-2-ones was designed and synthesized that displays potent norepinephrine reuptake inhibition while maintaining high selectivity (>100-fold) against the human serotonin and dopamine transporters.

MeSH terms

  • Humans
  • Indoles / chemical synthesis*
  • Indoles / chemistry
  • Indoles / pharmacology*
  • Molecular Structure
  • Neurotransmitter Uptake Inhibitors / chemical synthesis*
  • Neurotransmitter Uptake Inhibitors / chemistry
  • Neurotransmitter Uptake Inhibitors / pharmacology*
  • Norepinephrine / antagonists & inhibitors*
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Indoles
  • Neurotransmitter Uptake Inhibitors
  • indolin-2-one
  • Norepinephrine