Novel, achiral aminoheterocycles as selective monoamine reuptake inhibitors

Bioorg Med Chem Lett. 2009 Aug 15;19(16):4630-3. doi: 10.1016/j.bmcl.2009.06.076. Epub 2009 Jun 25.

Abstract

A variety of novel aminoheterocycle scaffolds as selective monoamine reuptake inhibitors have been prepared and one of these scaffolds is achiral. The main elements responsible for hERG channel, CYP2D6 and CYP3A4 inhibition were identified.

MeSH terms

  • Cytochrome P-450 CYP2D6 / metabolism
  • Cytochrome P-450 CYP2D6 Inhibitors*
  • Cytochrome P-450 CYP3A / metabolism
  • Cytochrome P-450 CYP3A Inhibitors*
  • Heterocyclic Compounds / chemical synthesis
  • Heterocyclic Compounds / chemistry*
  • Heterocyclic Compounds / pharmacology
  • Humans
  • Microsomes, Liver / metabolism
  • Neurotransmitter Uptake Inhibitors / chemical synthesis
  • Neurotransmitter Uptake Inhibitors / chemistry*
  • Neurotransmitter Uptake Inhibitors / pharmacology

Substances

  • Cytochrome P-450 CYP2D6 Inhibitors
  • Cytochrome P-450 CYP3A Inhibitors
  • Heterocyclic Compounds
  • Neurotransmitter Uptake Inhibitors
  • Cytochrome P-450 CYP2D6
  • Cytochrome P-450 CYP3A
  • CYP3A4 protein, human