New fused benzazepine as selective D3 receptor antagonists. Synthesis and biological evaluation. Part one: [h]-fused tricyclic systems

Bioorg Med Chem Lett. 2008 Feb 1;18(3):901-7. doi: 10.1016/j.bmcl.2007.12.066. Epub 2008 Jan 3.

Abstract

The synthesis and SAR of a new series of potent and selective dopamine D(3) receptor antagonists is reported. The introduction of a tricyclic [h]-fused benzazepine moiety on the recently disclosed scaffold of 1,2,4-triazol-3-yl-thiopropyl-tetrahydrobenzazepines is reported. A full rat pharmacokinetic characterization is also reported.

MeSH terms

  • Animals
  • Benzazepines / chemical synthesis*
  • Benzazepines / chemistry
  • Benzazepines / pharmacology*
  • Combinatorial Chemistry Techniques
  • Dopamine Antagonists / chemical synthesis*
  • Dopamine Antagonists / chemistry
  • Dopamine Antagonists / pharmacology*
  • Drug Design
  • Molecular Structure
  • Rats
  • Receptors, Dopamine D3 / antagonists & inhibitors*
  • Structure-Activity Relationship

Substances

  • Benzazepines
  • Dopamine Antagonists
  • Receptors, Dopamine D3