N-alkyl-5H-pyrido[4,3-b]indol-1-amines and derivatives as novel urotensin-II receptor antagonists

Bioorg Med Chem Lett. 2008 Sep 15;18(18):4936-9. doi: 10.1016/j.bmcl.2008.08.054. Epub 2008 Aug 22.

Abstract

High throughput screening of our compound collection led to the discovery of a novel series of N-alkyl-5H-pyrido[4,3-b]indol-1-amines as urotensin-II receptor antagonists. Synthesis, initial structure and activity relationships, functional and animal ortholog activities of the series are described.

MeSH terms

  • Amines / chemical synthesis*
  • Amines / chemistry
  • Amines / pharmacology*
  • Animals
  • Combinatorial Chemistry Techniques
  • Mice
  • Molecular Structure
  • Pyridines / chemical synthesis*
  • Pyridines / chemistry
  • Pyridines / pharmacology*
  • Structure-Activity Relationship
  • Urotensins / antagonists & inhibitors*

Substances

  • Amines
  • Pyridines
  • Urotensins
  • urotensin II