Identification of potent and selective oxytocin antagonists. Part 1: indole and benzofuran derivatives

Bioorg Med Chem Lett. 2002 May 20;12(10):1399-404. doi: 10.1016/s0960-894x(02)00159-2.

Abstract

Studies to discover novel, potent and selective oxytocin antagonists are reported. Combinatorial libraries designed to find novel replacements of fragments of oxytocin antagonist L-371,257, identified pyrimidine, thiazole, indole and benzofuran as potential alternatives to the benzoic acid moiety of L-371,257. Additional investigations identified indole and benzofuran derivatives with potent oxytocin antagonist activity.

MeSH terms

  • Animals
  • Benzofurans / chemical synthesis*
  • Benzofurans / chemistry
  • Benzofurans / pharmacokinetics
  • Benzofurans / pharmacology
  • Biological Availability
  • Dogs
  • Drug Design
  • Humans
  • Indoles / chemical synthesis*
  • Indoles / chemistry
  • Indoles / pharmacokinetics
  • Indoles / pharmacology
  • Kinetics
  • Models, Molecular
  • Molecular Conformation
  • Oxytocin / antagonists & inhibitors*
  • Receptors, Oxytocin / antagonists & inhibitors*
  • Structure-Activity Relationship

Substances

  • Benzofurans
  • Indoles
  • Receptors, Oxytocin
  • Oxytocin