Solid-phase synthesis of 2,3-disubstituted indoles: discovery of a novel, high-affinity, selective h5-HT2A antagonist

Bioorg Med Chem Lett. 2000 Dec 18;10(24):2693-6. doi: 10.1016/s0960-894x(00)00558-8.

Abstract

The application of a novel solid-phase synthesis of 2,3-disubstituted indoles utilizing a carbamate indole linker is described resulting in the identification of the novel, high-affinity, selective h5-HT2A antagonist 19.

MeSH terms

  • Binding, Competitive
  • Combinatorial Chemistry Techniques
  • Humans
  • Indoles / chemical synthesis*
  • Indoles / pharmacology*
  • Receptors, Dopamine D2 / metabolism
  • Receptors, Serotonin / metabolism
  • Serotonin Antagonists / chemical synthesis*
  • Serotonin Antagonists / pharmacology
  • Tryptamines / chemistry
  • Tryptamines / pharmacology

Substances

  • Indoles
  • Receptors, Dopamine D2
  • Receptors, Serotonin
  • Serotonin Antagonists
  • Tryptamines