Heterocyclic derivatives of 2-(3,5-dimethylphenyl)tryptamine as GnRH receptor antagonists

Bioorg Med Chem Lett. 2001 Apr 23;11(8):1077-80. doi: 10.1016/s0960-894x(01)00133-0.

Abstract

A series of heterocyclic 2-(3,5-dimethylphenyl)tryptamine derivatives was prepared and evaluated on a rat gonadotropin releasing hormone receptor assay. The carbon tether length and heterocyclic ring attached to the amino group of 2-(3,5-dimethylphenyl)tryptamine were varied. Several of these derivatives were potent GnRH antagonists with the most potent compound having an IC50 of 16 nM.

MeSH terms

  • Animals
  • Binding Sites / physiology
  • Drug Design
  • Female
  • Heterocyclic Compounds / chemical synthesis*
  • Hormone Antagonists / chemistry
  • Hormone Antagonists / metabolism*
  • Inhibitory Concentration 50
  • Rats
  • Receptors, LHRH / metabolism*
  • Tryptamines / chemical synthesis*
  • Tryptamines / metabolism*

Substances

  • Heterocyclic Compounds
  • Hormone Antagonists
  • Receptors, LHRH
  • Tryptamines
  • tryptamine