Initial structure-activity relationship studies of a novel series of pyrrolo[1,2-a]pyrimid-7-ones as GnRH receptor antagonists

Bioorg Med Chem Lett. 2002 Feb 11;12(3):399-402. doi: 10.1016/s0960-894x(01)00779-x.

Abstract

Initial SAR studies on 1-aminomethyl-2-aryl-3-cyano-pyrrolo[1,2-a]pyrimid-7-one-6-carboxylates as human GnRH receptor antagonists were discussed. 2-(2-Methylaminoethyl)pyridine was discovered to be a key feature for generating active compounds. The best compound from the series had 25 nM (K(i)) binding affinity to human GnRH receptor.

MeSH terms

  • Animals
  • Humans
  • Indicators and Reagents
  • Kinetics
  • Pyrimidinones / chemical synthesis*
  • Pyrimidinones / pharmacology*
  • Pyrroles / chemical synthesis*
  • Pyrroles / pharmacology*
  • Radioligand Assay
  • Rats
  • Receptors, LHRH / antagonists & inhibitors*
  • Structure-Activity Relationship

Substances

  • Indicators and Reagents
  • Pyrimidinones
  • Pyrroles
  • Receptors, LHRH