Design, synthesis and structure-activity relationships of novel imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists

Bioorg Med Chem Lett. 2002 Aug 19;12(16):2185-7. doi: 10.1016/s0960-894x(02)00371-2.

Abstract

SAR studies of lead GnRH receptor antagonists 2a and 2b reported earlier resulted in the discovery of compound 10b which showed much higher potency (K(i)=4.6 nM, compared with 2b, K(i)=230 nM) in which the 7-position of the imidazolo[1,2-a]pyrimidone core was substituted with a methyl group, and the ester at the 6-position was replaced by the 3-methoxyphenyl group.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Binding Sites
  • Drug Design*
  • Humans
  • Molecular Structure
  • Pyrimidinones / chemical synthesis*
  • Pyrimidinones / chemistry
  • Pyrimidinones / pharmacology*
  • Rats
  • Receptors, LHRH / antagonists & inhibitors*
  • Structure-Activity Relationship

Substances

  • Pyrimidinones
  • Receptors, LHRH