Quinolones as gonadotropin releasing hormone (GnRH) antagonists: simultaneous optimization of the C(3)-aryl and C(6)-substituents

Bioorg Med Chem Lett. 2000 Aug 7;10(15):1723-7. doi: 10.1016/s0960-894x(00)00318-8.

Abstract

A series of 3-arylquinolones was prepared and evaluated for their ability to act as gonadotropin releasing hormone (GnRH) antagonists. A variety of substitution patterns of the 3-aryl substituent are described. The 3,4,5-trimethylphenyl substituent (23h) was found to be optimal.

MeSH terms

  • Gonadotropin-Releasing Hormone / antagonists & inhibitors*
  • Quinolones / chemistry
  • Quinolones / pharmacology*
  • Structure-Activity Relationship

Substances

  • Quinolones
  • Gonadotropin-Releasing Hormone