Synthesis and SAR of amino acid-derived heterocyclic progesterone receptor full and partial agonists

Bioorg Med Chem Lett. 2009 May 15;19(10):2637-41. doi: 10.1016/j.bmcl.2009.03.146. Epub 2009 Apr 5.

Abstract

Two classes of amino acid-derived heterocyclic progesterone receptor ligands were developed to address the metabolic issues posed by the dimethyl amide functionality of the lead compound (1). The tetrazole-derived ligands behaved as potent partial agonists, while the 1,2,4-triazole ligands behaved as potent full agonists.

MeSH terms

  • Amino Acids / chemistry
  • Animals
  • Rats
  • Receptors, Progesterone / agonists*
  • Receptors, Progesterone / metabolism
  • Structure-Activity Relationship
  • Tetrazoles / chemical synthesis*
  • Tetrazoles / chemistry
  • Tetrazoles / pharmacokinetics

Substances

  • Amino Acids
  • Receptors, Progesterone
  • Tetrazoles