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

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.