Synthesis and initial structure–Activity relationships of a novel series of imidazolo[1,2- a]pyrimid-5-ones as potent GnRH receptor antagonists

Abstract

SAR studies of 2-arylimidazolo[1,2- a]pyrimid-5-ones 10a– m, which were derived from initial lead 3a, resulted in the discovery of a series of potent nonpeptide human GnRH receptor antagonists. Compounds with good potency (e.g., 10e, K i=7.5 nM) were prepared by introduction of a 2-(2-pyridyl)ethyl at the basic nitrogen and a 3-pentyl ester at the 6-position of the bicyclic core.