Nonpeptide oxytocin antagonists: Analogs of L-371,257 with improved potency

Abstract Structure-activity studies on the oxytocin antagonist 1 (L-371,257; K i = 9.3 nM) have led to the identification of a related series of compounds containing an ortho-trifluoroethoxyphenylacetyl core which are orally bioavailable and have significantly improved potency in vitro and in vivo, e.g., compound 8 (L-374,943; K i = 1.4 nM).