Williams P D, Bock M G, Evans B E, Freidinger R M, Gallicchio S N, Guidotti M T, Jacobson M A, Kuo M S, Levy M R, Lis E V, Michelson S R, Pawluczyk J M, Perlow D S, Pettibone D J, Quigley A G, Reiss D R, Salvatore C, Stauffer K J, Woyden C J
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA.
Bioorg Med Chem Lett. 1999 May 3;9(9):1311-6. doi: 10.1016/s0960-894x(99)00181-x.
Structure-activity studies on the oxytocin antagonist 1 (L-371,257; Ki = 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; Ki = 1.4 nM).
