229001-15-4Relevant articles and documents
Nonpeptide oxytocin antagonists: Analogs of L-371,257 with improved potency
Williams, Peter D.,Bock, Mark G.,Evans, Ben E.,Freidinger, Roger M.,Gallicchio, Steven N.,Guidotti, Maribeth T.,Jacobson, Marlene A.,Michelle S, Kuo,Levy, Michelle R.,Edward V, Lis,Michelson, Stuart R.,Pawluczyk, Joseph M.,Perlow, Debra S.,Pettibone, Douglas J.,Quigley, Amy G.,Reiss, Duane R.,Salvatore, Christopher,Stauffer, Kenneth J.,Woyden, Carla J.
, p. 1311 - 1316 (2007/10/03)
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).
