Bioorganic and Medicinal Chemistry Letters p. 1311 - 1316 (1999)
Update date:2022-08-05
Topics:
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.
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).
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