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

Authors
Williams, PD Bock, MG Evans, BE Freidinger, RM Gallicchio, SN Guidotti, MT Jacobson, MA Kuo, MS Levy, MR Lis, EV Michelson, SR Pawluczyk, JM Perlow, DS Pettibone, DJ Quigley, AG Reiss, DR Salvatore, C Stauffer, KJ Woyden, CJ
Citation
Pd. Williams et al., Nonpeptide oxytocin antagonists: Analogs of L-371,257 with improved potency, BIOORG MED, 9(9), 1999, pp. 1311-1316
Citations number
9
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
9
Year of publication
1999
Pages
1311 - 1316
Database
ISI
SICI code
0960-894X(19990503)9:9<1311:NOAAOL>2.0.ZU;2-K
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 cont aining an ortho-trifluoroethoxyphenylacetyl core which are orally bioavaila ble and have significantly improved potency in vitro and in vivo, e.g., com pound 8 (L-374,943; K-i = 1.4 nM), (C) 1999 Elsevier Science Ltd. All right s reserved.