Discovery and development of a new class of potent, selective, orally active oxytocin receptor antagonists

…, C Bradshaw, AM De Raemy-Schenk…

Index: Quattropani, Anna; Dorbais, Jerome; Covini, David; Pittet, Pierre-Andre; Colovray, Veronique; Thomas, Russell J.; Coxhead, Richard; Halazy, Serge; Scheer, Alexander; Missotten, Marc; Ayala, Guidon; Bradshaw, Charles; De Raemy-Schenk, Anne-Marie; Nichols, Anthony; Cirillo, Rocco; Tos, Enrico Gillio; Giachetti, Claudio; Golzio, Lucia; Marinelli, Paolo; Church, Dennis J.; Barberis, Claude; Chollet, Andre; Schwarz, Matthias K. Journal of Medicinal Chemistry, 2005 , vol. 48, # 24 p. 7882 - 7905

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Citation Number: 27

Abstract

We report a novel chemical class of potent oxytocin receptor antagonists showing a high degree of selectivity against the closely related vasopressin receptors (V1a, V1b, V2). An initial compound, 7, was shown to be active in an animal model of preterm labor when administered by the intravenous but not by the oral route. Stepwise SAR investigations around the different structural elements revealed one position, the arenesulfonyl moiety, to ...

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