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ChemInform 2009, 40, issue 40 © 2009 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim www.cheminform.wiley-vch.de Pyrazine derivatives R 0550 Aryloxypyrazines as Highly Selective Antagonists of Oxytocin. — Eleven title compound of type (IX) are prepared by reaction of (VII) with various phenols and screened as selective antagonists of oxytocin. The most active derivative (IXb) com- bines excellent OT activity with significantly improved V1A selectivity (> 330 fold se- lectivity for OT over V1A receptor). — (BROWN*, A.; ELLIS, D.; PEARCE, D.; RALPH, M.; SCIAMMETTA, N.; Bioorg. Med. Chem. Lett. 19 (2009) 10, 2634-2636; Discovery Chem., Pfizer Global Res. Dev., Sandwich, Kent CT13 9NJ, UK; Eng.) — M. Bohle 40- 156

ChemInform Abstract: Aryloxypyrazines as Highly Selective Antagonists of Oxytocin

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Pyrazine derivativesR 0550 Aryloxypyrazines as Highly Selective Antagonists of Oxytocin. — Eleven title

compound of type (IX) are prepared by reaction of (VII) with various phenols and screened as selective antagonists of oxytocin. The most active derivative (IXb) com-bines excellent OT activity with significantly improved V1A selectivity (> 330 fold se-lectivity for OT over V1A receptor). — (BROWN*, A.; ELLIS, D.; PEARCE, D.; RALPH, M.; SCIAMMETTA, N.; Bioorg. Med. Chem. Lett. 19 (2009) 10, 2634-2636; Discovery Chem., Pfizer Global Res. Dev., Sandwich, Kent CT13 9NJ, UK; Eng.) — M. Bohle

40- 156

ChemInform 2009, 40, issue 40 © 2009 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim