Discovery and optimisation of a potent and selective tertiary sulfonamide oxytocin antagonist

NP Barton, BR Bellenie, AT Doran, AJ Emmons…

Index: Barton, Nicholas P.; Bellenie, Benjamin R.; Doran, Andrew T.; Emmons, Amanda J.; Heer, Jag P.; Salvagno, Cristian M. Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 2 p. 528 - 532

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Citation Number: 5

Abstract

The optimisation of a tertiary sulfonamide high-throughput screening hit is described. A combination of high-throughput chemistry, pharmacophore analysis and in silico PK profiling resulted in the discovery of potent sulfonamide oxytocin receptor antagonists with oral exposure and good selectivity over vasopressin receptors.