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ID: ALA1154542

Journal: Bioorg Med Chem Lett

Title: Discovery and optimisation of a potent and selective tertiary sulfonamide oxytocin antagonist.

Authors: Barton NP, Bellenie BR, Doran AT, Emmons AJ, Heer JP, Salvagno CM.

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.

CiteXplore: 19081251

DOI: 10.1016/j.bmcl.2008.11.018