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Discovery and optimisation of a potent and selective tertiary sulfonamide oxytocin antagonist
Nicholas P Barton1, Benjamin R Bellenie, Andrew T Doran
1GlaxoSmithKline Pharmaceuticals, New Frontiers Science Park (North), Coldharbour Road, Harlow, Essex CM19 5AD, England, UK.
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.
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