The discovery of GSK221149A: a potent and selective oxytocin antagonist

  • Bioorg Med Chem Lett. 2008 Jan 1;18(1):90-4. doi: 10.1016/j.bmcl.2007.11.008.
John Liddle  1 ,  Michael J Allen ,  Alan D Borthwick ,  David P Brooks ,  David E Davies ,  Richard M Edwards ,  Anne M Exall ,  Chris Hamlett ,  Wendy R Irving ,  Andrew M Mason ,  Gerald P McCafferty ,  Fabrizio Nerozzi ,  Simon Peace ,  Joanne Philp ,  Derek Pollard ,  Mark A Pullen ,  Shaila S Shabbir ,  Steve L Sollis ,  Timothy D Westfall ,  Pat M Woollard ,  Charlene Wu ,  Deirdre M B Hickey
Affiliations
  • 1. Department of Medicinal Chemistry, GlaxoSmithKline Research and Development, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, UK. [email protected]
PMID: 18032036 DOI: 10.1016/j.bmcl.2007.11.008
Abstract

Optimisation of a series of oxazole diketopiperazines has led to the discovery of a very potent and selective oxytocin antagonist GSK221149A. GSK221149A has been shown to inhibit oxytocin-induced uterine contractions in the anaesthetised rat.

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