2. Academic Validation
  3. The discovery of GSK221149A: a potent and selective oxytocin antagonist

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

Affiliation

  • 1 Department of Medicinal Chemistry, GlaxoSmithKline Research and Development, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, UK. john.2.liddle@gsk.com
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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