Design and optimization of potent, selective antagonists of Oxytocin

  • Bioorg Med Chem Lett. 2008 Aug 1;18(15):4278-81. doi: 10.1016/j.bmcl.2008.06.098.
Alan Brown  1 ,  Lindsay Brown ,  Dave Ellis ,  Nicholas Puhalo ,  Chris R Smith ,  Olga Wallace ,  Lesa Watson
Affiliations
  • 1. Discovery Chemistry, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK. [email protected]
PMID: 18639455 DOI: 10.1016/j.bmcl.2008.06.098
Abstract

A novel series of Oxytocin antagonists are described. This series was identified through pharmacophoric overlap of in-house and literature antagonists. Subsequent optimization led to a series of potent, selective antagonists. Several analogues displayed oral bioavailability in vivo in the rat.

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