2. Academic Validation
  3. Design and optimization of potent, selective antagonists of Oxytocin

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

Affiliation

  • 1 Discovery Chemistry, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK. Alan.D.Brown@pfizer.com
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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