The design of orally bioavailable 2, 5-diketopiperazine oxytocin antagonists: from concept to clinical candidate for premature labor.

@article{Borthwick2011TheDO,
  title={The design of orally bioavailable 2, 5-diketopiperazine oxytocin antagonists: from concept to clinical candidate for premature labor.},
  author={Alan David Borthwick and John Liddle},
  journal={Medicinal research reviews},
  year={2011},
  volume={31 4},
  pages={
          576-604
        }
}
A short, efficient and highly stereoselective synthesis has been developed for a series of 6-indanyl-3-alkyl-7-aryl/heterocyclic-(3R, 6R, 7R)-2, 5-diketopiperazine amides that are potent and selective oxytocin (OT) antagonists. Property-based design using an estimate of human oral absorption enabled focus to be directed to those templates with the greatest chance of delivering high bioavailability in humans. This led to the 2', 4'-difluorophenyl dimethylamide 40, a highly potent (pK(i) =9.2… CONTINUE READING
BETA

References

Publications referenced by this paper.
SHOWING 1-10 OF 41 REFERENCES

OXYTOCIN ANTAGONISTS K 603 Medicinal Research Reviews DOI 10.1002/med

  • J Liddle, MJ Allen, +13 authors MA Pullen
  • Bioorg Med Chem Lett
  • 2008

The discovery of GSK 221149 A : A potent and selective oxytocin antagonist

  • SS Shabbir, SL Sollis, TD Westfall, PM Woollard, C Wu, Hickey DMB
  • Bioorg Med Chem Lett
  • 2008

Preterm labour

  • PR Benntt
  • 7th ed. Malden, MA: Blackwell;
  • 2007

Similar Papers

Loading similar papers…