Aryloxypyrazines as highly selective antagonists of Oxytocin

Bioorg Med Chem Lett. 2009 May 15;19(10):2634-6. doi: 10.1016/j.bmcl.2009.03.160. Epub 2009 Apr 5.

Abstract

A series of aryloxypyrazines were designed based on structural overlap with previously reported arylpyrazine Oxytocin antagonists. Similarly high levels of Oxytocin antagonism were achievable in this new series. In addition, significant improvements in selectivity over the related vasopressin V(1A) receptor were also possible.

MeSH terms

  • Antidiuretic Hormone Receptor Antagonists
  • Oxytocin / antagonists & inhibitors*
  • Pyrazines / chemical synthesis
  • Pyrazines / chemistry*

Substances

  • Antidiuretic Hormone Receptor Antagonists
  • Pyrazines
  • Oxytocin