Synthesis and structure-activity relationships of pyrido[3,2-b]pyrazin-3(4H)-ones and pteridin-7(8H)-ones as corticotropin-releasing factor-1 receptor antagonists

Bioorg Med Chem Lett. 2012 Aug 1;22(15):4986-9. doi: 10.1016/j.bmcl.2012.06.034. Epub 2012 Jun 16.

Abstract

Pyrido[3,2-b]pyrazin-3(4H)-ones and pteridin-7(8H)-ones were evaluated as corticotropin-releasing factor-1 receptor antagonists. The synthesis, SAR studies and pharmacokinetic evaluation of these analogs are described herein.

MeSH terms

  • Animals
  • Anti-Anxiety Agents / chemical synthesis
  • Anti-Anxiety Agents / chemistry
  • Anti-Anxiety Agents / pharmacokinetics
  • Half-Life
  • Pteridines / chemical synthesis
  • Pteridines / chemistry*
  • Pteridines / pharmacokinetics
  • Pyrazines / chemical synthesis
  • Pyrazines / chemistry*
  • Pyrazines / pharmacokinetics
  • Rats
  • Receptors, Corticotropin-Releasing Hormone / antagonists & inhibitors*
  • Receptors, Corticotropin-Releasing Hormone / metabolism
  • Structure-Activity Relationship

Substances

  • Anti-Anxiety Agents
  • Pteridines
  • Pyrazines
  • Receptors, Corticotropin-Releasing Hormone
  • CRF receptor type 1