5-arylamino-1,2,4-triazin-6(1H)-one CRF1 receptor antagonists

Bioorg Med Chem Lett. 2010 Jun 15;20(12):3579-83. doi: 10.1016/j.bmcl.2010.04.121. Epub 2010 May 17.

Abstract

A series of 5-arylamino-1,2,4-triazin-6(1H)-ones was synthesized and evaluated as antagonists at the corticotropin releasing factor receptor. Formation of CYP-mediated oxidative reactive metabolites previously observed in a related N(3)-phenylpyrazinone structure was minimized by incorporation of the additional ring nitrogen found in the triazinones.

MeSH terms

  • Animals
  • Humans
  • Inhibitory Concentration 50
  • Oxidation-Reduction
  • Pyrazines
  • Rats
  • Receptors, Corticotropin-Releasing Hormone / antagonists & inhibitors*
  • Structure-Activity Relationship
  • Triazines / chemical synthesis*
  • Triazines / pharmacology*

Substances

  • Pyrazines
  • Receptors, Corticotropin-Releasing Hormone
  • Triazines
  • CRF receptor type 1