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

The structure–activity relationships of a series of 5-arylamino-1,2,4-triazin-6(1H)-ones as corticotropin releasing factor-1 receptor antagonists was investigated. 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 N3-phenylpyrazinone structure was minimized by incorporation of the additional ring nitrogen found in the triazinones.