- 5-arylamino-1,2,4-triazin-6(1H)-one CRF1 receptor antagonists.
5-arylamino-1,2,4-triazin-6(1H)-one CRF1 receptor antagonists.
Bioorganic & medicinal chemistry letters (2010-05-21)
William D Schmitz, Allison B Brenner, Joanne J Bronson, Jonathan L Ditta, Corrine R Griffin, Yu-Wen Li, Nicholas J Lodge, Thaddeus F Molski, Richard E Olson, Xiaoliang Zhuo, John E Macor
PMID20483614
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.