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

Bioorg Med Chem Lett

Neuroscience Discovery Chemistry, Bristol-Myers Squibb Research and Development, Wallingford, CT 06492, USA.

Published: June 2010

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.

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http://dx.doi.org/10.1016/j.bmcl.2010.04.121DOI Listing

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