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Bioorg Med Chem Lett ; 20(12): 3579-83, 2010 Jun 15.
Article in English | MEDLINE | ID: mdl-20483614

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.


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