Synthesis and structure–activity relationships of N 3-pyridylpyrazinones as corticotropin-releasing factor-1 (CRF 1) receptor antagonists

…, TF Molski, GK Mattson, NJ Lodge, JJ Bronson…

Index: Hartz, Richard A.; Ahuja, Vijay T.; Schmitz, William D.; Molski, Thaddeus F.; Mattson, Gail K.; Lodge, Nicholas J.; Bronson, Joanne J.; Macor, John E. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 6 p. 1890 - 1894

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Citation Number: 10

Abstract

A series of N3-pyridylpyrazinones was investigated as corticotropin-releasing factor-1 receptor antagonists. It was observed that the binding affinity of analogues containing a pyridyl group was influenced not only by the substitution pattern on the pyridyl group, but also by the pKa of the pyridyl nitrogen. Analogues containing a novel 6-(difluoromethoxy)-2, 5-dimethylpyridin-3-amine group were among the most potent N3-pyridylpyrazinones ...