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…

文献索引：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

全文：HTML全文

被引用次数: 10

摘要

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 ...