Pyrazolo[1,5-a]pyrimidine CRF-1 receptor antagonists

A series of 3-phenylpyrazolo[1,5- a]pyrimidines was prepared and found to have affinity for the human CRF-1 receptor. The 3-dimensional structure of one of the most potent analogs in this series, 10d, was determined by X-ray crystallography and suggests the spatial requirements for potent CRF-1 receptor binding affinity in this series. A series of 3-phenylpyrazolo[1,5-a]pyrimidines was prepared and found to have affinity for the human CRF-1 receptor. The X-ray structure of one of the most potent analogs suggests the spatial requirements for potent CRF-1 receptor binding affinity in this series.