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

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Abstract

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.

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Wustrow, D. J., Capiris, T., Rubin, R., Knobelsdorf, J. A., Akunne, H., Duff Davis, M., … Wise, L. D. (1998). Pyrazolo[1,5-a]pyrimidine CRF-1 receptor antagonists. Bioorganic and Medicinal Chemistry Letters, 8(16), 2067–2070. https://doi.org/10.1016/S0960-894X(98)00372-2

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