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

David J. Wustrow, Thomas Capiris, Ronald Rubin, James A. Knobelsdorf, Hyacinth Akunne, M. Duff Davis, Robert MacKenzie, Thomas A. Pugsley, Kim T. Zoski, Thomas G. Heffner, Lawrence D. Wise

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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.

Original languageEnglish (US)
Pages (from-to)2067-2070
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume8
Issue number16
DOIs
StatePublished - Aug 18 1998

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ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Cite this

Wustrow, D. J., Capiris, T., Rubin, R., Knobelsdorf, J. A., Akunne, H., Duff Davis, M., MacKenzie, R., Pugsley, T. A., Zoski, K. T., Heffner, T. G., & 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