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

Research output: Contribution to journalArticle

130 Citations (Scopus)

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
Externally publishedYes

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Pyrimidines
X ray crystallography
X Ray Crystallography
CRF receptor type 1
pyrazolo(1,5-a)pyrimidine

ASJC Scopus subject areas

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

Cite this

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

Pyrazolo[1,5-a]pyrimidine CRF-1 receptor antagonists. / Wustrow, David J.; Capiris, Thomas; Rubin, Ronald; Knobelsdorf, James A.; Akunne, Hyacinth; Duff Davis, M.; MacKenzie, Robert; Pugsley, Thomas A.; Zoski, Kim T.; Heffner, Thomas G.; Wise, Lawrence D.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 8, No. 16, 18.08.1998, p. 2067-2070.

Research output: Contribution to journalArticle

Wustrow, DJ, Capiris, T, Rubin, R, Knobelsdorf, JA, Akunne, H, Duff Davis, M, MacKenzie, R, Pugsley, TA, Zoski, KT, Heffner, TG & Wise, LD 1998, 'Pyrazolo[1,5-a]pyrimidine CRF-1 receptor antagonists', Bioorganic and Medicinal Chemistry Letters, vol. 8, no. 16, pp. 2067-2070. https://doi.org/10.1016/S0960-894X(98)00372-2
Wustrow DJ, Capiris T, Rubin R, Knobelsdorf JA, Akunne H, Duff Davis M et al. Pyrazolo[1,5-a]pyrimidine CRF-1 receptor antagonists. Bioorganic and Medicinal Chemistry Letters. 1998 Aug 18;8(16):2067-2070. https://doi.org/10.1016/S0960-894X(98)00372-2
Wustrow, David J. ; Capiris, Thomas ; Rubin, Ronald ; Knobelsdorf, James A. ; Akunne, Hyacinth ; Duff Davis, M. ; MacKenzie, Robert ; Pugsley, Thomas A. ; Zoski, Kim T. ; Heffner, Thomas G. ; Wise, Lawrence D. / Pyrazolo[1,5-a]pyrimidine CRF-1 receptor antagonists. In: Bioorganic and Medicinal Chemistry Letters. 1998 ; Vol. 8, No. 16. pp. 2067-2070.
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