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

doi:10.1016/S0960-894X(98)00372-2

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

Pharmacology

Research output: Contribution to journal › Article › peer-review

134 Scopus citations

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 language	English (US)
Pages (from-to)	2067-2070
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	8
Issue number	16
DOIs	https://doi.org/10.1016/S0960-894X(98)00372-2
State	Published - Aug 18 1998

ASJC Scopus subject areas

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

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10.1016/S0960-894X(98)00372-2

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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 journal › Article › peer-review

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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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AU - Capiris, Thomas

AU - Rubin, Ronald

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AU - Akunne, Hyacinth

AU - Duff Davis, M.

AU - MacKenzie, Robert

AU - Pugsley, Thomas A.

AU - Zoski, Kim T.

AU - Heffner, Thomas G.

AU - Wise, Lawrence D.

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

Abstract

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