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

Department of Pharmacology

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

140 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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title = "Pyrazolo[1,5-a]pyrimidine CRF-1 receptor antagonists",

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.",

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

year = "1998",

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doi = "10.1016/S0960-894X(98)00372-2",

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TY - JOUR

T1 - Pyrazolo[1,5-a]pyrimidine CRF-1 receptor antagonists

AU - Wustrow, David J.

AU - Capiris, Thomas

AU - Rubin, Ronald

AU - Knobelsdorf, James A.

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.

PY - 1998/8/18

Y1 - 1998/8/18

N2 - 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.

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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U2 - 10.1016/S0960-894X(98)00372-2

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

M3 - Article

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AN - SCOPUS:0032544170

VL - 8

SP - 2067

EP - 2070

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

SN - 0960-894X

IS - 16

ER -

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

Abstract

ASJC Scopus subject areas

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