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.
MeSH terms
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Corticotropin-Releasing Hormone / antagonists & inhibitors*
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Crystallography, X-Ray
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Drug Design
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Humans
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Kinetics
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Models, Molecular
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Molecular Conformation
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Molecular Structure
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Pyrazoles / chemical synthesis*
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Pyrazoles / chemistry*
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Pyrazoles / pharmacology
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Pyrimidines / chemical synthesis*
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Pyrimidines / chemistry*
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Pyrimidines / pharmacology
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Receptors, Corticotropin-Releasing Hormone / antagonists & inhibitors*
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Structure-Activity Relationship
Substances
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Pyrazoles
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Pyrimidines
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Receptors, Corticotropin-Releasing Hormone
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CRF receptor type 1
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Corticotropin-Releasing Hormone