Abstract
A new series of 4-substituted pipecolic acid derivatives was prepared and incorporated into dipeptoids. The resulting products behave as moderately potent CCK-B antagonists but their constrained structure and its comparison with structurally related compounds yield valuable information about the conformational requirements for optimal recognition of the CCK-B receptor by antagonists.
MeSH terms
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Animals
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CHO Cells
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Cerebral Cortex / metabolism
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Cholecystokinin / metabolism*
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Cricetinae
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Guinea Pigs
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In Vitro Techniques
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Models, Molecular
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Molecular Conformation
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Pancreas / metabolism
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Pipecolic Acids / chemical synthesis*
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Pipecolic Acids / chemistry
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Pipecolic Acids / pharmacology
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Protein Conformation
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Rats
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Receptor, Cholecystokinin B
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Receptors, Cholecystokinin / antagonists & inhibitors*
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Structure-Activity Relationship
Substances
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Pipecolic Acids
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Receptor, Cholecystokinin B
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Receptors, Cholecystokinin
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Cholecystokinin