Novel constrained CCK-B dipeptoid antagonists derived from pipecolic acid

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 con...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1998-06, Vol.8 (11), p.1419-1424
Main Authors: BELLIER, B, DA NASCIMENTO, S, MEUDAL, H, GINCEL, E, ROQUES, B. P, GARBAY, C
Format: Article
Language:English
Subjects:
Animals
Biological and medical sciences
Cerebral Cortex - metabolism
CHO Cells
Cholecystokinin - metabolism
Cricetinae
Guinea Pigs
In Vitro Techniques
Life Sciences
Medical sciences
Models, Molecular
Molecular Conformation
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pancreas - metabolism
Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems
Pharmacology. Drug treatments
Pipecolic Acids - chemical synthesis
Pipecolic Acids - chemistry
Pipecolic Acids - pharmacology
Protein Conformation
Rats
Receptor, Cholecystokinin B
Receptors, Cholecystokinin - antagonists & inhibitors
Structure-Activity Relationship
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Summary: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(98)00231-5