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 conformational requirements for optimal recognition of the CCK-B receptor by antagonists.
Bellier
B
B
Département de Pharmacochimie Moléculaire et Structurale, INSERM U266, CNRS URA D1500, UFR des Sciences Pharmaceutiques et Biologiques, Paris, France.
Da Nascimento
S
S
Meudal
H
H
Gincel
E
E
Roques
B P
BP
Garbay
C
C
D000818:Animals; D016466:CHO Cells; D002540:Cerebral Cortex / Q000378:metabolism; D002766:Cholecystokinin / Q000378:metabolism*; D006224:Cricetinae; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008958:Models, Molecular; D008968:Molecular Conformation; D010179:Pancreas / Q000378:metabolism; D010875:Pipecolic Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011487:Protein Conformation; D051381:Rats; D043887:Receptor, Cholecystokinin B; D011949:Receptors, Cholecystokinin / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D010875:Pipecolic Acids; D043887:Receptor, Cholecystokinin B; D011949:Receptors, Cholecystokinin; D002766:Cholecystokinin