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beta-Turned dipeptoids as potent and selective CCK(1) receptor antagonists.
TLDR
It is proposed that the presence of a beta-turn-like conformation within the peptide backbone of dipeptoids could contribute to their bioactive conformation at the CCK(1) receptor subtype.
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Conformationally constrained CCK4 analogues incorporating IBTM and BTD beta-turn mimetics.
TLDR
The structure-conformation-activity relationship study in the IBTM series has shown some essential requirement of these CCK4 derivatives to favorably interact with CCK1 receptors, including the adoption of turnlike conformations and the presence of an L-Phe residue and a C-terminal carboxamide moiety.
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Highly constrained dipeptoid analogues containing a type II' beta-turn mimic as novel and selective CCK-A receptor ligands.
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2-Oxopiperazine-Based γ-Turn Conformationally Constrained Peptides: Synthesis of CCK-4 Analogues
TLDR
Results suggest the absence of a γ-turn in the bioactive conformation of the C-terminal tripeptide of CCK-4.
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5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1) receptor antagonists: structure-activity relationship studies on the central…
TLDR
The results of the evaluation of the new analogues as CCK receptor ligands showed that, whereas replacement of oxygen with sulfur is allowed, reduction of the 1- or 3-oxo groups or the contraction of the fused piperidine ring lead to the complete loss of binding affinity at CCK(1) receptors.
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Highly Constrained Dipeptoid Analogues Containing a Type II′ β-Turn Mimic as Novel and Selective CCK-A Receptor Ligands.
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Pharmacological Study of IQM-97,423, a Potent and Selective CCK1 Receptor Antagonist with Protective Effect in Experimental Acute Pancreatitis
TLDR
The pyridopyrimidine derivative IQM-97,423 is a potent and highly selective CCK1 receptor antagonist with preventive effects in two experimental models of acute pancreatitis and a potential therapeutic interest.
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Effects of the Incorporation of IBTM β‐Turn Mimetics into the Dipeptoid CCK1 Receptor Agonist PD 170292.
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5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1) receptor antagonists: structural modifications at the tryptophan domain.
TLDR
Replacement of this acid-labile group with 3, 3-dimethylbutyryl or tert-butylaminocarbonyl conferred acid stability to analogues 14a and 15a, which retained a high potency and selectivity in binding to CCK(1) receptors, as well as an in vivo antagonist activity against the acute pancreatitis induced by caerulein in rats.
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5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1)receptor antagonists: structure-activity relationship studies on the substituent at N2-position.
TLDR
The results confirm the (4aS,5R)-stereochemistry at the central bicyclic skeleton as an essential structural requirement for potent binding to this receptor subtype.
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