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C-terminal anthranoyl-anthranilic acid derivatives and their evaluation on CCK receptors.
TLDR
A series of C-terminal anthranoyl-anthranilic acid derivatives arising from a strict bond disconnection approach of asperlicin were synthesized and examined for their CCK receptor affinities, confirming that the anthranilic Acid dimer represents a useful template for the development of selective CCK-A receptor ligands. Expand
Synthesis of new anthranilic acid dimer derivatives and their evaluation on CCK receptors.
TLDR
A new series of anthranilic acid dimer derivatives, characterized by the presence of the tryptophan residue in the C-terminus of the dimer, is described, which exhibited an improved affinity for the CCK-A receptor in comparison to that of either, the N-unsubstituted derivative and asperlicin. Expand
Anthranilic acid derivatives: a new class of non-peptide CCK1 receptor antagonists.
TLDR
On the basis of the main pharmacophoric groups of the obtained new lead compound (1) (coded VL-0395) a receptor binding hypothesis has been provided and simplified analogues reducing the anthranilic acid dimer to a monomer are proposed. Expand
Anthranilic acid based CCK1 antagonists: the 2-indole moiety may represent a "needle" according to the recent homonymous concept.
TLDR
The obtained results confirm that this group establishes very specific interactions with this receptor sub-site and may be viewed as a "needle" group. Expand
N-terminal anthranoyl-phenylalanine derivatives as CCK1 receptor antagonists: the final approach.
TLDR
Improvements for both affinity and selectivity towards CCK1 receptors have been accomplished through introduction of the fluoro substituent at C-5 and C-7 position of the indole ring together with the appropriate configuration of the aminoacidic chiral center. Expand
Anthranilic acid based CCK1 receptor antagonists: preliminary investigation on their second "touch point".
TLDR
The result of this work is the identification of a new CCK ligand, which possesses an affinity one order of magnitude greater than the lead and points out how the hypothesized receptorial pocket which accommodates the Phe residue allows much more structural modification than that interacting with the N-terminal group. Expand
Synthesis of N-terminal substituted anthranilic acid dimer derivatives for evaluation on CCK receptors.
TLDR
A series of new N-substituted anthranilic acid dimer derivatives having a C-terminal Phe residue was synthesized and evaluated for their affinity for CCK receptors, characterized by about 1000-fold greater affinity forCCK-A receptor than the C- terminal tetrapeptide. Expand
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