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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
Quinazolinone derivatives: synthesis and binding evaluation on cholecystokinin receptors.
TLDR
The obtained results confirm that the 4(3H)-quinazolinone nucleous represent a useful template for the development of selective CCK-B receptor ligands. Expand
Quinolone derivatives: synthesis and binding evaluation on cholecystokinin receptors.
A series of 1,2-dihydro-4-phenylquinolin-2-one-3-carboxylic acid and of 3-amino-4-phenylcarbostyril derivatives were synthesized and examined for their CCK receptor affinities. These compoundsExpand
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
Anthranilic acid based CCK1 receptor antagonists: blocking the receptor with the same 'words' of the endogenous ligand.
TLDR
It is demonstrated that the CCK(1) receptor affinity depends on the nature of the aminoacidic side chain as well as that the free carboxy group of the alpha-aminoacids is crucial for the binding. Expand
Anthranilic acid based CCK1 receptor antagonists and CCK-8 have a common step in their "receptor desmodynamic processes".
TLDR
Conformational studies, using NMR and energy minimization procedures, have allowed formulation of a new hypothesis on the CCK(1)-R binding mode of the anthranilic antagonists. Expand
Twenty years of non-peptide CCK1 receptor antagonists: all that glitters is not gold
During the last 20 years, pharmaceutical industry and academic efforts have led to several structurally unrelated classes of non-peptide cholecystokinin-1 receptor (CCK1-R) antagonists. Due to theExpand
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