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Highly constrained dipeptoid analogues containing a type II' beta-turn mimic as novel and selective CCK-A receptor ligands.
Conformationally constrained dipeptoid analogues containing the type II' beta-turn mimic (2S,5s,11bR)-2-amino-3-oxohexahydroindolizino[8,7-b]indole-5 -carboxylate framework in place of theExpand
beta-Turned dipeptoids as potent and selective CCK(1) receptor antagonists.
To improve our knowledge of the bioactive conformation of CCK(1) antagonists, we previously described that replacement of the alpha-MeTrp residue of dipeptoids with the (2S,5S,Expand
2-Oxopiperazine-Based γ-Turn Conformationally Constrained Peptides: Synthesis of CCK-4 Analogues
2-Oxopiperazine derivatives 1 have been designed as mimetics of γ-turn conformationally constrained tripeptides. The synthetic pathway devised for the preparation of both epimers of 1 at C5 involvesExpand
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
To further define the pharmacophore of the potent and selective 5-(tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based CCK(1) receptor antagonists the electronic and topographicExpand
Conformationally constrained CCK4 analogues incorporating IBTM and BTD beta-turn mimetics.
To test whether a turnlike arrangement is involved in the bioactive conformation of CCK4 analogues upon CCK1 receptor recognition, we describe the preparation of two series of CCK4 derivatives, inExpand
5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1) receptor antagonists: structural modifications at the tryptophan domain.
Analogues of the previously reported potent and highly selective CCK(1) receptor antagonist (4aS, 5R)-2-benzyl-5-(N-Boc-tryptophyl)amino-1,3-dioxoperhydropyrido-[1, 2-c]pyrimidine (2a) were preparedExpand
Pharmacological Study of IQM-97,423, a Potent and Selective CCK1 Receptor Antagonist with Protective Effect in Experimental Acute Pancreatitis
The pharmacological profile of the new CCK1 receptor antagonist IQM-97,423, (4aS,5R)-2-benzyl-5-(tert-butylaminocarbonyl-tryptophyl)amino-1,3-dioxoperhydropyrido-[1,2-c]pyrimidine, was examined in inExpand
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.
To establish structure-activity relationships a new series of analogues of the highly potent and selective CCK(1) receptor antagonistExpand
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