Synthesis and biological activity of partially modified retro-inverso pseudopeptide derivatives of the C-terminal tetrapeptide of gastrin

M Rodriguez, P Dubreuil, JP Bali…

Index: Rodriguez; Dubreuil; Bali; Martinez Journal of Medicinal Chemistry, 1987 , vol. 30, # 5 p. 758 - 763

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Citation Number: 74

Abstract

The effects of partial retro-inverso modifications of selected peptide bonds of the N-terminal tetrapeptide of gastrin have been studied. In some of the synthesized compounds, the phenylalanyl residue has been replaced by the (R, S)-2-benzylmalonyl, 3-phenylpropionyl, benzylcarbamoyl, or benzyloxycarbonyl moieties. All pseudopeptides showed affinity for the gastrin receptor, in vitro, with potencies varying from IC, 0= M. These compounds ...