Journal of Medicinal Chemistry p. 769 - 774 (1985)
Update date:2022-08-05
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Salvadori, Severo
Marastoni, Mauro
Balboni, Gianfranco
Sarto, Gian Pietro
Tomatis, Roberto
We studied the effect of partial retro-inverso modification of selected peptide bonds of N-terminal tetrapeptide analogues of dermorphin (H-Tyr-D-Ala-Phe-Gly-Tyr-Pro-Ser-NH2).Among the 14 compounds synthesized and tested for opioid activity, some tetrapeptides have the C-terminus carrying different amide moieties; retromodifications concern the Phe-Gly bond (Ia-f) and/or the C-terminal carboxamide function (IIIa-d, IIa-d).All pseudotetrapeptide derivatives showed opioid activity in vitro and in vivo.The most potent compounds (II) have a biological potency comparable with that of the original tetrapeptides in the guinea pig ileum preparation and in the mouse tail-flick test after intracerebral or subcutaneous administration.
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