Issue 8, 2018

Design, synthesis and biological profile of mixed opioid agonist/N-VGCC blocker peptides

Abstract

In this paper we reported the synthesis and the in vitro and the in vivo biological evaluation of linear pseudo-peptides incorporating the N-VGCC blocker tripeptide Phe-NMe-Leu-Tyr(OBz)-NtBu and the biphalin pharmacophore Tyr-D-Ala-Gly-Phe. The novel sequences have been designed by using amino acids of different length to join the two pharmacophores and explore the structure–activity relationships of the novel compounds.

Graphical abstract: Design, synthesis and biological profile of mixed opioid agonist/N-VGCC blocker peptides

Supplementary files

Article information

Article type
Letter
Submitted
14 Dec 2017
Accepted
02 Mar 2018
First published
05 Mar 2018

New J. Chem., 2018,42, 5656-5659

Design, synthesis and biological profile of mixed opioid agonist/N-VGCC blocker peptides

A. Stefanucci, E. Novellino, G. Macedonio, M. P. Dimmito, S. Mirzaie, F. Caldas Cardoso, R. Lewis, F. Zádor, A. I. Erdei, S. Dvorácskó, C. Tömböly, S. Benyhe, S. Pieretti, P. Minosi and A. Mollica, New J. Chem., 2018, 42, 5656 DOI: 10.1039/C7NJ04969B

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