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

Azzurra Stefanucci, Ettore Novellino, Giorgia Macedonio, Marilisa Pia Dimmito, Sako Mirzaie, Fernanda Caldas Cardoso, Richard Lewis, Ferenc Zádor, Anna I. Erdei, Szabolcs Dvorácskó, Csaba Tömböly, Sandor Benyhe, Stefano Pieretti, Paola Minosi, Adriano Mollica

Research output: Contribution to journalArticle

2 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)5656-5659
Number of pages4
JournalNew Journal of Chemistry
Volume42
Issue number8
DOIs
Publication statusPublished - Jan 1 2018

ASJC Scopus subject areas

  • Catalysis
  • Chemistry(all)
  • Materials Chemistry

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    Stefanucci, A., Novellino, E., Macedonio, G., Dimmito, M. P., Mirzaie, S., Caldas Cardoso, F., Lewis, R., Zádor, F., Erdei, A. I., Dvorácskó, S., Tömböly, C., Benyhe, S., Pieretti, S., Minosi, P., & Mollica, A. (2018). Design, synthesis and biological profile of mixed opioid agonist/N-VGCC blocker peptides. New Journal of Chemistry, 42(8), 5656-5659. https://doi.org/10.1039/c7nj04969b