Acylhydrazones are very versatile ligands and their coordination properties can be easily tuned, giving rise to metal complexes with different nuclearities. In the last few years, we have been looking for new pharmacophores able to coordinate simultaneously two metal ions, because many enzymes have two metal ions in the active site and their coordination can be a successful strategy to inhibit the activity of the metalloenzyme. As a part of this ongoing research, we synthesized the acylhydrazone H<inf>2</inf>L and its complexes with Mg(II), Mn(II), Co(II), Ni(II), Cu(II) and Zn(II). Their characterization, both in solution - also by means of potentiometric studies - and in the solid state, evidenced the ability of the o-vanillin hydrazone scaffold to give rise to different types of metal complexes, depending on the metal and the reaction conditions. Furthermore, we evaluated both the free ligand and its metal complexes in in vitro studies against a panel of diverse DNA- and RNA-viruses. In particular, the Mg(II), Mn(II), Ni(II) and Zn(II) complexes had EC<inf>50</inf> values in the low micromolar range, with a pronounced activity against vaccinia virus.

A versatile salicyl hydrazonic ligand and its metal complexes as antiviral agents / Rogolino, D; Carcelli, M.; Bacchi, A.; Compari, C.; Contardi, Laura; Fisicaro, E.; Gatti, A.; Sechi, M.; Stevaert, A.; Naesens, L.. - In: JOURNAL OF INORGANIC BIOCHEMISTRY. - ISSN 0162-0134. - 150:(2015), pp. 9-17. [10.1016/j.jinorgbio.2015.05.013]

A versatile salicyl hydrazonic ligand and its metal complexes as antiviral agents

SECHI, Mario;
2015

Abstract

Acylhydrazones are very versatile ligands and their coordination properties can be easily tuned, giving rise to metal complexes with different nuclearities. In the last few years, we have been looking for new pharmacophores able to coordinate simultaneously two metal ions, because many enzymes have two metal ions in the active site and their coordination can be a successful strategy to inhibit the activity of the metalloenzyme. As a part of this ongoing research, we synthesized the acylhydrazone H2L and its complexes with Mg(II), Mn(II), Co(II), Ni(II), Cu(II) and Zn(II). Their characterization, both in solution - also by means of potentiometric studies - and in the solid state, evidenced the ability of the o-vanillin hydrazone scaffold to give rise to different types of metal complexes, depending on the metal and the reaction conditions. Furthermore, we evaluated both the free ligand and its metal complexes in in vitro studies against a panel of diverse DNA- and RNA-viruses. In particular, the Mg(II), Mn(II), Ni(II) and Zn(II) complexes had EC50 values in the low micromolar range, with a pronounced activity against vaccinia virus.
A versatile salicyl hydrazonic ligand and its metal complexes as antiviral agents / Rogolino, D; Carcelli, M.; Bacchi, A.; Compari, C.; Contardi, Laura; Fisicaro, E.; Gatti, A.; Sechi, M.; Stevaert, A.; Naesens, L.. - In: JOURNAL OF INORGANIC BIOCHEMISTRY. - ISSN 0162-0134. - 150:(2015), pp. 9-17. [10.1016/j.jinorgbio.2015.05.013]
File in questo prodotto:
Non ci sono file associati a questo prodotto.

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11388/168113
Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus 41
  • ???jsp.display-item.citation.isi??? 39
social impact