In vitro and in vivo studies of the dermally absorbed Cu(II) complexes of N5O2 donor ligands – Potential anti-inflammatory drugs

Sebusi Odisitse, Graham E. Jackson

Research output: Contribution to journalArticle

10 Citations (Scopus)

Abstract

Copper complexes of N,N′-di(aminoethylene)-2,6-pyridinedicarbonylamine and bis-(N,N-dimethylethyl)-2,6-pyridinedicarboxamide have been studied by glass electrode potentiometry, NMR, UV and IR spectroscopy as potential anti-inflammatory agents for the alleviation of inflammation associated with rheumatoid arthritis. The protonation and formation constants with Cu(II), Zn(II) and Ca(II), determined at 25 °C and an ionic strength of 0.15 mol dm-3 were used to calculate the copper plasma mobilizing index of the ligands. Spectroscopic studies suggested that metal ion complexation promotes deprotonation and coordination of the amide nitrogens resulting in overall tetragonal distorted copper complexes. Bio-distribution and dermal absorption studies showed the complexes to have relatively long biological half-lives with 50% of the injected dose remaining in the body 24 h after administration.

Original languageEnglish
Pages (from-to)125-135
Number of pages11
JournalInorganica Chimica Acta
Volume362
Issue number1
DOIs
Publication statusPublished - 2009

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Copper
drugs
Anti-Inflammatory Agents
Ligands
copper
ligands
Pharmaceutical Preparations
glass electrodes
potentiometric analysis
arthritis
Deprotonation
Protonation
Ionic strength
Ultraviolet spectroscopy
Complexation
Amides
half life
amides
Nuclear magnetic resonance spectroscopy
Metal ions

All Science Journal Classification (ASJC) codes

  • Physical and Theoretical Chemistry
  • Inorganic Chemistry
  • Materials Chemistry

Cite this

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abstract = "Copper complexes of N,N′-di(aminoethylene)-2,6-pyridinedicarbonylamine and bis-(N,N-dimethylethyl)-2,6-pyridinedicarboxamide have been studied by glass electrode potentiometry, NMR, UV and IR spectroscopy as potential anti-inflammatory agents for the alleviation of inflammation associated with rheumatoid arthritis. The protonation and formation constants with Cu(II), Zn(II) and Ca(II), determined at 25 °C and an ionic strength of 0.15 mol dm-3 were used to calculate the copper plasma mobilizing index of the ligands. Spectroscopic studies suggested that metal ion complexation promotes deprotonation and coordination of the amide nitrogens resulting in overall tetragonal distorted copper complexes. Bio-distribution and dermal absorption studies showed the complexes to have relatively long biological half-lives with 50{\%} of the injected dose remaining in the body 24 h after administration.",
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In vitro and in vivo studies of the dermally absorbed Cu(II) complexes of N5O2 donor ligands – Potential anti-inflammatory drugs. / Odisitse, Sebusi; Jackson, Graham E.

In: Inorganica Chimica Acta, Vol. 362, No. 1, 2009, p. 125-135.

Research output: Contribution to journalArticle

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