Synthesis and antioxidant activity of 3-(Pyridin-2-ylmethyl)-1,3-thiazinan(thiazolidin)-4-ones

J Biochem Mol Toxicol. 2014 Sep;28(9):425-32. doi: 10.1002/jbt.21581. Epub 2014 Jun 17.

Abstract

The antioxidant properties of two series of thiazolidinones and thiazinanones were reported. The novel six-membered thiazinanones were synthesized from the efficient multicomponent reaction of 2-picolylamine (2-aminomethylpyridine), arenaldehydes, and the 3-mercaptopropionic acid in moderate to excellent yields. These novel compounds were fully identified and characterized by NMR and GC-MS techniques. In vitro antioxidant activities of all compounds were evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azinobis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) tests. The antioxidant assays of thiobarbituric acid reactive species and total thiol content levels in the cerebral cortex and liver of rats were also performed. Thiazinanone 5a showed the best radical scavenging activity in DPPH and ABTS tests, as well as reduced lipid peroxidation and increased total thiol group in biological systems. Altogether, the results may be considered a good starting point for the discovery of a new radical scavenger.

Keywords: Antioxidant; Cerebral cortex; Liver; Thiazinanones; Thiazolidinones.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Free Radical Scavengers* / chemical synthesis
  • Free Radical Scavengers* / chemistry
  • Free Radical Scavengers* / pharmacology
  • Heterocyclic Compounds, 3-Ring* / chemical synthesis
  • Heterocyclic Compounds, 3-Ring* / chemistry
  • Heterocyclic Compounds, 3-Ring* / pharmacology
  • Lipid Peroxidation / drug effects*
  • Rats
  • Rats, Wistar

Substances

  • Free Radical Scavengers
  • Heterocyclic Compounds, 3-Ring