Synthesis and anti-inflammatory activity of new 1,2,4-triazole derivatives

Bioorg Med Chem Lett. 2015 Jul 1;25(13):2664-7. doi: 10.1016/j.bmcl.2015.04.079. Epub 2015 Apr 30.

Abstract

The series of new 1,2,4-triazole derivatives with methacrylic acid moiety were synthesized and characterized by NMR and IR spectroscopy as well as X-ray crystallography. The influence of newly synthesized compounds on the inflammation on the level of cytokine production and the proliferation of human peripheral blood mononuclear cells (PBMC) were experimentally evaluated. Obtained triazoles showed antiproliferative activity and diverse effects on cytokine production. Two compounds demonstrated potentially anti-inflammatory activity and comparable effects with ibuprofen.

Keywords: Amidrazone; IL-10; IL-6; Ibuprofen; PBMC; Proliferation; TNF-α; Triazole.

MeSH terms

  • Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis*
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Cell Proliferation / drug effects
  • Crystallography, X-Ray
  • Cytokines / biosynthesis
  • Drug Design
  • Humans
  • In Vitro Techniques
  • Leukocytes, Mononuclear / cytology
  • Leukocytes, Mononuclear / drug effects*
  • Leukocytes, Mononuclear / immunology
  • Magnetic Resonance Spectroscopy
  • Spectrophotometry, Infrared
  • Structure-Activity Relationship
  • Triazoles / chemical synthesis*
  • Triazoles / chemistry
  • Triazoles / pharmacology*

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Cytokines
  • Triazoles