Synthesis and protective effect of new ligustrazine-benzoic acid derivatives against CoCl2-induced neurotoxicity in differentiated PC12 cells

Molecules. 2013 Oct 18;18(10):13027-42. doi: 10.3390/molecules181013027.

Abstract

A series of novel ligustrazine-benzoic acid derivatives were synthesized and evaluated for their protective effect against cobalt chloride-induced neurotoxicity in differentiated PC12 cells. Combining hematoxylin and eosin staining, we found compound that (3,5,6-trimethylpyrazin-2-yl)methyl 3-methoxy-4-[(3,5,6-trimethylpyrazin-2-yl)methoxy]benzoate (4a) displayed promising protective effect on the proliferation of the injured PC12 cells (EC50 = 4.249 µM). Structure-activity relationships are briefly discussed.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Benzoates / chemical synthesis*
  • Benzoates / pharmacology
  • Cell Differentiation
  • Cell Proliferation
  • Cell Survival / drug effects
  • Cobalt / toxicity
  • Inhibitory Concentration 50
  • Neurons / drug effects
  • Neurons / physiology*
  • Neuroprotective Agents / chemical synthesis
  • Neuroprotective Agents / pharmacology
  • PC12 Cells
  • Pyrazines / chemistry*
  • Rats

Substances

  • Benzoates
  • Neuroprotective Agents
  • Pyrazines
  • Cobalt
  • cobaltous chloride
  • tetramethylpyrazine