Synthesis and positive inotropic activity evaluation of liguzinediol metabolites

Bioorg Med Chem Lett. 2016 Feb 1;26(3):882-884. doi: 10.1016/j.bmcl.2015.12.072. Epub 2015 Dec 21.

Abstract

2,5-Dihydroxymethyl-3,6-dimethylpyrazine (liguzinediol) has been recently discovered as a potential agent for treatment of heart failure with low safety risk. In the present study, four main metabolites of liguzinediol were synthesized and their positive inotropic activities were evaluated. Synthetic compounds were identical with the isolated metabolites of liguzinediol. Pharmacological examinations showed that the four major metabolites were not observed positive inotropic activity, and revealed that the positive inotropic activity of liguzinediol was essentially attributed to the parent agent.

Keywords: Heart failure; Liguzinediol; Metabolite; Synthesis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Blood Pressure / drug effects
  • Cardiotonic Agents / chemical synthesis*
  • Cardiotonic Agents / pharmacology
  • Cardiotonic Agents / therapeutic use
  • Heart Failure / drug therapy
  • Heart Rate / drug effects
  • Male
  • Muscle Contraction / drug effects
  • Pyrazines / chemical synthesis
  • Pyrazines / metabolism*
  • Pyrazines / pharmacology
  • Rats
  • Rats, Sprague-Dawley

Substances

  • 2,5-dihydroxymethyl-3,6-dimethylpyrazine
  • Cardiotonic Agents
  • Pyrazines