Recent advances in the structural modification of ligustrazine: Cerebro- and cardiovascular activity of ligustrazine derivatives

Abstract

Recent advances in the structural modification of ligustrazine and studies on the bioactivities of ligustrazine derivatives are reviewed in this article. Due to its rapid metabolism and short half-life, ligustrazine is not suitable for application in clinical practice. Derivatives of ligustrazine were therefore designed and synthesized, including ether, amine, amide, hydrocarbon and deuterated derivatives of ligustrazine and ester and alcohol derivatives of 2-hydroxymethyl-3,5,6-trimethylpyrazine, an active metabolite of ligustrazine. Some of these compounds present better cerebro- arid cardiovascular activities and more favorable pharmacokinetic properties compared to the parent compound.