An overview on structural modifications of ligustrazine and biological evaluation of its synthetic derivatives

Ligustrazine, a natural product from Rhizoma Chuanxiong containing a pyrazine ring, has been widely used in China for treatment of heart diseases. Because of its remarkable effects but rapid metabolism, studies on structural modification of ligustrazine have attracted much attention. Ligustrazine synthetic derivatives reported in recent decades can be divided into ethers, esters, amides and piperazines, olefins, and others. These derivatives are mainly derived from four primary intermediates. The lack of a comprehensive and recent review on this topic prompted us to gather more new information. This paper is a compilation of almost all of the 304 synthetic ligustrazine derivatives we encountered; the information included is expected to be of benefit to further studies of ligustrazine.