Synthesis and Preliminary Evaluation of Danshensutetramethylpyrazine Derivatives

In this study, a series of novel Danshensu-tetramethylpyrazine derivatives were synthesized, and their cardioprotective effects and water solubility in vitro were evaluated. The results illustrated that esterification at phenol hydroxyl group was superior to etherification in biological activity. The modification with short-chain fatty acids at the alcoholic hydroxyl group should be avoided. In addition, the introduction of amino acids to the phenol hydroxyl group and the alcoholic hydroxyl group may be a useful strategy for improving the water solubility. This work provides valuable information in structure-activity relationship for further development of DSS derivatives as cardioprotective agents.