947243-87-0Relevant academic research and scientific papers
Design, synthesis and biological evaluation of novel ligustrazinylated derivatives as potent cardiovascular agents
Chen, Hongfei,Li, Guoning,Zhan, Peng,Guo, Xiuli,Ding, Qian,Wang, Shouxun,Liu, Xinyong
, p. 827 - 832 (2013/08/26)
A series of novel ligustrazinylated derivatives was designed, synthesized and evaluated for their protective effects against hydrogen peroxide (H 2O2)-induced oxidative damage on ECV-304 cells, and also assayed for their inhibition effects on platelet aggregation induced by adenosine diphosphate (ADP). Biological results showed that some compounds exhibited moderate to potent activities in one or both of the assays. Among these compounds, compound 3 displayed the highest protective effect on the damaged ECV-304 cells with EC50 = 0.0040 mM, and compound 1c was the most active platelet aggregation inhibitor (EC50 = 0.40 mM). Structure-activity relationships were briefly discussed. The Royal Society of Chemistry 2013.
Synthesis of novel ligustrazine derivatives as Na+/H+ exchange inhibitors
Ren, Mei,Dong, Jin,Xu, Yungen,Wen, Nan,Gong, Guoqing
, p. 2727 - 2736 (2011/08/06)
A novel series of 3,5,6-trimethylpyrazine-2-methoxy (or methylamino) substituted benzoyl-guanidine derivatives were designed and synthesized as Na+/H+ exchange (NHE) inhibitors. In this study, compounds with electron-withdrawing substituents on the benzene ring seemed to improve NHE-1 inhibitory activities. Compounds 6d, 6k, and 6l were found to be potent inhibitors of NHE-1 (IC50=3.0±1.6, 3.0±1.4, and 1.6±0.4nmol/l, resp.). Furthermore, they showed a remarkable reduction of infarct size in the rat myocardial infarction model in vivo.
