947243-97-2Relevant articles and documents
Synthesis of novel ligustrazine derivatives as Na+/H+ exchange inhibitors
Ren, Mei,Dong, Jin,Xu, Yungen,Wen, Nan,Gong, Guoqing
experimental part, 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.