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DU Ping, ZHANG Di, ZHANG Guo-min, REN Shu-juan, GONG Guo-qing, XU Yun-gen. Synthesis and Na+/H+ exchanger 1 inhibitory activity of substituted benzoylguanidine-trimetazidine conjugates[J]. Journal of China Pharmaceutical University, 2011, 42(1): 22-28.
Citation: DU Ping, ZHANG Di, ZHANG Guo-min, REN Shu-juan, GONG Guo-qing, XU Yun-gen. Synthesis and Na+/H+ exchanger 1 inhibitory activity of substituted benzoylguanidine-trimetazidine conjugates[J]. Journal of China Pharmaceutical University, 2011, 42(1): 22-28.

Synthesis and Na+/H+ exchanger 1 inhibitory activity of substituted benzoylguanidine-trimetazidine conjugates

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  • In order to search for drugs with protective effects against myocardial ischemic-reperfusion injury,and study the structure-activity relationship of benzoylguanidine derivatives,a novel series of 4-[4-(2,3,4-trimethoxybenzyl)piperazin-1-yl]-methyl and 4-{1-[4-(2,3,4-trimethoxy -benzyl)piperazin-1-yl]}-ethyl benzoylguanidine derivatives were designed and synthesized,and their structures were characterized by MS,IR,1H NMR.Na+/H+ exchanger 1 (NHE1) inhibitory activity of twelve target compounds was evaluated in a rat platelet swelling assay.Among all the tested compounds,the IC50 values of compounds 9b and 9c were 4.7 and 4.3 times more potent than cariporide(IC50=12.1 nmol/L),respectively.

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