Synthesis and Na +/H + exchanger inhibitory activity of benzoylguanidine derivatives
European Journal of Medicinal Chemistry(2011)
Abstract
Twenty-two compounds of substituted benzoylguanidine derivatives were designed and synthesized as potent NHE1 inhibitors. Twelve compounds showed more potent NHE1 inhibitory activity than cariporide. The activities of compounds 7e, 7h and 7j (IC50=0.073±0.021, 0.084±0.012 and 0.068±0.021nmol/L, respectively) were two orders of magnitude higher than that of cariporide (30.7±2.5nmol/L). Myocardial cells in vitro screening showed 7j had highlighted protective effect on cardiomyocytes subjected to hypoxia/reoxygenation. Thus it is valuable for further investigation.
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Key words
Na+/H+ exchanger inhibitors,Myocardial ischemic–reperfusion injury,Benzoylguanidine derivatives
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