Synthesis and Na+/H+ exchanger inhibitory activity of benzoylguanidine derivatives

►We synthesized 22 compounds as potent NHE1 inhibitors. ►All the compounds were evaluated for NHE1 inhibitory activity screening. ►12 Compounds showed more potent NHE1 inhibitory activity than cariporide. ►3 Compounds were two orders of magnitude higher than that of cariporide. ►1 Compound had highlighted protective effect on cardiomyocytes.