Design, synthesis and Na⁺/H⁺ exchanger isoform-1 inhibitory activity of feruloylagmatine analogues

In order to search for novel inhibitors of Na⁺/H⁺ exchanger isoform-1 (NHE-1), nine feruloylagmatine analogues were designed and synthesized from ferulic acid and agmatine.  The structures of the synthesized compounds were confirmed by ¹H NMR, ¹³C NMR and mass spectra, among which compounds 5f−5i were novel compounds.  The results of preliminary pharmacological test showed that some of the compounds possessed strong NHE-1 inhibitory activity, among which compounds 5a, 5b and 6c were more potent than cariporide in NHE-1 inhibition.