Synthesis and Biological Activity of N-(Aminoiminomethyl)-1H-indole Carboxamide Derivatives as Na⁺/H⁺ Exchanger Inhibitors

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A series of N-(aminoiminomethyl)-1H-indole carboxamide derivatives were synthesized and their inhibitory potencies against the Na⁺/H⁺ exchanger were measured. Variation of the carbonylguanidine group at the 2- to 7-position of the indole ring system showed that a substitution at the 2-position improved the Na⁺/H⁺ exchanger inhibitory activity the most in vitro. This led to the synthesis and evaluation of an extensive series of N-(aminoiminomethyl)-1H-indole-2-carboxamide derivatives. Derivatives having an alkyl or substituted alkyl group at the 1-position of the indole ring system showed higher levels of in vitro activities. N-(aminoiminomethyl)-1-(2-phenylethyl)-1H-indole-2-carboxamide (49) had the strongest activity.