Synthesis and biological activity of N-(aminoiminomethyl)-1H-indole carboxamide derivatives as Na+/H+ exchanger inhibitors

DOI: 10.1248/cpb.47.1538

Source and publish data:

Chemical and Pharmaceutical Bulletin p. 1538 - 1548 (1999)

Update date:2022-07-30

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Authors:

Kitano, Masafumi

Kojima, Atsuyuki

Nakano, Kazuhiro

Miyagishi, Akira

Noguchi, Tsuyoshi

Ohashi, Naohito

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Article abstract of DOI:10.1248/cpb.47.1538

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.

Full text of DOI:10.1248/cpb.47.1538

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